Allosteric Modulation of Human P-glycoprotein
نویسندگان
چکیده
منابع مشابه
Allosteric modulation of human P-glycoprotein. Inhibition of transport by preventing substrate translocation and dissociation.
The human multidrug transporter P-glycoprotein (Pgp, ABCB1) contributes to the poor bioavailability of many anticancer and antimicrobial agents as well as to drug resistance at the cellular level. For rational design of effective Pgp inhibitors, a clear understanding of its mechanism of action and functional regulation is essential. In this study, we demonstrate that inhibition of Pgp-mediated ...
متن کاملModulation of P-glycoprotein by Zosuquidar Trihydrochloride
P-glycoprotein (P-gp), a major contributor in multidrug resistance (MDR), is a cell surface drug efflux pump restricting the intracellular accumulation of many agents used in cancer chemotherapy leading to treatment failure. Over expression of P-gp is a significant indicator of poor outcome in cancer including acute myelogenous leukaemia (AML). In addition to its primary drug efflux role, P-gp...
متن کاملEffect of Honey on CYP3A4 Enzyme and P-Glycoprotein Activity in Healthy Human Volunteers
The activity of cytochrome p450 isozyme 3A4 (CYP3A4) enzyme and P-glycoprotein (P-gp) is modulated by grapefruit juice and herbal drugs. CYP3A4 is the major phase I drug metabolizing enzyme and P-gp is an ATP-dependent drug efflux pump that regulates the intestinal absorption of orally administered drugs. Honey is commonly consumed as a dietary supplement. However, its influence on human CY...
متن کاملA Role of P-glycoprotein in Modulation of Antibiotic Pharmacokinetics
P-glycoprotein (P-gp) belongs to superfamily of ABC (ATP-binding cassette) drug transporters. It is expressed in intestines, brain, kidneys, testes, liver, adrenal gland, lungs heart and eyes. This protein functions as a biological barrier by extruding toxic substances and xenobiotics out of cells. P-gp could modulate pharmacokinetics of antibacterial drugs through limitation of their oral abso...
متن کاملModulation of drug-stimulated ATPase activity of human MDR1/P-glycoprotein by cholesterol.
MDR1 (multidrug resistance 1)/P-glycoprotein is an ATP-driven transporter which excretes a wide variety of structurally unrelated hydrophobic compounds from cells. It is suggested that drugs bind to MDR1 directly from the lipid bilayer and that cholesterol in the bilayer also interacts with MDR1. However, the effects of cholesterol on drug-MDR1 interactions are still unclear. To examine these e...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: Journal of Biological Chemistry
سال: 2003
ISSN: 0021-9258
DOI: 10.1074/jbc.m210413200