2iei: Difference between revisions
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New page: left|200px<br /><applet load="2iei" size="450" color="white" frame="true" align="right" spinBox="true" caption="2iei, resolution 1.91Å" /> '''Crystal structure of... |
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[[Image:2iei.gif|left|200px]]<br /><applet load="2iei" size=" | [[Image:2iei.gif|left|200px]]<br /><applet load="2iei" size="350" color="white" frame="true" align="right" spinBox="true" | ||
caption="2iei, resolution 1.91Å" /> | caption="2iei, resolution 1.91Å" /> | ||
'''Crystal structure of rabbit muscle glycogen phosphorylase in complex with 3,4-dihydro-2-quinolone'''<br /> | '''Crystal structure of rabbit muscle glycogen phosphorylase in complex with 3,4-dihydro-2-quinolone'''<br /> | ||
==Overview== | ==Overview== | ||
A series of substituted 3,4-dihydro-2-quinolone glycogen phosphorylase | 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== | ==About this Structure== | ||
2IEI is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Oryctolagus_cuniculus Oryctolagus cuniculus] with PLR and FRX as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [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] Full crystallographic information is available from [http:// | 2IEI is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Oryctolagus_cuniculus Oryctolagus cuniculus] with <scene name='pdbligand=PLR:'>PLR</scene> and <scene name='pdbligand=FRX:'>FRX</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [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] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2IEI OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: Phosphorylase]] | [[Category: Phosphorylase]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Birch, A | [[Category: Birch, A M.]] | ||
[[Category: Breed, J.]] | [[Category: Breed, J.]] | ||
[[Category: Kenny, P | [[Category: Kenny, P W.]] | ||
[[Category: Minshull, C.]] | [[Category: Minshull, C.]] | ||
[[Category: Oikonomakos, N | [[Category: Oikonomakos, N G.]] | ||
[[Category: Otterbein, L.]] | [[Category: Otterbein, L.]] | ||
[[Category: Pannifer, A.]] | [[Category: Pannifer, A.]] | ||
| Line 24: | Line 24: | ||
[[Category: Rowsell, S.]] | [[Category: Rowsell, S.]] | ||
[[Category: Schofield, P.]] | [[Category: Schofield, P.]] | ||
[[Category: Whalley, D | [[Category: Whalley, D P.]] | ||
[[Category: Whittamore, P | [[Category: Whittamore, P R.O.]] | ||
[[Category: FRX]] | [[Category: FRX]] | ||
[[Category: PLR]] | [[Category: PLR]] | ||
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[[Category: glycogen phosphorylase]] | [[Category: glycogen phosphorylase]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:51:50 2008'' | ||
