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2fix
From Proteopedia
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(New page: 200px<br /> <applet load="2fix" size="450" color="white" frame="true" align="right" spinBox="true" caption="2fix, resolution 3.50Å" /> '''Structure of human ...)
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Revision as of 19:59, 12 November 2007
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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-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
