2ieg
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(New page: 200px<br /><applet load="2ieg" size="450" color="white" frame="true" align="right" spinBox="true" caption="2ieg, resolution 1.90Å" /> '''Crystal structure of...)
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Revision as of 10:09, 21 November 2007
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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 with PLR and FRY as ligands. Active as Phosphorylase, with EC number 2.4.1.1 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 Wed Nov 21 12:16:50 2007
Categories: Oryctolagus cuniculus | Phosphorylase | Single protein | Birch, A.M. | Breed, J. | Kenny, P.W. | Minshull, C. | Oikonomakos, N.G. | Otterbein, L. | Pannifer, A. | Pauptit, R. | Rowsell, S. | Schofield, P. | Whalley, D.P. | Whittamore, P.R.O. | FRY | PLR | Diabetes | Glycogen phosphorylase | Glypho
