2ieg

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[[Image:2ieg.gif|left|200px]]
[[Image:2ieg.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2ieg |SIZE=350|CAPTION= <scene name='initialview01'>2ieg</scene>, resolution 1.90&Aring;
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The line below this paragraph, containing "STRUCTURE_2ieg", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=FRY:(2S)-N-[(3S)-1-(2-AMINO-2-OXOETHYL)-2-OXO-1,2,3,4-TETRAHYDROQUINOLIN-3-YL]-2-CHLORO-2H-THIENO[2,3-B]PYRROLE-5-CARBOXAMIDE'>FRY</scene>, <scene name='pdbligand=PLR:(5-HYDROXY-4,6-DIMETHYLPYRIDIN-3-YL)METHYL+DIHYDROGEN+PHOSPHATE'>PLR</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Phosphorylase Phosphorylase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.4.1.1 2.4.1.1] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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-->
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|DOMAIN=
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{{STRUCTURE_2ieg| PDB=2ieg | SCENE= }}
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|RELATEDENTRY=[[2iei|2IEI]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2ieg FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2ieg OCA], [http://www.ebi.ac.uk/pdbsum/2ieg PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2ieg RCSB]</span>
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}}
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'''Crystal structure of rabbit muscle glycogen phosphorylase in complex with 3,4-dihydro-2-quinolone'''
'''Crystal structure of rabbit muscle glycogen phosphorylase in complex with 3,4-dihydro-2-quinolone'''
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[[Category: Whalley, D P.]]
[[Category: Whalley, D P.]]
[[Category: Whittamore, P R.O.]]
[[Category: Whittamore, P R.O.]]
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[[Category: diabetes]]
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[[Category: Diabetes]]
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[[Category: glycogen phosphorylase]]
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[[Category: Glycogen phosphorylase]]
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[[Category: glypho]]
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[[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 Mon Mar 31 03:43:12 2008''
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Revision as of 04:24, 4 May 2008

Image:2ieg.gif

Template:STRUCTURE 2ieg

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


Overview

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.

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 Page seeded by OCA on Sun May 4 07:24:28 2008

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