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Reversal of P-glycoprotein-mediated multidrug resistance by a potent cyclopropyldibenzosuberane modulator, LY335979.
LY335979 is an extremely potent, efficacious modulator that apparently lacks pharmacokinetic interactions with coadministered anticancer drugs and is, therefore, an exciting new agent for clinical evaluation for reversal of Pgp-associated MDR.
Selectivity of the multidrug resistance modulator, LY335979, for P-glycoprotein and effect on cytochrome P-450 activities.
- A. Dantzig, R. Shepard, S. Wrighton
- BiologyThe Journal of pharmacology and experimental…
- 1 August 1999
LY335979 is an extremely potent Pgp modulator, and not MRP1 or MRP2, modulator and has a significantly lower affinity for CYP3A than for Pgp, which is in good agreement with the previously determined K(i) value.
Three-dimensional quantitative structure-activity relationships of inhibitors of P-glycoprotein.
Three-dimensional quantitative structure-activity relationship (3D-QSAR) models were generated using in vitro data associated with inhibition of P-gp function and may prove to be of value for prediction of molecules that may modulate one or more P- gp binding sites.
The multidrug resistance protein 5 (ABCC5) confers resistance to 5-fluorouracil and transports its monophosphorylated metabolites
- S. Pratt, R. Shepard, R. Kandasamy, P. Johnston, William L Perry, A. Dantzig
- Biology, ChemistryMolecular Cancer Therapeutics
- 1 May 2005
The present study shows that the ATP-dependent multidrug resistance protein-5 (MRP5, ABCC5) confers resistance to 5-FU by transporting the monophosphate metabolites.
Application of three-dimensional quantitative structure-activity relationships of P-glycoprotein inhibitors and substrates.
The degree of similarity in rank ordering prediction by these inhibitor pharmacophore models generated to date confirms a likely overlap in the sites to which the three P-gp substrates used in these studies (verapamil, vinblastine, and digoxin) bind.
Considerations in the design and development of transport inhibitors as adjuncts to drug therapy.
Uptake of the cephalosporin, cephalexin, by a dipeptide transport carrier in the human intestinal cell line, Caco-2.
Modulation of P‐glycoprotein but not MRP1‐ or BCRP‐mediated drug resistance by LY335979
It is demonstrated that LY335979 is highly specific for Pgp and does not modulate MRP1‐ or BCRP‐mediated resistance and can be used in combination with mitoxantrone and vinorelbine in tumor cells.
Association of intestinal peptide transport with a protein related to the cadherin superfamily.
A monoclonal antibody that blocked uptake of cephalexin was used to identify and clone a gene that encodes an approximately 92-kilodalton membrane protein that was associated with the acquisition of peptide transport activity by transport-deficient cells.
Synthesis, crystallization, and biological evaluation of an orally active prodrug of gemcitabine.
Valproate amide 3 is orally bioavailable and releases gemcitabine into the systemic circulation after passing through the intestinal mucosa and has entered clinical trials and is being evaluated as a potential new anticancer agent.