All three N276 compounds almost completely reversed the acquired resistance to vincristine (VCR), vinblastine (VBL), and doxorubicin (DXR) in MDR1-overexpressing human cancer cell lines (KB/VJ300 and T24/VCR).
The fact that P-GP modulators alter the pharmacokinetics of anti-cancer drugs can potentially increase toxicities if the dose of anticancer drugs is not appropriately reduced.
P-glycoprotein (P-gp) of membrane transporters, a product of the multiple drug resistance (MDR)-1 gene, is known to play a pivotal role in the acquisition of drug resistance to chemotherapy in malignancy.
P-glycoprotein (P-gp) is a transmembrane protein responsible for drug efflux, which decreases drug intracellular bioavailability, consequently decreasing their efficacy against cancer.
This induction of Pgp expression likely confers multidrug resistance to the cancer cells and may affect the efficacy of subsequent or concurrent chemotherapy.
In light of the overexpression of MGC4175 in association with taxol exposure, drug resistance, the coexpression of MDR1 and the mitochondrial localization of its protein, we propose to name this transcript MDR1 and Mitochondrial Taxol Resistance Associated Gene (MM-TRAG) and suggest that MM-TRAG may play a role in the development of taxol resistance in human cancer.
Sequential influences of leukemia-specific and genetic factors on p-glycoprotein expression in blasts from 817 patients entered into the National Cancer Research Network acute myeloid leukemia 14 and 15 trials.
In conclusion, both in silico and in vitro studies confirm that PIP is an inhibitor of P-gp mediated DOX efflux, suggesting PIP as a promising adjuvant to DOX cancer chemotherapy.
P-glycoprotein (ABCB1) is an ATP-binding cassette transporter that plays an important role in the clearance of drugs and xenobiotics and is associated with multi-drug resistance in cancer.
The link between bacterial and viral infections to cancer compels us to highlight fascinating reports from coumarin isolation from microorganisms; comment on the recent bioavailability studies of natural or derived coumarins; and discuss our perspectives with respect to bioisosterism in coumarins, p-glycoprotein inhibition and covalent modification, and bioprobes.
These results open new insights into transcriptional decoy and anti-gene therapies of MDR cancers that overproduce Pgp.Gene Therapy (2000) 7, 1224-1233.
In this study, at achievable nontoxic plasma concentrations, citrus flavonoid tangeretin has been shown to reverse ABCB1-mediated cancer resistance to a variety of chemotherapeutic agents effectively.
Multidrug resistance (MDR) is one of the major obstacles confronted in cancer chemotherapy; this obstacle is mainly due to the overexpression of P-glycoprotein (P-gp).
Our objective was to determine the elimination constant (kH) for hepatic elimination of technetium Tc 99m-labeled sestamibi (99mTc-MIBI) in patients with cancer and to compare this putative indicator of ABCB1 phenotype with clinical features and common ABCB1 genetic variants.
P-glycoprotein (Pgp)-conferred multidrug resistance (MDR) is expressed in cancer and in normal colon tissues and has important physiological functions.
P-glycoprotein (P-gp) of membrane transporters, a product of the multiple drug resistance (MDR)-1 gene, is known to play a pivotal role in the acquisition of drug resistance to chemotherapies in malignancy.