2gj4
From Proteopedia
(New page: 200px<br /><applet load="2gj4" size="450" color="white" frame="true" align="right" spinBox="true" caption="2gj4, resolution 1.60Å" /> '''Structure of rabbit ...) |
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| - | [[Image:2gj4.gif|left|200px]]<br /><applet load="2gj4" size=" | + | [[Image:2gj4.gif|left|200px]]<br /><applet load="2gj4" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="2gj4, resolution 1.60Å" /> | caption="2gj4, resolution 1.60Å" /> | ||
'''Structure of rabbit muscle glycogen phosphorylase in complex with ligand'''<br /> | '''Structure of rabbit muscle glycogen phosphorylase in complex with ligand'''<br /> | ||
==Overview== | ==Overview== | ||
| - | Two series of novel thienopyrrole inhibitors of recombinant human liver | + | Two series of novel thienopyrrole inhibitors of recombinant human liver glycogen phosphorylase a (GPa) which are effective in reducing glucose output from rat hepatocytes are described. Representative compounds have been shown to bind at the dimer interface site of the rabbit muscle enzyme by X-ray crystallography. |
==About this Structure== | ==About this Structure== | ||
| - | 2GJ4 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 SO4, PLR and 2TH 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:// | + | 2GJ4 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=SO4:'>SO4</scene>, <scene name='pdbligand=PLR:'>PLR</scene> and <scene name='pdbligand=2TH:'>2TH</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=2GJ4 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Breed, J.]] | [[Category: Breed, J.]] | ||
[[Category: Claire, M.]] | [[Category: Claire, M.]] | ||
| - | [[Category: Oikonomakos, N | + | [[Category: Oikonomakos, N G.]] |
| - | [[Category: Otterbein, L | + | [[Category: Otterbein, L R.]] |
| - | [[Category: Pannifer, A | + | [[Category: Pannifer, A D.]] |
| - | [[Category: Pauptit, R | + | [[Category: Pauptit, R A.]] |
[[Category: Rowsell, S.]] | [[Category: Rowsell, S.]] | ||
[[Category: Tucker, J.]] | [[Category: Tucker, J.]] | ||
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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 17:32:09 2008'' |
Revision as of 15:32, 21 February 2008
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Structure of rabbit muscle glycogen phosphorylase in complex with ligand
Overview
Two series of novel thienopyrrole inhibitors of recombinant human liver glycogen phosphorylase a (GPa) which are effective in reducing glucose output from rat hepatocytes are described. Representative compounds have been shown to bind at the dimer interface site of the rabbit muscle enzyme by X-ray crystallography.
About this Structure
2GJ4 is a Single protein structure of sequence from Oryctolagus cuniculus with , and as ligands. Active as Phosphorylase, with EC number 2.4.1.1 Full crystallographic information is available from OCA.
Reference
Novel thienopyrrole glycogen phosphorylase inhibitors: synthesis, in vitro SAR and crystallographic studies., Whittamore PR, Addie MS, Bennett SN, Birch AM, Butters M, Godfrey L, Kenny PW, Morley AD, Murray PM, Oikonomakos NG, Otterbein LR, Pannifer AD, Parker JS, Readman K, Siedlecki PS, Schofield P, Stocker A, Taylor MJ, Townsend LA, Whalley DP, Whitehouse J, Bioorg Med Chem Lett. 2006 Nov 1;16(21):5567-71. Epub 2006 Aug 30. PMID:16945526
Page seeded by OCA on Thu Feb 21 17:32:09 2008
