2ieg

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{{STRUCTURE_2ieg| PDB=2ieg | SCENE= }}
{{STRUCTURE_2ieg| PDB=2ieg | SCENE= }}
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'''Crystal structure of rabbit muscle glycogen phosphorylase in complex with 3,4-dihydro-2-quinolone'''
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===Crystal structure of rabbit muscle glycogen phosphorylase in complex with 3,4-dihydro-2-quinolone===
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==Overview==
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A series of substituted 3,4-dihydro-2-quinolone glycogen phosphorylase inhibitors, which have potential as antidiabetic agents, is described. Initial members of the series showed good enzyme inhibitory potency but poor physical properties. Optimisation of the 1-substituent led to 2,3-dihydroxypropyl compounds which showed good in vitro potency and improved physical properties, together with good DMPK profiles and acute in vivo efficacy in a rat model. X-ray crystallographic data are presented, showing an unexpected variety of binding orientations at the dimer interface site.
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(as it appears on PubMed at http://www.pubmed.gov), where 17095214 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17095214}}
==About this Structure==
==About this Structure==
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[[Category: Glycogen phosphorylase]]
[[Category: Glycogen phosphorylase]]
[[Category: Glypho]]
[[Category: Glypho]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 07:24:28 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 14:29:26 2008''

Revision as of 11:29, 29 July 2008

Image:2ieg.png

Template:STRUCTURE 2ieg

Crystal structure of rabbit muscle glycogen phosphorylase in complex with 3,4-dihydro-2-quinolone

Template:ABSTRACT PUBMED 17095214

About this Structure

2IEG is a Single protein structure of sequence from Oryctolagus cuniculus. Full crystallographic information is available from OCA.

Reference

Development of potent, orally active 1-substituted-3,4-dihydro-2-quinolone glycogen phosphorylase inhibitors., Birch AM, Kenny PW, Oikonomakos NG, Otterbein L, Schofield P, Whittamore PR, Whalley DP, Bioorg Med Chem Lett. 2007 Jan 15;17(2):394-9. Epub 2006 Oct 19. PMID:17095214

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