2fie

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[[Image:2fie.gif|left|200px]]
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{{Seed}}
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[[Image:2fie.png|left|200px]]
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{{STRUCTURE_2fie| PDB=2fie | SCENE= }}
{{STRUCTURE_2fie| PDB=2fie | SCENE= }}
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'''Structure of human liver FBPase complexed with potent benzoxazole allosteric inhibitors'''
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===Structure of human liver FBPase complexed with potent benzoxazole allosteric inhibitors===
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==Overview==
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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.
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The line below this paragraph, {{ABSTRACT_PUBMED_16446092}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 16446092 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16446092}}
==About this Structure==
==About this Structure==
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==Reference==
==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:[http://www.ncbi.nlm.nih.gov/pubmed/16446092 16446092]
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:[http://www.ncbi.nlm.nih.gov/pubmed/16446092 16446092]
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Benzoxazole benzenesulfonamides are novel allosteric inhibitors of fructose-1,6-bisphosphatase with a distinct binding mode., von Geldern TW, Lai C, Gum RJ, Daly M, Sun C, Fry EH, Abad-Zapatero C, Bioorg Med Chem Lett. 2006 Apr 1;16(7):1811-5. Epub 2006 Jan 25. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/16442285 16442285]
[[Category: Fructose-bisphosphatase]]
[[Category: Fructose-bisphosphatase]]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Benzoxazole]]
[[Category: Benzoxazole]]
[[Category: Intersubunit allosteric inhibitors of human liver fbpase]]
[[Category: Intersubunit allosteric inhibitors of human liver fbpase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 03:56:07 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 14:54:52 2008''

Revision as of 11:54, 27 July 2008

Image:2fie.png

Template:STRUCTURE 2fie

Structure of human liver FBPase complexed with potent benzoxazole allosteric inhibitors

Template:ABSTRACT PUBMED 16446092

About this Structure

2FIE 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

Benzoxazole benzenesulfonamides are novel allosteric inhibitors of fructose-1,6-bisphosphatase with a distinct binding mode., von Geldern TW, Lai C, Gum RJ, Daly M, Sun C, Fry EH, Abad-Zapatero C, Bioorg Med Chem Lett. 2006 Apr 1;16(7):1811-5. Epub 2006 Jan 25. PMID:16442285

Page seeded by OCA on Sun Jul 27 14:54:52 2008

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