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Titolo:
Regulation of biliary drug efflux pump expression by hormones and xenobiotics
Autore:
Fardel, O; Payen, L; Courtois, A; Vernhet, L; Lecureur, V;
Indirizzi:
Fac Pharm, INSERM, U456, F-35043 Rennes, France Fac Pharm Rennes France F-35043 rm, INSERM, U456, F-35043 Rennes, France
Titolo Testata:
TOXICOLOGY
fascicolo: 1, volume: 167, anno: 2001,
pagine: 37 - 46
SICI:
0300-483X(20011005)167:1<37:ROBDEP>2.0.ZU;2-F
Fonte:
ISI
Lingua:
ENG
Soggetto:
P-GLYCOPROTEIN EXPRESSION; RESISTANCE GENE-EXPRESSION; ORGANIC ANION TRANSPORTER; CONJUGATE EXPORT PUMP; RAT-LIVER CELLS; PROTEIN-2 MRP2 GENE; MULTIDRUG-RESISTANCE; MESSENGER-RNA; UP-REGULATION; CULTURED RAT;
Keywords:
bile salt export pump; hepatocytes; hormone; multidrug resistance-associated protein 2; P-glycoprotein; xenobiotic;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
69
Recensione:
Indirizzi per estratti:
Indirizzo: Fardel, O Fac Pharm, INSERM, U456, 2 Ave Pr L Bernard, F-35043 Rennes, France Fac Pharm 2 Ave Pr L Bernard Rennes France F-35043 nnes, France
Citazione:
O. Fardel et al., "Regulation of biliary drug efflux pump expression by hormones and xenobiotics", TOXICOLOGY, 167(1), 2001, pp. 37-46

Abstract

Biliary elimination of endogenous compounds and xenobiotics usually requires carrier-mediated systems allowing movement across the canalicular membrane of hepatocytes. The major systems implicated belong to the ATP binding cassette transporter family: P-glycoprotein (P-gp) and multidrug resistance-associated protein 2 (MRP2), principally mediate the passage into the bile of cationic and anionic compounds, respectively, whereas the bile salt export pump (BSEP) handles biliary acids and also some anticancer drugs. Expression of these canalicular proteins can be altered in response to various hormones and structurally unrelated xenobiotics. Indeed, glucocorticoids up-regulate expression of both MRP2 and BSEP in rat hepatocytes, whereas insulin induces P-gp. P-gp expression is also up-regulated by numerous chemical carcinogens, such as polycyclic aromatic hydrocarbons and 2-acetylaminofluorene and by some anticancer drugs, such as anthracyclins. 2-Acetylaminofluorene also induces MRP2; in addition, expression of this transporter in livercells is increased in response to various drugs, such as the barbiturate phenobarbital, the chemopreventive agent, oltipraz and the anticancer drug, cisplatin. Most of the chemical inducers acting on canalicular transporter levels are well-known to up-regulate some hepatic drug metabolizing enzymes, suggesting a coordinate regulation of liver detoxifying proteins in response to these compounds. (C) 2001 Elsevier Science Ireland Ltd. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/07/20 alle ore 05:24:57