Sj/011

Role of Serum and Glucocoritcoid [sic] inducible Kinase SGK1 in the regulation of glucose transport

von Dr. Sankarganesh Jeyaraj

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[1.] Sj/Fragment 011 01 - Diskussion Zuletzt bearbeitet: 2016-11-28 21:00:48 WiseWoman

Fragment, Gesichtet, SMWFragment, Schutzlevel sysop, Sj, Uldry and Thorens 2004, Verschleierung

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Quelle: Uldry and Thorens 2004 Seite(n): 481, Zeilen: r.col: 48ff

[An iodinated derivative] of forskolin (7-aminoalkylcarbamate) with a very high affinity (IC50 200 nM) has also been described (37). Glucose transport activity of GLUT1 is inhibited by HgCl2 (IC50 3.5 μM), phloretin (IC50 49 μM), phlorizin (IC50 355 μM) and 4,6-O-ethylidene-D-glucose (IC50 12 mM), which bind to the external glucose binding site where glutamine 161 appears to be critical for inhibitor binding (16). 16. Mueckler,M, Makepeace,C: Transmembrane segment 12 of the Glut1 glucose transporter is an outer helix and is not directly involved in the transport mechanism. J.Biol.Chem. 281:36993-36998, 2006 37. Harrison,SA, Buxton,JM, Czech,MP: Suppressed intrinsic catalytic activity of GLUT1 glucose transporters in insulin-sensitive 3T3-L1 adipocytes. Proc.Natl.Acad.Sci.U.S.A 88:7839-7843, 1991

An iodinated derivative of forskolin (7-aminoalkylcarbamate) with a very high affinity (IC50 200 nM) has also been described [51]. Glucose transport activity of GLUT1 is inhibited by HgCl2 (IC50 3.5 μM), phloretin (IC50 49 μM) phlorizin (IC50 355 μM) [37] and 4,6-O-ethylidene-d-glucose (IC50 12 mM), which binds to the external glucose binding site where glutamine 161 appears to be critical for inhibitor binding [54] 37. Kasahara T, Kasahara M (1996) Expression of the rat GLUT1 glucose transporter in the yeast Saccharomyces cerevisiae. Biochem J 315:177–182 51. Morris DI, Robbins JD, Ruoho AE, Sutkowski EM, Seamon KB (1991) Forskolin photoaffinity labels with specificity for adenylyl cyclase and the glucose transporter. J Biol Chem 266:13377–13384 54. Mueckler M, Weng W, Kruse M (1994) Glutamine 161 of Glut1 glucose transporter is critical for transport activity and exofacial ligand binding. J Biol Chem 269:20533–20538

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Sichter (Hindemith) LieschenMueller

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