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P-glycoprotein family

P-Glycoprotein (P-gp), a member of the adenosine triphosphate (ATP)-binding cassette family of membrane transporters, is encoded by the human multidrug-resistance (MDRl, ABCBl) gene (15). This integral membrane protein serves as an... [Pg.25]

Other mechanisms of interaction have also been reported, such as altered activity of other enzymes within the CYP450 family (14—17). Moreover, GFJ may also inhibit the intestinal P-glycoprotein (P-gp)-mediated efflux transport of drugs such as cyclosporine to increase its oral bioavailability (18-21). GFJ and other fruit juices have recently been shown to be potent in vitro inhibitors of a number of organic anion-transporting polypeptides (OATPs) (22,23). [Pg.148]

BSEP also known as sister-P-glycoprotein (SPGP) was originally cloned from pig liver (185). BSEP is localized on the canalicular membrane of hepa-tocytes and is responsible for the secretion of bile salts across the canalicular membrane into bile. BSEP appears to be the predominant bile salt efflux system for hepatocytes, and is a critical component in the enterohepatic circulation of bile acids. A number of mutations in the transporter were found to the basis for progressive familial intrahepatic cholestasis type 2 (PFIC2) (186-188). Mutations found in PFIC2 patients include frameshifts, missense mutations, and premature termination codons. Most PFIC2 patients lack immunohistochemically detectable BSEP in their liver. Recently, seven... [Pg.128]

Endicott JA, Sarangi F, Ling V. Complete cDNA sequences encoding the Chinese hamster P-glycoprotein gene family. DNA Seq 1991 2(2) 89-101. [Pg.433]


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P-glycoprotein

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