2fix

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Image:2fix.gif

Template:STRUCTURE 2fix

Structure of human liver FBPase complexed with potent benzoxazole allosteric inhibitiors


Overview

A series of novel benzoxazole benzenesulfonamides was synthesized as inhibitors of fructose-1,6-bisphosphatase (FBPase-1). Extensive SAR studies led to a potent inhibitor, 53, with an IC(50) of 0.57microM. Compound 17 exhibited excellent bioavailability and a good pharmacokinetic profile in rats.

About this Structure

2FIX is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Benzoxazole benzenesulfonamides as allosteric inhibitors of fructose-1,6-bisphosphatase., Lai C, Gum RJ, Daly M, Fry EH, Hutchins C, Abad-Zapatero C, von Geldern TW, Bioorg Med Chem Lett. 2006 Apr 1;16(7):1807-10. Epub 2006 Jan 30. PMID:16446092 Page seeded by OCA on Sun May 4 03:57:16 2008

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