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Biochemical, cellular, and pharmacological aspects of the multidrug transporter.
- S. Ambudkar, S. Dey, C. Hrycyna, M. Ramachandra, I. Pastan, M. Gottesman
- Medicine, Biology
- Annual review of pharmacology and toxicology
Considerable evidence has accumulated indicating that the multidrug transporter or P-glycoprotein plays a role in the development of simultaneous resistance to multiple cytotoxic drugs in cancer… Expand
A "Silent" Polymorphism in the MDR1 Gene Changes Substrate Specificity
Synonymous single-nucleotide polymorphisms (SNPs) do not produce altered coding sequences, and therefore they are not expected to change the function of the protein in which they occur. We report… Expand
P-glycoprotein: from genomics to mechanism
Resistance to chemically different natural product anti-cancer drugs (multidrug resistance, or MDR) results from decreased drug accumulation, resulting from expression of one or more ATP-dependent… Expand
Brca1 breast tumors contain distinct CD44+/CD24- and CD133+ cells with cancer stem cell characteristics
- Mollie H. Wright, A. M. Calcagno, C. D. Salcido, Marisa D Carlson, S. Ambudkar, L. Varticovski
- Biology, Medicine
- Breast Cancer Research
- 1 February 2008
IntroductionWhether cancer stem cells occur in BRCA1-associated breast cancer and contribute to therapeutic response is not known.MethodsWe generated and characterized 16 cell lines from five… Expand
Peripheral CB1 cannabinoid receptor blockade improves cardiometabolic risk in mouse models of obesity.
Obesity and its metabolic consequences are a major public health concern worldwide. Obesity is associated with overactivity of the endocannabinoid system, which is involved in the regulation of… Expand
Reconstitution of functional water channels in liposomes containing purified red cell CHIP28 protein.
Water rapidly crosses the plasma membranes of red blood cells (RBCs) and renal tubules through highly specialized channels. CHIP28 is an abundant integral membrane protein in RBCs and renal tubules,… Expand
HIV-1 protease inhibitors are substrates for the MDR1 multidrug transporter.
The FDA approved HIV-1 protease inhibitors, ritonavir, saquinavir, and indinavir, are very effective in inhibiting HIV-1 replication, but their long-term efficacy is unknown. Since in vivo efficacy… Expand
Modulation of P-glycoprotein expression and function by curcumin in multidrug-resistant human KB cells.
- S. Anuchapreeda, P. Leechanachai, M. M. Smith, S. Ambudkar, P. Limtrakul
- Medicine, Chemistry
- Biochemical pharmacology
- 15 August 2002
Multidrug resistance (MDR) is a phenomenon that is often associated with decreased intracellular drug accumulation in the tumor cells of a patient, resulting from enhanced drug efflux. It is often… Expand
Sunitinib (Sutent, SU11248), a Small-Molecule Receptor Tyrosine Kinase Inhibitor, Blocks Function of the ATP-Binding Cassette (ABC) Transporters P-Glycoprotein (ABCB1) and ABCG2
- S. Shukla, R. Robey, S. Bates, S. Ambudkar
- Medicine, Chemistry
- Drug Metabolism and Disposition
- 1 February 2009
Sunitinib malate (Sutent, SU11248) is a small-molecule receptor tyrosine kinase inhibitor that inhibits cellular signaling of multiple targets such as the platelet-derived growth factor receptors and… Expand
Imatinib mesylate and nilotinib (AMN107) exhibit high-affinity interaction with ABCG2 on primitive hematopoietic stem cells
The majority of chronic phase chronic myeloid leukemia (CML) patients treated with the tyrosine kinase inhibitor (TKI) imatinib mesylate maintain durable responses to the drug. However, most patients… Expand