2fix

From Proteopedia

Revision as of 19:59, 12 November 2007 by OCA (Talk | contribs)
(diff) ←Older revision | Current revision (diff) | Newer revision→ (diff)
Jump to: navigation, search
Image:2fix.gif

2fix, resolution 3.50Å

Drag the structure with the mouse to rotate

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-bisphosphatase deficiency OMIM:[229700]

About this Structure

2FIX is a Single protein structure of sequence from Homo sapiens with 870 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

Page seeded by OCA on Mon Nov 12 22:06:02 2007

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/2fix"
Personal tools