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Validated All-in-One™ qPCR Primer for ABCB1(NM_001348945.2) Search again
Product ID:
HQP158607
(click here to view gene annotation page)
Powered by BiozSpecies:
Human
Symbol:
Alias:
ABC20, CD243, CLCS, GP170, MDR1, P-GP, PGY1, p-170
Gene Description:
ATP binding cassette subfamily B member 1
Target Gene Accession:
NM_001348945.2(click here to view gene page)
Estimated Delivery:
Approximately 1-3 weeks, but may vary. Please email sales@genecopoeia.com or call 301-762-0888 to confirm ETA.
Important Note:
By default, qPCR primer pairs are designed to measure the expression level of the splice variant (accession number) you selected for this gene WITHOUT consideration of other possible variants of this gene. If this gene has multiple variants, and you would like to measure the expression levels of one particular variant, multiple variants, or all variants, please contact us for a custom service project at inquiry@genecopoeia.com.
Summary
The membrane-associated protein encoded by this gene is a member of the superfamily of ATP-binding cassette (ABC) transporters. ABC proteins transport various molecules across extra- and intra-cellular membranes. ABC genes are divided into seven distinct subfamilies (ABC1, MDR/TAP, MRP, ALD, OABP, GCN20, White). This protein is a member of the MDR/TAP subfamily. Members of the MDR/TAP subfamily are involved in multidrug resistance. The protein encoded by this gene is an ATP-dependent drug efflux pump for xenobiotic compounds with broad substrate specificity. It is responsible for decreased drug accumulation in multidrug-resistant cells and often mediates the development of resistance to anticancer drugs. This protein also functions as a transporter in the blood-brain barrier. [provided by RefSeq].
Gene References into function
- Overall, our data suggest that the MDR1 (official symbol of ABCB1) 3' UTR does not behave as an active destabilizing element in HepG2 cells.
- Oligonucleotides inhibit mdr1 induction in Hela cells.
- serum concentration of digoxin after single oral administration was lower in the subjects harboring a mutant allele (C3435T) at exon 26 of the MDR1 gene
- Expression in nasopharyngeal carcinoma
- Expression in nasopharyngeal carcinoma
- No apparent changes were observed between controls and Down Syndrome in levels of Pgp in all brain regions examined.
- role in transporting endogenous opioid peptides
- The in vitro induction of apoptosis was not associated with expression of p-gp expression in acute lymphoblastic leukaemia and non-Hodgkin's lymphoma in children.
- Precipitous release [observed] of methyl-CpG binding protein 2 and histone deacetylase 1 from the methylated human multidrug resistance gene (MDR1) on activation
- cysteine-scanning mutagenesis and cross-linking studies to identify residues that are exposed to the drug-binding site upon vanadate trapping
- involved in the drug resistance mechanism of tumors
- findings suggest that Tax-related drug resistance of ATL cells is due to LRP and not MDR1, as reported previously.
- Significance of P-glycoprotein expression in childhood malignant tumors: correlation between the level of P-glycoprotein expression and tumor histology, clinical outcome, use of therapy, relapse rate and metastatic disease was determined
- Induction of human MDR1 gene expression by 2-acetylaminofluorene is mediated by effectors of the phosphoinositide 3-kinase pathway that activate NF-kappaB signaling.
- Functional MDR1 polymorphisms (G2677T and C3435T) and TCF4 mutations in colorectal tumors with high microsatellite instability
- no difference of expression between diagnosis and relapse of AML; not associated with clinical resistant disease in AML
- The misfolding of P-gp in E. coli is due to the misrecognition of multiple P-gp sequences as topogenic signals. Thus, the alternative transmembrane topologies reported for P-gp in E. coli are artefacts of the heterologous expression system used.
- Review.Functional polymorphisms of the human multidrug resistance (MDR1) gene: correlate with P glycoprotein expression and activity in vivo.
- Review. In the current model, both MDR1 catalytic sites are active and ATP is hydrolyzed alternatively, triggering conformational changes resulting in drug transport at one site and re-setting the initial hig-affinity conformation at the other.
- Association of specific cytogenetic aberrations with mdr1 gene expression in adult myeloid leukemia
- mutations and functional polymorphisms in multidrug resistance 1 gene: correlation with microsatellite instability and lymphoid infiltration in colorectal cancers
- The known functional MDR1 gene polymorphisms are not major determinants of P-glycoprotein function in CD34+ hematopoietic stem cells.
- hydrolysis of linker region modulates ATPase function
- Common MDR1 coding polymorphisms result in P-gps with a cell surface distribution and function similar to wild-type P-gp.
- Introduction of the most common cystic fibrosis mutation (Delta F508) into human P-glycoprotein disrupts packing of the transmembrane segments
- Coexpression of P-glycoprotein, Ets-1, and p53 in oral carcinoma is associated with poor prognosis
- directly interacts with several tyrosine kinase inhibitors
- Association of the P-glycoprotein transporter MDR1(C3435T) polymorphism with the susceptibility to renal epithelial tumors. Association between T allele frequency and the occurrence of tumors. The highest risk for homozygote TT allele carriers.
- Stimulation of T cells resulted in the preferential retention of the photosensitizer TH9402 transported by P-GP in activated T cells, both CD4+ and CD8+.
- The preferential expression of a mutant allele of the amplified MDR1 (ABCB1) gene has been investigated in drug-resistant variants of human sarcoma.
- MRP1 is demonstrated to play a constitutive role in the intrinsic chemoresistance of gliomas and their normal cell counterpart.
- MDR1 protein expression is an independent predictor of complete remission in newly diagnosed adult acute lymphoblastic leukemia.
- multidrug transporter, P-glycoprotein, actively mediates cholesterol redistribution in the cell membrane
- Review. Pgp has a drug-independent role in the apoptosis inhibition of AML blasts perhaps by modulation of cytokine efflux, signalling lipids and intracellular pH.
- Results show efficient GTP hydrolysis by the N-terminal nucleotide binding domain (NBD1) of Pgp, and a minor role of phosphorylation in the control of Pgp NBD1 ATPase activity.
- data strongly support the hypothesis that strong LD between the neutral SNP exon 26 3435C>T and a nearby unobserved causal SNP underlies the observed associations between the neutral SNP and MDR1 functional differences.
- the C3435T polymorphism of MDR1 was suggested to correlate with the enterocyte expression of CYP3A4 rather than Pgp linking unknown genetic variation in CYP3A4 gene.
- correlation of gene expression with histopathological findings and clinical outcome in ovarian and breast cancer patients
- MDR1 exon 21 and exon 26 polymorphisms are related to steroid weaning in a pediatric heart transplant population
- Immunohistochemical analyses of Pgp or MRP expression are potential tools for predicting patients' chemotherapy response in SCLC
- MDR1 gene polymorphisms affect therapy outcome in acute myeloid leukemia patients.
- common residues are involved in the binding of structurally different drug substrates to MRP1 and it has a common drug-binding site
- cysteine-scanning mutagenesis and cross-linking analysis demonstrate that the signature sequence in each nucleotide-binding domain (NBD) is close to the site in the opposing NBD
- These results indicates that (-)epicatechin may bind to and activate an allosteric site that enhances P-glycoprotein overall function or efficiency.
- Expression of polymorphism in this gene is related to Parkinson disease.
- Deposition of Alzheimer beta amyloid is inversely correlated with expression of this protein in the brains of elderly non-demented humans.
- MDR1 gene is upregulated in arsenic trioxide-resistant acute promyelocytic leukemia
- REVIEW: potential signaling pathways leading to modulation of mdr1 expression in acute myeloid leukemia and, particularly, potential possibilities of Ras influence on mdr1 activity
- influence of MDR1 polymorphisms on P-glycoprotein tissue expression, drug disposition, treatment outcome and disease risk [rewiev]
- relationship between soluble resistance-related calcium-binding protein (sorcin) gene and multidrug resistance gene (mdr1), and their significance in clinical drug resistance and prognosis of acute myeloid leukemia (AML)
- Glutathione plays a role in the intermediate structural states of this protein involved in drug transport.
- importance of the conserved Walker B glutamate residues, 556 and 1201, for the completion of the catalytic cycle of ATP hydrolysis by human protein
- P-gp expression may be considered as an index for evaluating multidrug resistance, guiding drug use, and judging prognosis of the patients with metastatic breast carcinoma.
- Transcriptional regulation of the gene at the level of the inverted MED-1 promoter region
- Association between the C3435T MDR1 gene polymorphism and susceptibility for ulcerative colitis. Increased frequencies of the 3435T allele and the 3435TT genotype in ulcerative colitis.
- role in drug resistance in cancer cells induced by NF-kappa B
- MDR1 function may be effected by St.John's wort in healthy subjects.
- Nuclear expression of YB-1 protein correlates with P-glycoprotein expression in human breast carcinoma.
- RNA expression of this protein in breast cancer correlates with response to chemotherapy.
- Contrary to adult patients, expression of this multidrug resistance gene fails to define a poor prognostic group in childhood AML.
- Function of the ABC transporters, P-gp, multidrug resistance protein and BCRP, in minimal residual disease in acute myeloid leukemia
- packing of the TM segments in the drug-binding site of P-glycoprotein (P-gp) is changed when P-gp binds to a particular substrate
- electrically passive anion transport via MDR-TCBD fusion protein, but only at low [ATP]
- Some polychlorinated biphenyls congeners can bind to the MDR1 transporter; however, they may not be transported by it
- C3435T SNP of this gene predicts response to preoperative chemotherapy in locally advanced breast cancer
- This identifies a genetic factor associated with resistance to antiepileptic drugs. Patients with drug-resistant epilepsy were more likely to have the CC genotype at ABCB1 3435 than the TT genotype than patients with drug-responsive epilepsy.
- Covalent modification of I306C affects the long range linkage between the drug-binding site and the distal ATP-binding sites.
- polymorphisms possibly linked to genetic factors in Parkinson's disease
- structural model for the open conformation of the mdr1 P-glycoprotein
- MDR1 expression was inhibited by two small interfering RNA constructs.
- Results describe a Saccharomyces cerevisiae expression system for the multidrug-resistance protein 1 (MRP1) allowing for rapid generation of mutants and yielding milligram amounts of protein.
- P-gp per se has little effect on membrane fluidity or membrane potential, and it does not have H(+) pump activity.
- Data show that the MycN protein activates MDR1 transcription both in exogenous transient MYCN-transfected cells and in endogenous metastatic neuroblasts.
- Transcription factor c-Jun plays a principal role in down-regulation of mdr-1 expression and induction of apoptosis in salvicine-treated human MDR K562/A02 cells.
- the common drug-binding pocket in P-gp is large enough to accommodate both verapamil and TMEA simultaneously, and the substrates must occupy different regions in the common drug-binding pocket
- Pgp assumes at least two distinct conformational states, which catalyze two ATP hydrolysis events in the drug transport cycle, and the linker region mediates the transition between these two states of Pgp.
- human P-glycoprotein is activated by methanethiosulfonate derivatives of rhodamine and verapamil at different sites
- 9 haplotypes exists in the Japanese population
- An atomic detail model of P-glycoprotein.
- REVIEW: biology, genetics, and biochemistry of P-glycoprotein
- ABCB1 mutations are important for plasma concentrations and central nervous system actions of the opiod loperamide.
- Homozygosity for the ABCB1 allele is associated with reduced risk of chronic renal dysfunction among liver transplantation patients receiving an immunosuppressive regimen containing calcineurin inhibitors.
- The ABCB1 variant type showed a lower incidence of osteonecrosis of the femoral head.
- association of the common Ala893 polymorphism with inflammatory bowel disease specifically and, more broadly, provides additional support for its contribution to interindividual pharmacogenetic variation.
- Data show that T2677T and T3435T alleles of MDR1 are not a factor predisposing to lymphoproliferative diseases, but they determine the efficiency of chemotherapy.
- The amino-terminal and carboxy-proximal functional boundaries of MDR1 cytoplasmic loop 3 required for basolateral trafficking of the protein have been defined as Cys-208 and Asn-260, respectively.
- studies identify multidrug resistance protein MDR1 as the major glucosyl ceramide flippase required for neutral glycosphingolipid anabolism and demonstrate dichotomy between neutral and acid glycosphingolipid synthesis
- determined that the cytoplasmic end of TM2 in the N-terminal half is in close contact with TM11 in the C-terminal half; the TM2/TM11 interface encloses the drug-binding pocket at the cytoplasmic side of P-gp
- MDR1 polymorphisms modify Balkan endemic nephropathy risk in Bulgarian population.
- MDR1 is upregulated by RNA helicase A in the MEF1 transcription factor complex in multidrug-resistant cancer cells
- Co-expression of this gene with WT1 did not significantly influence the complete response rate to induction therapy.
- independent mutational events may have occurred to confer positive selection in the non-African and African-American populations, respectively
- Refractory epilepsy phenotype in tuberous sclerosis can be associated with the expression of multidrug resistance MDR-1 transporter in epileptogenic cortical tubers.
- MRP1 expressed in 90% of stained tumor cells in 14/15 high-grade gliomas. Also strongly expressed at vascular endothelial cells in tumor. Permeability to anticancer drugs could be also limited across brain tumor vessels.
- elevated cellular cholesterol levels can markedly increase P-gp activity in human PBMCs
- The C3435T MDR1 polymorphism may involve susceptibility to & the clinical outcome of childhood ALL. Carriers of the TT genotype are more at risk of developing ALL than others, whereas CC genotype carriers are supposed to have worse prognosis.
- Lymphocyte P-gp expression determines the degree of inhibition of proliferation by CsA ex vivo; whether this also affects CsA effectiveness in vivo and therefore graft survival requires further study.
- MDR1 has a role in breast carcinoma progression
- "...high-dose administration of glucocorticoids for the treatment of ulcerative colitis results in increased expression of MDR1 mRNA in peripheral blood mononuclear cells, which may impair successful glucocorticoid therapy in these patients."
- Pgp-induced mulitdrug resistance involves both ATPase-dependent drug efflux and ATPase-independent inhibition of apoptosis
- MDR1 gene expression in gallbladder carcinoma is correlated with some biological characteristics, takes part in the carcinogenesis of gallbladder tissues, and acts as a valuable biomarker of prognosis.
- HAX-1 binds bile salt export protein (BSEP), cortactin, MDR1, and MDR2. HAX-1 and cortactin regulate BSEP abundance in the apical membrane of cells.
- Impact of MDR1 polymorphism on the risk and clinical outcome of haematological malignancies. (review)
- In four different groups of marrow samples (20 normal, 56 acute myeloid leukemias (AML) at diagnosis, 48 AMLs at relapse, and 51 regenerating marrows), caveolin-1 and MDR-1 gene expressions were positively correlated
- cross-talk between the cytoplasmic and the transmembrane domains is required for establishment of proper domain-domain interactions that occur during folding of P-glycoprotein
- This review addresses functional aspects of the genetic polymorphism of ABCB1 and provides the standard method to evaluate the effect of polymorphisms on the function.
- The inverted MED1 element and the LRP130 protein have a role in transcription of the MDR1 gene.
- the MDR1 gene may be important for interindividual differences of P-glycoprotein expression
- No association between gene polymorphism and gingival overgrowth was revealed in kidney transplant patients administered cyclosporine A as a principal immunosuppressive agent
- Bcl-2 is over-expressed in CD34+ acute myeloid leukemia (AML); conversely, MDR1 is over-expressed in CD34- AML.
- MDR functional phenotype could be associated with p53 mutation in the advanced stage of leukemias
- Residue Ile-306(transmembrane 5) of P-Glycoprotein is close to the verapamil-binding site
- flow cytometry analysis of raft association and actin cytoskeleton anchorage of Pgp expressed at physiologically relevant levels
- The CGC haplotype, containing the C allele at the exon 26 SNP, is associated with treatment failure of temporal lobe epilepsy The degree of pharmacoresistance may be modulated by this gene. The association is seen most strongly in the mesial TLE subgroup
- The CC genotype at the ABCB1 C3435T polymorphism was reported to associate with multidrug resistance. A replication study in drug-resistant & drug-responsive subjects showed no significant association between the CC genotype and drug-resistant epilepsy.
- interaction of TAP1 and TAP2 and P-glycoprotein with proteasome subunits beta-5 and beta-5i suggest direct targeting of antigenic peptides to the ER via a TAP-proteasome association and a possible role for P-glycoprotein
- Overexpression of caveolin-1 reversed drug resistance of transfectants and lowered their P-gp transport activity in breast cancer cells.
- An association was found between MDR1 alleles, polymorphisms and haplotypes and refractory Crohn disease patients, who do not respond to standard therapy, including patients who develop fistulas.
- P-glycoprotein may be part of a central pathway mediating viral compartmentalization in the brains of HIV-infected individuals and may play a significant part in HIV disease progression in the brain.
- significant correlation with pregnane-x-receptor(PXR) mRNA in peripheral blood cells
- the dileucine motif is not a plasma membrane targeting signal, and the COOH terminus is required for proper folding of P-gp but not for activity
- MDR1 expression in childhood ALL is an independent adverse prognostic factor on outcome, and could be a useful biological marker of response
- protein kinase Calpha transcriptional repression via Sp1 by wild type p53 is involved in inhibition of multidrug resistance 1 P-glycoprotein phosphorylation
- C allele frequencies of the MDR1 C3435T polymorphism are similar among Ashkenazi, Yemenite, and North-African Jewish populations, slightly lower among Mediterranean Jews, and significantly lower among Near-Eastern Jews.
- Cyclosporin A inhibits P-gp function at low micromolar concentrations.
- P-glycoprotein probably contributes to the selective absorption of sphingosine from dietary sphingolipids in the digestive tract
- single nucleotide polymorphisms of MDR1 gene affects the export of Nelfinavir from HIV-positive patients' lymphoblastoid cell lines
- presence of mutant 6+139T allele is a factor determining resistance to lymphoproliferative diseases
- Results describe intercellular transfer of functional P-glycoprotein from P-gp-positive to P-gp-negative tumor cells in vitro and in vivo.
- Allelic variations of the MDR1 gene determine disease extent as well as susceptibility to ulcerative colitis in the Scottish population.
- Multiple MDR1 polymorphisms have been described in various allelic combinations. Frequencies of MDR1 depend on racial background.
- findings demonstrated age-related differences in the body's capacity to metabolize steroids and xenobiotic compounds and suggest an important role for SXR and its target genes, CYP3A4 and MDR1 in this process
- Significant reductions in risk of CNS relapse were observed for patients homozygous for the GSTP1 Val105 allele as well as for patients with the MDR1 3435T/T or C/T genotype in acute lymphoblastic leukemia
- A model to study transsgenic MDR and the efficacy of drugs and modulators on malignant cells where human Plycoprotein is a major factor of multidrug resistance.
- An MDR1 haplotype containing single nucleotide polymorphisms (SNPs) e21/2677T and e26/3435T protects against Parkinson disease in ethnic Chinese.
- hyaluronan, phosphoinositide 3-kinase, and ErbB2 receptor kinase form a positive feedback loop that strongly amplifies multidrug resistance 1(MDR1) expression and regulates drug resistance in human breast carcinoma cells
- CD3(+)/CD8(+) cells and NK cells, exhibited significantly increased P-gp activity compared with the other cell populations.
- involved in the absorption and disposition of saquinovir in vivo.
- In operable non-small lung cell cancers, there may be different relationship of this protein with paatient outcome.
- Intestinal mRNA level of MDR1 is a useful molecular marker for determination of the personalized oral dose of tacrolimus in recipients of living donor liver transplants immediately after surgery.
- MDR1 C3435T polymorphism was not an important factor in tacrolimus pharmacokinetics in liver transplasntation.
- The increased glycolipid content in MDR1-transfected liver neoplasm cells is caused by a transcriptional up-regulation of the enzyme lactosylceramide synthase.
- ABCB1 may maintain neural stem/progenitor cells in an undifferentiated state and could be a neural stem/progenitor marker.
- Expression of P-gp, but not BCRP, decreases dramatically with gestational age in human placentae.
- Expression of P-glycoprotein does not induce resistance to caspase-8 and -3 activation or anti-Fas-induced cell apoptosis.
- -glycoprotein (Pgp) is a well-defined ATP-binding cassette (ABC) protein and a close relative of cystic fibrosis transmembrane conductance regulator (CFTR), whose dysfunction causes cystic fibrosis (CF).
- Sesquiterpenes show similar effectiveness to the classical P-glycoprotein modulator verapamil when reversing resistance to daunorubicin
- Abeta clearance may be altered in diminished P-gp. Impairment of Abeta clearance could lead to accumulation and earlier deposition of Abeta, in walls of blood vessels and in brain, elevating risk of cerebral amyloid angiopathy and Alzheimer's disease.
- MDR1 has independent effects on lipid changes following fluvastatin treatment.
- three loci of ABCB1 jointly influence the treatment response for epileptic patients
- ABCB1, ABCC1, ABCC2, and ABCG2 haplotypes influence response to nelfinavir
- Rearrangement of P-glycoprotein transmembrane segment 11 may contribute to the release of drug substrate during ATP hydrolysis.
- The frequencies of MDR1 2677G>A variant and haplotype profiles showed significant differences between the Korean and Vietnamese populations.
- P-gp-mediated multidrug resistance (MDR) is abolished under conditions of elevated ROS levels.
- Overexpression of P-gp encoded by the MDR1 gene following chemotherapy can severely limit the efficacy of antineoplastic agents. Drugs induce epigenetic modifications at the MDR1 locus, concomitant with MDR1 up-regulation mediated by trans-activation.
- Drug-resistant and drug-sensitive acute leukemia patients were compared for single nucleotide polymorphisms.
- The atypical MDR phenotype, which refers to other chemoresistance mechanisms such as resistance to apoptosis also contributes to the chemoresistance of uveal melanoma. (review)
- acquisition of increased malignant behavior in neuroblastoma occurs concomitantly with multidrug-resistance and is P-gp-independent
- The reported length of the MDR1 gene in Genbank and other databases continues to evolve and varies between 6.3 kilobases (kb) and 210 kb. In DNA from human cell lines & tissues, the MDR1 genomic sequence is 209 kb.
- P-glycoprotein (P-gp, encoded by MDR1) play an important role in the absorption and metabolism of tacrolimus.
- In the case of MDR1/P-gp, its higher expression characterised cases of a higher grade , with lymph node involvement and shorter overall survival and progression in east cancer.
- ABCB1 expression was induced in a DNA-binding independent manner by E2A-HLF, E2A-PBX1, and truncated E2A polypeptides consisting of those portions of E2A present in leukemic fusion proteins.
- MDR1 overexpression is a form of multidrug resistance to chemotherapy. Down regulation of MDR1 by a combination of small interfering RNAs enhanced the chemosensitivity of daunorubicin in parental human mammary adenocarcinoma cell lines.
- contribution of MDR1 gene to inter-individual phenytoin pharmacokinetic variation
- The combination of retinoic acid and the novel histone deacetylase inhibitor (HDACI) depsipeptide (FK228) induced P-gp expression and prevented growth inhibition and apoptosis in acute promyelocytic leukemia cells.
- Pgp activity at the blood-brain barrier could affect risk for developing Alzheimer disease; data establish a direct link between Pgp and amyloid-beta protein metabolism in vivo
- In both cord blood and adult peripheral blood, ABCB1 activity precisely discriminates naive from transitional and all memory B cells.
- The mouse lymphoma line (L5718) has the human gene MDR1. Resistance modifiers induce apoptosis and necrosis in the tumor cells.
- The MDR1 gene in a mouse lymphoma tumor cell line can have its multidrug resistance reversed by several phenothiazines.
- ABCB1, ABCC1, and ABCG1 are expressed differently in gastric and nongastric gastrointestinal stromal tumors and do not impair the initial response of the tumor to imatinib
- MRP3, BCRP, and P-glycoprotein have roles in progression of adult acute myeloid leukemia
- Overexpression of sirt1 induced expression of P-glycoprotein and rendered cancer cells resistant to doxorubicin.
- Tacrolimus dose requirement and dose-adjusted trough levels were correlated with MDR1 3435 (C-->T) polymorphism, and MDR1 3435 (C-->T) polymorphism analysis is helpful to individualize tacrolimus administration.
- Results suggest that ABCB1 3435C>T polymorphism is associated with antiemetic treatment efficacy in patients with cancer treated with 5-HT(3) antagonists.
- this work proves for the first time the involvement of the C3435T MDR1 polymorphism with Crohns disease susceptibility and is different than the 3435T ulcerative colitis risk allele.
- western blots showed an overexpression of MDR-1 in the taxol-resistant clone, while alpha- and beta-tubulins and p48/IRF9 were expressed in equal amounts in both cell lines.
- We profiled gene expression and gene copy number alterations in 11 multidrug resistant ovarian cancer cell using cDNA microarrays and identified a cluster of genes coactivated with MDR1 in 7q21.11-13.
- The C3435T polymorphism is associated with some therapeutic response to bromperidol in schizophrenic patients, possibly by different drug concentration in the brain.
- it is concluded that CIAPIN1 confers multidrug resistance in gastric cancer cells, likely by upregulating MDR-1 and MRP-1
- MDR1 gene determines susceptibility and phenotype in ulcerative colitis.
- MDR1 C3435T polymorphism is associated with susceptibility to later onset ulcerative colitis.
- The recombinant adenoviral mdr1 vector would introduce the antisense mdr1 gene into the human multidrug resistance hepatocellular cell line effectively.
- Taken together, our results demonstrate a distinct mechanism of Pgp modulation that involves allosteric disruption of molecular cross talk between the substrate, and the ATP, sites without any direct interference with their individual functions.
- These results suggest that transmembrane domain 1 of P-glycoprotein contributes to the drug-binding pocket.
- in the nucleotide-trapped low affinity state of Pgp, the allosteric site remains accessible and responsive to modulation by flupentixol, which can reset the high affinity state for [125I]IAAP binding without any further nucleotide hydrolysis
- Expression predicts response to anticancer drugs in advanced hepatocellular carcinoma.
- Results indicate that Creutzfeldt-Jakob disease, like Alzheimer's disease, is associated with a decrease in the expression of cerebrovascular P-glycoprotein.
- Relevance of MDR1 polymorphisms to certain human diseases has been reviewed.
- single nucleotide polymorphisms in Polish population were similar to those reported for other Caucasian populations, 2677G-3435C--0.453, 2677G-3435T--0.143, 2677T-3435C--0.015, 2677T-3435T--0.370, 2677A-3435C--0.008, 2677A-3435T--0.011
- ABCB1 polymorphisms G2677A/T and C3435T are not associated with drug resistance in schizophrenia.
- P-glycoprotein (ABCB1) mediated efflux activity was only slightly and in the opposite direction affected ganglioside. depletion
- The expression of mRNA for MDR1 and LRP was determined in bone marrow samples from control, de novo acute myelocytic leukemia, myelodysplastic syndrome(MDS), MDS at the time of overt leukemia(OL) transformation (MDS --> OL),and after transformation (OL).
- Common MDR1 gene polymorphisms do not affect disposition of budesonide in early PBC.
- Results suggest that the MDR1 promoter region is largely invariant but that different haplotypes have differential effects on the MDR1 promoter activity in different cell lines.
- MDR1 expression affects complete remission and survival rates in acute leukemia
- ABCB1 sequence variants are associated with a small increase in the risk of developing UC and may influence disease behavior.
- T3587G MDR1 mutation may affect the pharmacokinetics of MDR1-related anticancer agents in patients carrying this allele.
- Data show that nitrogen monoxide stimulates iron and glutathione efflux from cells via multidrug resistance-associated protein 1.
- REVIEW: new drug transport model of P-glycoprotein from the results of mutagenic, quantitative thermodynamic and kinetic studies
- BCRP was over-expressed in 24 patients and was significantly co-expressed with P-glycoprotein in acute myeloid leukemia.
- When present in rafts, P-gp interacts with protein partners regulating its activity. P-gp is a lipid translocase that handles the raft-constituting lipids with particular efficiency, and it also influences membrane trafficking in the cell.
- These data implicate the involvement of PKA-RIIalpha anchoring apical targeting of distinct proteins and glycosphingolipids to apical plasma membrane domains and suggest that rerouting may underlie the delayed Golgi-to-apical surface transport of MDR1.
- MDR can be reversed by the shRNA-mediated MDRI suppression in HepG2/ADM cells, which provides a valuable clue to make multidrug-resistant hepatoma cells sensitive to anti-cancer drugs.
- The data argue that ABCB1 modulation is not an effective strategy to circumvent drug extrusion from primitive leukemic progenitor cells and may preferentially target residual normal progenitors in AML.
- ABCB1 polymorphisms may influence the antiepileptic drug responsiveness without significant changes in the plasma concentrations of carbamazepine
- Regarding the ABCB1 G2677T/A and C3435T polymorphisms, a trend was observed between the different genotypes and the area under the time concentration curve (AUC0-12)
- G2677T/A genotype seems to be associated with stem cell transplantation outcomes, especially non-relapse mortality.
- P glycoprotein level in tumor cells is not a predictive marker for response to paclitaxel in women with metastatic breast cancer.
- study undertook a meta-analysis of the available findings obtained with two SNPs polymorphism (C3435T and G2677T/A) in IBD; a significant association of 3435T allele and 3435TT genotype has been found with ulcerative colitis
- ABCB1 genotype modulates the expression in the unaffected renal cortex of renal cell cancer patients
- Knowledge of ABCB1 genotype may be useful to adjust the optimal dose of tacrolimus in transplant patients, thereby rapidly achieving target concentrations.
- The genotypes and allele frequencies of the MDR1/C3435T, FMO3/G488A, FMO3/A923G and CYP1A2/G-3860 A polymorphisms were not significantly different in cancer-free subjects and CRC patients.
- MDR1 T-129C, but not G2677A,T and C3435T, was associated with the lower expression of MDR1 mRNA in colorectal adenocarcinoma.
- These results suggested that both ribozymes can reverse the MDR phenotype by inhibiting the expression of mdr1 mRNA and P-gp, and the RZ135 showed the better cleavage efficiency.
- Results identify stable reaction intermediates in the progression of the P-glycoprotein-mediated ATPase reaction.
- We could not confirm the relationships between ABCB1 and UGT1A1 polymorphisms and Ir PK.
- IAP family proteins may the prognosis of multiple myeloma patients in association with chemotherapy-induced overexpression of MDR1 or LRP.
- Results describe the behavior of P-glycoprotein in its natural lipid environment within the membrane of CEM cells expressing Pgp in the quantities varying from 0% to 32% of the total amount of all membrane proteins.
- The mRNA induction of MDR1, MRP1, MRP2 and MRP3 by rifampicin (Rif), dexamethasone (Dex) and omeprazole (Ome) was investigated in primary cultures of cryopreserved human and rat hepatocytes.
- (99m)Tc-MIBI SPECT could predict anti-cancer drug resistance related to the expression of multidrug-resistance (MDR-1) gene product P-glycoprotein (Pgp) in pituitary adenomas.
- These results have important implications for understanding the mechanisms by which MDR1 gene therapy can protect normal tissues from radiation- or chemotherapy-induced damage during tumor treatment.
- drug selection with natural products targeting DNA or microtubules leads to DNA damage, nonhomologous recombination, and acquired drug resistance, wherein MDR-1 expression is driven by a random but constitutively active promoter
- Data show that tetrahydrocurcumin inhibits the efflux function of ABCB1, ABCC1, and ABCG2 and it is able to extend the multidrug resistance reversing activity of curcuminoids in vivo.
- MDR-1 haplotypes have a relatively minor association with tacrolimus pharmacokinetics in kidney transplantation.
- Cytochrome p450 geme induce co-repressor ligands in effecting its transcriptional down-regulation of MDR1 gene.
- Therefore, P-gp could be involved in the protection of mitochondrial DNA from damage due to antiproliferative drugs.
- In locally advanced breast cancer, ABCB1 gene expression during chemotherapy contributes to clinical unresponsiveness.
- The effects of genetic polymorphisms of CYP3A4, CYP3A5 and MDR1 on cyclosporine dose adjusted trough blood concentration during the early period after renal transplantation in Chinese patients is reported.
- No difference was observed in Tacrolimus pharmacokinetic parameters in relation to ABCB1 polymorphisms.
- A study evaluating the simultaneous administration of digoxin and midazolam to determine P-glycoprotein and cytochrome P450 3A4/5 activity is reported.
- distribution of G2677A/T single nucleotide polymorphisms in a group of 86 Polish ovarian cancer patients with poor tumor differentiation.
- MDR1 C3435T polymorphism in 150 healthy volunteers in Denizli province of Turkey.
- suggest a role for MDR-1 and MDR-3 in chemoresistant disease
- saturation kinectic parameters of the frequently occurring ABCB1 triallelic variants 893Ser (exon 21, 2677T) and 893Thr (2677A) were considerably different from wild-type 893Ala (2677G), despite similar protein expression levels
- In acute myeloid leukemia patients, 60 years and older, ABCB1 gene polymorphism does not exert a major impact on drug resistance.
- MDR1 single nucleotside polymorphismss are correlated with cyclosporine exposure in the early kidney post-transplant period.
- Significant association between tacrolimus levels per dose mg/kg/d and MDR1 gene C3435T polymorphism in kidney transplantation
- We investigated the relationships between exon 21 G2677T and exon 26 C3435T genetic variants of MDR1 gene with susceptibility and treatment response in female schizophrenic patients.
- The existence of polymorphisms in the ABCB1 gene and, specifically, the presence of the G2677T mutation can be crucial in conferring susceptibility to lung cancer.
- unable to observe the original association of drug-resistant epilepsy with C3435T, nor any association with other functional variants at SNP or haplotype level in the ABCB1 gene
- The interaction of genetic and lifestyle risk factors should be taken into account to elucidate the genetic influence of MDR1 variability on cancer susceptibility.
- These data indicate that retroviral MDR1 gene transfer results in preferential P-glycoprotein expression in myeloid progenitor cells, which is the target cell population for myelotoxicity of cytostatic drugs.
- P-gp is expressed before treatment of non-Hodgkin's lymphoma of HIV patients, and is related to poor response to treatment and overall survival.
- These findings indicate that P-gp is functionally active in the human alveolar airspace and that human alveolar epithelial cells monolayers might provide a suitable in vitro model for studying P-gp function mechanistically in the distal human lung.
- A possible role is outlined for MDR-1 as a prognostic factor, dependent and independent of multidrug resistance in selected cases of renal cell carcinoma, clear cell type, with long-term follow-up.
- we report that a synonymous SNP in the MDR1 gene results in P-gp with altered drug & inhibitor interactions; similar mRNA & protein levels, but altered conformations, were found for wild-type & polymorphic P-gp
- Single nucleotide polymorphism (SNP) at location 3435C-->T plays a significant role in ABCB1 gene function and may be a basis for studies of relationships between ABCB1 genotypes and drug efficacy, drug toxicity, and disease susceptibility phenotypes.
- (R)-lansoprazole concentrations significantly increased in CYP2C19 extensive metabolizers with ABCB1 C3435T C allele.
- The frequencies of MDR1 C3435 and T3435 alleles in Tamilian population were 0.46 and 0.54 respectively, and the distribution of CC, CT and TT genotypes was 0.18, 0.56 and 0.26 respectively.
- P-glycoprotein has a role in progression of hepatocellular carcinoma
- A significant association was found between the MDR1 C3435T polymorphism and patients with ileo-colonic CD
- MDR1 expression is strongly decreased in inflamed IE of patients with gastrointestinal disorders and this is independent of PXR protein levels. Low MDR1 levels may aggravate intestinal inflammation.
- MCJ is required in these cells to prevent c-Jun-mediated expression of ABCB1 and maintain drug response.
- there is no significant association between polymorphisms in CYP3A4, CYP3A5, MDR1, GSTM1 and GSTT1 and outcome either after treatment with induction chemotherapy or after high-dose therapy for multiple myeloma
- MDR1 C3435T polymorphism is correlated with endometrial cancer susceptibility.
- An association between polymorphisms in GSTP1 and ABCB1 and risk of acquiring intratumoral TP53 mutations suggests the existence of putative predisposing genotype backgrounds.
- The present study demonstrates that the ABCB1 3435 genotype affects angiotensin II-stimulated serum aldosterone levels and salt-stimulated urinary sodium excretion.
- Modulation of histone H4 acetylation level can be associated with up- or down-regulation of the MDR1 gene in ovarian carcinoma cell line.
- CD34-related MDR1/BCRP coexpression remained significantly associated with a lower CR rate, thereby identifying a clinically resistant subgroup of elderly AML patients
- The role of ABCB1 in brain absorption of avermectin pesticides is discussed, as well as the potential impact of the reported functional effects and population frequencies of known ABCB1 polymorphisms on avermectin toxicity. [review]
- ABCB1 polymorphism has no pronounced effect on saquinavir exposure.
- ABCB1 and CYP3A5 genes interact with urinary sodium excretion in their effect on ambulatory blood pressure, suggesting a gene-gene-environment interaction.
- Data suggest that transcriptional inactivation of MDR1 gene due to increased MDR1 promoter methylation may be a contributing factor in pathogenesis and progression of neuroblastoma tumors.
- Valproic acid to up-regulates MDR1 through direct activation of CAR and/or PXR pathways.
- R-cetirizine up-regulates MDR1 expression while S-cetirizine down-regulates MDR1 expression
- high and low P-glycoprotein, glutathione S-transferase pi expression, excision repair cross-complementing 1 alterations, and tumor suppressor p53 mutation were candidates for future clinical trials of chemosensitivity tests in lung cancer patients.
- conclusion, the data demonstrate the utility of the analyzed RNAs as powerful laboratory tools and indicate that YB-1 is not involved in the regulation of the MDR1 gene.
- ABCB1 was significantly hypersensitive against KP772.
- C3435T polymorphism in ABCB1 is unlikely to be a marker for epilepsy multidrug resistance.
- This study has demonstrated a decrease in expression of P-gp and down regulation of MDR-1 gene consistently on mesenchymal stem cell during chondrogenesis.
- data suggested a longer overall survival for multiple myeloma patients with C/T and T/T genotypes (log-rank test, P = 0.02) compared with patients with C/C genotype
- Methoxyflavones inhibit P-glycoprotein to affect multidrug resistance in tumor cell lines.
- ABCB1 single nucleotide polymorphisms influence the metabolic clearance rate of imatinib in cancer patients.
- MDR1 polymorphisms are associated with differences in cyclosporine exposure only in the first week after kidney transplantation.
- Patients with drug-resistant epilepsy were more likely to have the TT genotype compared with those with drug-responsive epilepsy.
- p53 genetic alterations found in gastric stump carcinomas & intestinal-type primary gastric carcinomas could originate from a similar pathway; no association found between p53 gene status & P-gp expression
- Results suggest that Rab5 and RalA regulate P-gp trafficking between the plasma membrane and an intracellular compartment.
- inhibition of the p44/42-MAPK phosphorylation by high-dose acetaminophen could abolish the doxorubicin-induced cell death pathway
- Tamoxifen activated the SXR-mediated transcription through CYP3A4 and MDR1 promoters in a ligand- and receptor concentration-dependent manner.
- The PGY1 linker domain encodes high-affinity binding sequences to alpha- and beta-tubulins.
- Knock-down of SRI induces up-regulation of MDR1 in HeLa cells.
- There is a correlation of induction of ABCB1 and mRNA with differentiation of colonic neoplasms.
- Compounds present in grapefruit juice are able to inhibit the P-gp activity modifying the disposition of drugs that are P-gp substrates such as talinolol.
- We conclude that daptomycin is subject to efflux from THP-1 macrophages and MDCK cells by P-gp, which reduces its intracellular activity against phagocytized S. aureus.
- The risk of breast carcinoma in patients with MDR-1 polymorphism was significantly associated with the higher body mass index, where women with BMI >30 kg/m(2) and C allele in genotype had a higher risk of disease
- MDR1 gene polymorphism was not a predisposing factor for terminal kidney failure leading to renal transplantation.
- polymorphisms of 2677G, 2677T, & 2677A exhibit wide ethnic differences in allele frequency, these nonsynonymous polymorphisms are suggested to be clinically important because of their altered ATPase activity & substrate specificity toward different drugs
- These findings suggest that prolactin concentrations in females are much higher than in males but the major MDR1 variants are not associated with the plasma concentration of prolactin.
- results of the present study demonstrated a 1.5-fold increased risk for development of breast cancer in T allele carriers
- The IL-10 G-1082A and CYP3A5()3 polymorphisms may influence the interindividual variability of tacrolimus pharmacokinetics in Chinese liver transplant patients.
- The MDR1 gene polymorphisms, -2352 G>A, -934A>G, -692T>C (5' regulatory region) and 3435C>T (exon 26), were examined in 157 ALL patients and 96 healthy children.
- may be relevant for dose recommendation of P-gp substrate drugs and also for studies of allele disease association in the Central American population
- P-glycoprotein expression is post-transcriptionally regulated in cancer cell lines
- Retinoblastoma intrinsically expresses both P-gp and MRP-1 and their expressions are not related to tumor differentiation. The expressions of P-gp and MRP-1 do not seem to be induced by chemotherapy and are not related to the degree of tumor invasion.
- 3435T/T polymorphism of MDR1 is associated with a reduced risk of gastric cancer in Japanese.
- In this review MDR1/ABCB1 is clinically important because it not only is involved in multidrug resistance in cancer but it also affects the pharmacokinetic properties of various drugs.
- Familial mediterranean fever patients with the TT genotype for the ABCB1 3435C to T variant responded better to colchicine in terms of treatment efficacy and colchicine dose requirements.
- The mean percentages of cancer cells expressing MDR among the 10 cancer samples was 35%.
- This finding reveal complex signatures of natural selection on both coding and regulatory regions of the human ABCBI gene.
- determination of frequencies of ABCB1 polymorphisms & haplotypes in healthy French individuals; frequencies of the 8 ABCB1 polymorphisms in this population are similar to those described in other Caucasian populations except for the C3435T polymorphism
- Neither the individual ABCB1 polymorphisms nor the ABCB1 haplotypes were associated with any pharmacokinetic parameter.
- Different drug-binding sites of P-glycoprotein may undergo different major structural rearrangements at the three energetic steps: ATP binding, ATP hydrolysis and ADP/inorganic phosphate (Pi) release.
- There was a significant negative relationship between age and P-gp efflux activity indicating that P-gp activity in PBMCs decreases with advancing age.
- CtBP1 might be one of the key transcription factors involved in the induction of MDR1 gene
- Combined MDR1 genotypes derived from positions 2677 and 3435 are possibly associated with young age onset of ulcerative colitis and severe course of disease in this patient group.
- In H69 drug-resistant SCLC cell line TSA induces downregulation of ABCB1 expression through a transcriptional mechanism, independently of promoter methylation, and MBD1 or PCAF recruitment.
- MDR1-independent resistance in human colon cancer cells is induced by histone deacetylase inhibitors suberoylanilide hydroxamic (Vorinostat) and valproic acid
- MDR1 2677G>T and 3435C>T polymorphism is not a risk factor for sporadic colon cancer among Bulgarians and that somatic mutation at these sites is not involved in the genesis of colon tumors.
- MDR1 overexpression is an unfavorable prognostic factor in acute myeloid leukemia.
- imatinib does not interact at the ATP-binding sites of either Pgp or ABCG2 despite their strong affinity for the ATP-binding pocket of the tyrosine kinases; it behaves like a transport substrate as it stimulates ATP hydrolysis by these transporters
- The mutation of one residue (G346C) in P-GP transmembrane segment adversely affected drug transport in cells. This mutation also affected the stimulation of ATPase activity, but had no effect on drug binding, ATP binding, or ADP release.
- No pharmacogenomic associations are found between the most common ABCB1 haplotypes and acute kidney injury or chronic kidney disease following myeloablative allogeneic hematopoietic cell transplantation.
- A homology model of P-glycoprotein representing an ATP-bound state is developed based on the biochemical and sequence similarity between Staphylococcus aureus Sav1866 and P-glycoprotein.
- analysis of the outward facing state of the human P-glycoprotein (ABCB1), and comparison to a model of the human MRP5 (ABCC5)
- Genotyping of the ABCB1 gene may be important for determining the tumor resistance to paclitaxel and provide useful information for individualized therapy.
- The data seem to support the association of the PXR locus with extensive ulcerative colitis and the interaction between PXR and MDR1 genes.
- MDR1 2677G-->T/A and 3435C-->T polymorphisms can be used to predict treatment response to vinorelbine-cisplatin chemotherapy in non-small cell lung cancer.
- The expression analyses of MRP1 and MDR1 drug efflux proteins in doxorubicin-sensitive and -resistant HL60 cells revealed, while there was no expression of MDR1 gene in parental cells, the expression of MDR1 gene was upregulated in HL60/DOX cells.
- role of CYP3A5, MDR1 and IL-10 genetic polymorphisms in the variability of tacrolimus population pharmacokinetic parameters
- statistically significant correlations between MRP1 and LRP expression and between MRP1 or LRP expression and MDR1 expression
- ABCB1 expression was comparable in the jejunum and ileum, but lower in the stomach.
- The multivariate logistic regression analyses demonstrated that the homozygous ABCB1 TT genotype was significantly associated with an overall increased risk for developing Upper aerodigestive tract cancers.
- ABCB1 genetic polymorphisms significantly influenced Tac hepatic concentrations, whereas their impact on blood concentrations seemed negligible.
- This study showed that manipulation of drug efflux transporters may be a useful strategy for increasing the intracellular concentration and thereby enhancing the clinical efficacy of lopinavir.
- relationship between T and C alleles and frequency of Pgp polymorphism as well as thyroid hormone distribution in patients with hypo- and hyperthyroidism was investigated.
- Pain relief variability was significantly (P<0.0001) associated with single-nucleotide polymorphism of the ABCB1 gene.
- MDR1 expression significantly elevated the risk for disease progression (p = 0.02), and this association remained statistically significant. No association was found between MDR1 expression and overall surviva.
- This study did not support any significant association between the MDR1 (C3435T) polymorphism and resistance to CBZ in epilepsy patients from Turkey.
- For both ethnic groups, the C allele of MDR1 C3435T was highly associated with being infected with HIV (p < 0.0001) compared to controls, but genotype did not influence change in CD4 counts over time in the patients.
- Detection of P-glycoprotein and metallothionein seems to add certain prognostic value in gastrointestinal stromal neoplasms (MT) or gastrointestinal leiomyosarcomas (P-GP).
- Single nucleotide polymorphisms contribute to drug-resistant epilepsy.
- P-gp, rather than BCRP or OCT1, is partially responsible for the development of imatinib-resistance due to constitutive and functional overexpression, leading to reduced intracellular accumulation of imatinib in resistant K562 cells.
- ABCB1 3'-UTR variants have no effect on ABCB1 mRNA stability
- Pgp is involved in migration and invasion of resistant melanoma cells.
- Upregulation of MDR1 by DeltaNp73alpha is mediated by interaction with p53 at the MDR1 promoter.
- Treatment with the anti-cancer drug paclitaxel have an increased copy number in the 7q21.12 region including the MDR1/ABCB1 gene.
- report the cloning and characterization of the MDR1 upstream promoter and studied its association with chemotherapy response in breast cancer patients
- Examine interactions of agents used to treat attention-deficit/hyperactivity disorder with P-glycoprotein.
- MDR1 promoter polymorphism is not associated with its activity and protein expression in acute myeloid leukemia
- a functional interplay between membrane Gb3 and MDR1 provides a more physiologically based approach to MDR1 regulation to increase the bioavailability of chemotherapeutic drugs.
- R230C/C230C genotypes were significantly more frequent in type 2 diabetic individuals than in control subjects in Mexicans.
- MDR1 expression might have significant prognostic value in patients suffering from metastatic non-seminomas
- Data show that exposing cells to the glucosylceramide synthase inhibitor, ethylenedioxy-P4, prevented ceramide's enhancement of MDR1 expression.
- review potential importance of SNPs in MDR
- DARPP-32 mediates multidrug resistance of gastric cancer through regulation of P-gp and ZNRD1.
- These findings suggest that downregulating CIAPIN1 could sensitize leukemia cells to chemotherapeutic drugs by downregulating MDR-1 and Bcl-2 and by upregulating Bax.
- Promoter polymorphisms and allelic imbalance influence ABCB1 mRNA expression
- Possible genes for antipsychotic treatment response were the dopamine D2 receptor gene (DRD2), the serotonin 2A and 2C receptor genes (HTR2A and HTR2C), the P-glycoprotein gene (ABCB1 or MDR1) and the drug-metabolizing cytochrome P450 2D6 gene (CYP2D6).
- gp is expressed early during human cerebral cortical microvessel development, and suggest that at midgestation there may be efflux activity that is regulated by interactions with the caveolar endothelial cell compartment.
- the present study highly suggest that GSTP1, MDR1, and MTHFR genotypes could be prognostic factors for Taiwanese patients with breast cancer.
- Anionic drug salinomycin is a substrate for p-gp.
- Determination of P-glycoprotein, MDR-related protein 1, breast cancer resistance protein, and lung-resistance protein expression in leukemic stem cells of acute myeloid leukemia.
- This study indicate that the combined consideration of both the medication's capacity to act as an ABCB1-transporter substrate and the patient's ABCB1 genotype are strong predictors for achieving a remission.
- While the distribution of individual alleles and genotypes did not differ between patients and controls, there were significant differences in the frequencies of some rare haplotypes and genotype combinations in the MDR1 gene between the two groups.
- Single nucleotide polymorphisms in multidrug resistance-1 was associated with central side effects to morphine in cancer patients
- Complete remission rates and overall, relapse-free and event-free survival rates were not significantly different among the C3435T polymorphism of the MDR1 genotypes.
- MDR1(+) cells had higher ability to form spheres in low attachment conditions, a hallmark of cancer. In conclusion, these novel findings imply that the MDR1(+) cells represent melanoma stem cells.
- These results suggest that guggulsterone, a natural dietary hypolipidemic agent have dual inhibitory effects on P-gp and MRP1 and the potencies to cause food-drug interactions.
- These functional data demonstrate that nonsynonymous polymorphisms in ABCB1 may selectively alter P-gp transport and drug-drug interactions in a substrate- and inhibitor-dependent manner.
- ABCB1 SNPs may affect function of P-glycoprotein by influencing the expression level and modify breast cancer prognosis.
- Self-identification according to the racial/color categories proposed by the Brazilian Census is insufficient to properly control for population stratification in pharmacogenomic studies of ABCB1.
- These results indicate that mtDNA depletion can induce increased P-glycoprotein expression via an increase of mRNA stability and suggest that the mtDNA depletion in cancer cells plays an important role in the induction of multidrug resistance phenotype.
- The effects of zidovudine and stavudine on human cells, measuring their effects on the levels of mtDNA, mtRNA and on induction of the multidrug resistance (MDR) gene MDR-1.
- Following transient expression of MDR-1 and MCJ, changes in the sensitivity of Sk-Ov-3 cells to paclitaxel were detected whereas expression of Src, Bcl-2 and Bcl-X(L) decreased the sensitivity of Sk-Ov-3 cells to carboplatin.
- C3435T polymorphism of ABCB1 gene was demonstrated in vivo to significantly influence the CSF/S PB concentration ratio and seizure frequency.
- ABCB1 1236C-->T, 2677G-->T, and 3435C-->T variants and the associated TTT haplotype were associated with higher digoxin serum concentrations
- ABCB1 polymorphisms influence cyclosporine intracellular concentration in transplant recipients
- Biochemical alterations seen in AN patients could lead to increased expression and/or activity of P-gp and therefore to diminished access of drugs to the brain.
- Our results show that ET-1 has no effect on Pgp expression of adult HBMECs, but does modulate Pgp transport activity.
- correlation between CIAPIN1 down regulation and decreased MDR1 transcriptional activity were observed.
- nuclear and histological degree, and estrogens, progesterone and c-erb B2 receptors did not correlate with the SNP C3435T. Patients with complete pathological response (12.5%) showed only the polymorphic genotype and not the wild genotype
- two closely spaced thyroid hormone receptor/retinoid X receptor-binding clusters are both required for the maximal induction of MDR1 gene expression mediated by thyroid hormone receptor
- Genetic variability of MDR1 should be considered as an important factor that influences the clinical outcome of multiple myeloma.
- Human ABCB1 polymorphisms may alter the interactions between Pgp and substrates, and provided functional evidence for ABCB1 haplotypes-associated epilepsy treatment responses.
- CYP3A5*1 genotype as well as the MDR1 mRNA level in enterocytes contributes to interindividual variation in the CL/F of tacrolimus in adult recipients early after living-donor liver transplantation.
- ABCB1 variants may have clinical relevance by influencing the methadone dose required to prevent withdrawal symptoms and relapse.
- This study findings failed to prove an association between C3435T polymorphism and drug resistance in a sample of Turkish patients with refractory epilepsy who underwent resective brain surgery.
- HA binding to tumor cells promotes Nanog protein association with CD44 followed by Nanog activation and the expression of pluripotent stem cell regulators, and forms a complex with Stat-3 in the nucleus leading to Stat-3 and MDR1 activation
- ABCB1 genotype may prove informative for assessment of genetic risk for obesity in Japanese individuals.
- MDR1/ABCB1 gene plays in the initiation and progression of high-microsatellite instability colorectal cancer development.
- Influence of ABCB1 polymorphism on prednisolone pharmacokinetics in renal transplant recipients was evaluated. Its allelic variants did not affect patient variability of plasma prednisolone concentration.
- Multidrug resistance gene (MDR1) polymorphisms are associated with major molecular responses to standard-dose imatinib in chronic myeloid leukemia.
- Suggest that Pgp inhibition by cyclodextrin treatment arises through modulation of its membrane microenvironment, rather than as a result of concomitant cytotoxicity.
- An ABCB1 polymorphism is associated with virological efficacy in HIV-infected patients treated with non-boosted protease inhibitor (PI)-containing regimens but not with those containing boosted PIs.
- MDR1 variants G2677T and C3435T are not associated with therapeutic response to paroxetine in patients with major depression
- Dasatinib is a substrate of both efflux proteins, ABCB1 and ABCG2.
- Report correlation between expression of MDR1 and drug resistance in glioblastomas.
- Observations suggest a possible down regulation/inhibition of P-gp by COX inhibitors, which may enhance the accumulation of chemotherapy agents.
- Report a novel nanocapsule delivery system to overcome intestinal degradation and drug transport limited absorption of P-glycoprotein substrate drugs.
- Our data do not justify genotyping of the investigated single nucleotide polymorphisms (SNPs) to assess the development of renal dysfunction post-HTx.
- These results indicate that Pgp down-regulates BCRP expression in a drug-free state in which JNK/c-Jun is involved.
- Data show that changes in P-glycoprotein are the result of many seizures; are caused by the anti-epileptic drugs, or truly reflect pharmacoresistance.
- Arginines in the first transmembrane segment promote maturation of a P-glycoprotein processing mutant by hydrogen bond interactions with tyrosines in transmembrane segment 11.
- vitamin D receptor induces MDR1 expression in a 1alpha,25-dihydroxyvitamin D(3)-dependent manner
- MicroRNAs miR-27a and miR-451 are involved in activating the expression of P-glycoprotein, the MDR1 gene product that
- bioavailability enhancement and reducing toxicity of irinotecan by P-gp inhibition but in another way also reiterate the significance of elucidating herb-drug interactions
- negative implications for docetaxel treatment in androgen-independent prostate cancer patients carrying ABCB1 variant genotypes.
- Association of MDR1, CYP3A4*18B, and CYP3A5*3 polymorphisms with cyclosporine pharmacokinetics in Chinese renal transplant recipients.
- results do not support major influence of MDR1 variants on the risk of myeloma in Caucasians.
- P-glycoprotein might not be involved in the carcinogenesis of H. pylori-related gastric cancer.
- Chemotoxicity of doxorubicin and surface expression of P-glycoprotein (MDR1) is regulated by the Pseudomonas aeruginosa toxin Cif.
- REIC/Dkk-3 overexpression downregulates P-glycoprotein in multidrug-resistant MCF7/ADR cells and induces apoptosis in breast cancer
- Structural insights into ABCB1 are described using a combination of small angle X-ray scattering data and cryo-electron crystallography data.
- MDR1 mRNA levels in gastric cancer cells are significantly lower than those in colon cancer cells, which is at least in part due to different epigenetic regulations such as DNA methylation and/or histone deacetylation.
- Results compare the relative amounts of ABCb1 (Pgp) and ABCc1 (Mrp1)at the blood-brain and blood-cerebrospinal fluid barriers, located respectively at the brain capillary endothelium and the choroid plexus epithelium.
- The genotype of the MDR1 exon12 C1236T SNP is a novel independent predictive factor for outcome of temozolomide treatment in glioblastoma patients.
- ubiquitination of P-gp and CD147 might be a novel method for tumor therapy
- in patients with femoral head osteonecrosis, The synergistic index between the ABCB1 and CBP genes was >1.00 (1.99), revealing the presence of an interaction
- significant association between gingival overgrowth and the 3435TT genotype was confirmed by logistic regression analysis
- in renal allograft recipients the CYP3A5*3/*1 genotype, but not polymorphisms of MDR1 or CYP3A4) is associated with a reduced susceptibility for the inhibitory effects of fluconazole on tacrolimus metabolism
- disrupt interactions between the nucleotide binding and transmembrane domains of P-glycoprotein and the cystic fibrosis transmembrane conductance regulator
- MDR1-deficient cells exhibited UCB uptake and cytotoxicity comparable with controls.
- Immunohistochemical expression and clinical significance of P-gp in previously untreated NK/T-cell lymphoma, nasal type, are reported.
- Women who carried the minor T/A alleles at the 2677G>T/A polymorphism were significantly less likely to relapse following treatment compared with homozygote GG carriers
- APE1 downregulation sensitizes MDR1-overexpressing tumor cells to cisplatin or doxorubicin, showing APE1's critical role in YB-1-mediated gene expression and drug resistance in tumor cells.
- Lapatinib reverses ABCB1- and ABCG2-mediated MDR by directly inhibiting their transport function.
- These data indicate that the tumor multidrug resistance mediated by P-gp could be reversed by sustained intracellular acidification through down-regulating the P-gp expression and activity.
- High expression of MDR1 mRNA in blood vessels of the nervous system and in other tissues support the physiological role of MDR1 as a regulator of intracellular levels of endogenous and exogenous compounds.
- These findings suggest that the increased expression of ABCB1 upon acquisition of docetaxel resistance in breast tumor cells can be multifactorial, involving both epigenetic changes in promoter usage and regional chromosome amplification.
- ABCB1 haplotypes modify the risk of acute rejection, suggesting that ABCB1 allelic arrangement is a stronger regulator of P-glycoprotein activity than single polymorphisms.
- common SNPs in the MDR1 gene are associated with an overall susceptibility for ulcerative colitis and specific disease phenotypes in North Indians
- Cytologic evaluation of GST-pi and P-gp expression may predictor the response to treatment and the survival of patients with advanced NSCLC.
- MDR1 siRNAs specifically reverse the multidrug resistance of colon cancer cells
- High levels of P-gp activity observed in the lymphocytes of children up to 6 months of age may affect the efficacy of intracellular drugs.
- silent MDR1 C1236T (Gly412Gly) polymorphism in a Turkish population
- ABCB1 polymorphisms were not related with transplantation outcome.
- A correlation between MDR1 genetic polymorphisms C3435T and G2677T/A, as well as haplotypes derived from C1236T, G2677T/A and C3435T, with methylation status of MDR1 promoter region was found in this study.
- Data provide new insights into the mode by which multidrug-resistant breast cancers evade cytotoxic attacks from P-glycoprotein substrates and also suggest a role for P-gp/cellular prion protein (PrP(c)) interaction in this process.
- Less P-GP is found after cyclosporine treatment than after tacrolimus treatment in kidney after kidney transplantation.
- The current study demonstrated that common polymorphisms in the 3' untranslated region of ABCB1 and ABCC1 may contribute to the etiology of lung cancer.
- ABCB1 gene induction decreases disease-free and overall survival in patients with locally advanced breast cancer
- ABCB1 immunostaining was observed in microvessel endothelial cells as early as 22 (0/7) weeks, increasing in prevalence and intensity with maturation in infants born at 22 (0/7)-42 (0/7) weeks of gestation
- ABCB1 polymorphisms are not associated with colon cancer risk and prognosis in a selected patient population.
- the protein possesses intrinsic structural flexibility to allow cross-links to occur between helices 6 and 12 of P-glycoprotein, thereby reconciling crystallographic models with available experimental data from cross-linking.
- ABCB1 haplotypes differentially affect the pharmacokinetics of the acid and lactone forms of simvastatin and atorvastatin