منابع مشابه
P-glycoprotein transporter in drug development
Drug discovery and development is a complex and time consuming process which requires multidisciplinary expertise (Pracha-yasittikul et al., 2015a). It is true that bioac-tive compounds will become useless if their pharmacokinetic properties are not adequate. Pharmacokinetic properties include absorption (A), distribution (D), metabolism (M), excretion (E) and toxicity (T), or ADMET. ADMET prop...
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P-glycoprotein (P-gp), an efflux membrane transporter, is widely distributed throughout the body and is responsible for limiting cellular uptake and the distribution of xenobiotics and toxic substances. Hundreds of structurally diverse therapeutic agents are substrates to it and it impedes the absorption, permeability, and retention of the drugs, extruding them out of the cells. It is overexpre...
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Autoimmune diseases such as systemic lupus erythematosus (SLE), rheumatoid arthritis (RA) and psoriatic arthritis (PsA) are chronic inflammatory disorders of unknown etiology characterized by a wide range of abnormalities of the immune system that may compromise the function of several organs, such as kidney, heart, joints, brain and skin. Corticosteroids (CCS), synthetic and biologic immunosup...
متن کاملFunctional interactions between P-glycoprotein and CYP3A in drug metabolism.
The interaction between drug-metabolising enzymes and active transporters is an emerging concept in pharmacokinetics. In the gut mucosa, P-glycoprotein and cytochrome P450 (CYP)3A functionally interact in three ways: i) drugs are repeatedly taken up and pumped out of the enterocytes by P-glycoprotein, thus increasing the probability of drugs being metabolised; ii) P-glycoprotein keeps intracell...
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Human P-glycoprotein (P-gp) is an ATP-binding cassette multidrug transporter that confers resistance to a wide range of chemotherapeutic agents in cancer cells by active efflux of the drugs from cells. P-gp also plays a key role in limiting oral absorption and brain penetration and in facilitating biliary and renal elimination of structurally diverse drugs. Thus, identification of drugs or new ...
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ژورنال
عنوان ژورنال: Drug Metabolism and Pharmacokinetics
سال: 1999
ISSN: 0916-1139
DOI: 10.2133/dmpk.14.326