Interaction of the P-glycoprotein Multidrug Transporter with Peptides and Ionophores
نویسندگان
چکیده
منابع مشابه
The P-glycoprotein multidrug transporter.
Pgp (P-glycoprotein) (ABCB1) is an ATP-powered efflux pump which can transport hundreds of structurally unrelated hydrophobic amphipathic compounds, including therapeutic drugs, peptides and lipid-like compounds. This 170 kDa polypeptide plays a crucial physiological role in protecting tissues from toxic xenobiotics and endogenous metabolites, and also affects the uptake and distribution of man...
متن کاملEvaluation the interaction of ABC multidrug transporter MDR1 with thymoquinone: substrate or inhibitor?
Objective(s): Thymoquinone (TQ) has valuable medical properties like anticancer effects. Development of multidrug resistance (MDR) phenotype is one of the most important factors in failure of cancer chemotherapy. The aim of this study was to evaluate the mode of interaction of TQ and MDR1, a major MDR-related protein in gastric cancer drug resistant EPG85-257RDB cells,...
متن کاملBivalent probes of the human multidrug transporter P-glycoprotein.
A small library of bivalent agents was designed to probe the substrate binding sites of the human multidrug transporter P-glycoprotein (P-gp). The bivalent agents were composed of two copies of the P-gp substrate emetine, linked by tethers of varied composition. An optimum distance between the emetine molecules of approximately 10 A was found to be necessary for blocking transport of the known ...
متن کاملCharacterization of two pharmacophores on the multidrug transporter P-glycoprotein.
The multidrug transporter P-glycoprotein is a plasma membrane protein involved in cell and tissue detoxification and the multidrug resistance (MDR) phenotype. It actively expels from cells a number of cytotoxic molecules, all amphiphilic but chemically unrelated. We investigated the molecular characteristics involved in the binding selectivity of P-glycoprotein by means of a molecular modeling ...
متن کاملAnalysis of Multidrug Transporter in Living Cells. Inhibition of P-glycoprotein-mediated Efflux of Anthracyclines by Ionophores
One of the major obstacles of chemotherapy is that, after repeated treatments, cellular resistance to the drug appears. The problem is that the tumor cells become resistant not only to the drugs which have been used during the treatment but also to other drugs which are structurally and functionally unrelated. This is termed 'multidrug resistance' (MDR). MDR is frequently associated with decrea...
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: 1995
ISSN: 0021-9258
DOI: 10.1074/jbc.270.17.10334