Literature DB >> 8224162

Differential inhibition by cyclosporins of primary-active ATP-dependent transporters in the hepatocyte canalicular membrane.

M Böhme1, M Büchler, M Müller, D Keppler.   

Abstract

The distinct ATP-dependent transporters for taurocholate, leukotriene C4, and daunorubicin, studied in rat liver canalicular membrane vesicles, are sensitive to inhibition by cyclosporin A and its non-immunosuppressive analog PSC 833. Ki values for cyclosporin A were 0.2, 3.4 and 1.5 microM for the transport of taurocholate, leukotriene C4, and daunorubicin, respectively. The corresponding Ki values for PSC 833 were 0.6, 29, and 0.3 microM. Both inhibitors were competitive with respect to the three substrates. The cyclosporins serve as new and potent tools to interfere with different potency with the distinct ATP-dependent export carriers in the hepatocyte canalicular membrane.

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Year:  1993        PMID： 8224162     DOI： 10.1016/0014-5793(93)80403-h

Source DB:  PubMed          Journal:  FEBS Lett        ISSN： 0014-5793            Impact factor:   4.124


  21 in total

1.  Transfected rat cMOAT is functionally expressed on the apical membrane in Madin-Darby canine kidney (MDCK) cells.

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Review 3.  Drug-induced cholestasis.

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4.  Cyclosporin A reduces canalicular membrane fluidity and regulates transporter function in rats.

Authors:  S Yasumiba; S Tazuma; H Ochi; K Chayama; G Kajiyama
Journal:  Biochem J       Date:  2001-03-15       Impact factor: 3.857

5.  Characterization of anti-Toxoplasma activity of SDZ 215-918, a cyclosporin derivative lacking immunosuppressive and peptidyl-prolyl-isomerase-inhibiting activity: possible role of a P glycoprotein in Toxoplasma physiology.

Authors:  J A Silverman; M L Hayes; B J Luft; K A Joiner
Journal:  Antimicrob Agents Chemother       Date:  1997-09       Impact factor: 5.191

6.  Comprehensive Synthesis of Amino Acid-Derived Thiazole Peptidomimetic Analogues to Understand the Enigmatic Drug/Substrate-Binding Site of P-Glycoprotein.

Authors:  Bhargav A Patel; Biebele Abel; Anna Maria Barbuti; Uday Kiran Velagapudi; Zhe-Sheng Chen; Suresh V Ambudkar; Tanaji T Talele
Journal:  J Med Chem       Date:  2018-01-23       Impact factor: 7.446

7.  Biliary excretion of 17beta-estradiol 17beta-D-glucuronide is predominantly mediated by cMOAT/MRP2.

Authors:  A Morikawa; Y Goto; H Suzuki; T Hirohashi; Y Sugiyama
Journal:  Pharm Res       Date:  2000-05       Impact factor: 4.200

8.  Association of ABCC2 and CDDP-Resistance in Two Sublines Resistant to CDDP Derived from a Human Nasopharyngeal Carcinoma Cell Line.

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Journal:  J Oncol       Date:  2010-06-13       Impact factor: 4.375

9.  The multidrug transporter, P-glycoprotein, actively mediates cholesterol redistribution in the cell membrane.

Authors:  Alexia Garrigues; Alexandre E Escargueil; Stephane Orlowski
Journal:  Proc Natl Acad Sci U S A       Date:  2002-07-26       Impact factor: 11.205

Review 10.  Biosynthesis and trafficking of the bile salt export pump, BSEP: therapeutic implications of BSEP mutations.

Authors:  Carol J Soroka; James L Boyer
Journal:  Mol Aspects Med       Date:  2013-05-15
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