2fix

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Image:2fix.gif

2fix, resolution 3.50Å

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Structure of human liver FBPase complexed with potent benzoxazole allosteric inhibitiors

Contents

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.

Disease

Known disease associated with this structure: Fructose-1,6-bidphosphatase deficiency OMIM:[611570]

About this Structure

2FIX is a Single protein structure of sequence from Homo sapiens with as ligand. Active as Fructose-bisphosphatase, with EC number 3.1.3.11 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

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