1l5r
From Proteopedia
(New page: 200px<br /> <applet load="1l5r" size="450" color="white" frame="true" align="right" spinBox="true" caption="1l5r, resolution 2.10Å" /> '''Human liver glycoge...) |
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| - | [[Image:1l5r. | + | [[Image:1l5r.jpg|left|200px]]<br /><applet load="1l5r" size="350" color="white" frame="true" align="right" spinBox="true" |
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caption="1l5r, resolution 2.10Å" /> | caption="1l5r, resolution 2.10Å" /> | ||
'''Human liver glycogen phosphorylase a complexed with riboflavin, N-Acetyl-beta-D-Glucopyranosylamine and CP-403,700'''<br /> | '''Human liver glycogen phosphorylase a complexed with riboflavin, N-Acetyl-beta-D-Glucopyranosylamine and CP-403,700'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1L5R is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with NBG, PLP, 700, RBF and MRD as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Transferase Transferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.4.4.1 2.4.4.1] Full crystallographic information is available from [http:// | + | 1L5R is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=NBG:'>NBG</scene>, <scene name='pdbligand=PLP:'>PLP</scene>, <scene name='pdbligand=700:'>700</scene>, <scene name='pdbligand=RBF:'>RBF</scene> and <scene name='pdbligand=MRD:'>MRD</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Transferase Transferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.4.4.1 2.4.4.1] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1L5R OCA]. |
==Reference== | ==Reference== | ||
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[[Category: purine site]] | [[Category: purine site]] | ||
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Revision as of 14:16, 15 February 2008
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Human liver glycogen phosphorylase a complexed with riboflavin, N-Acetyl-beta-D-Glucopyranosylamine and CP-403,700
Contents |
Overview
Human liver glycogen phosphorylase (HLGP) catalyzes the breakdown of, glycogen to maintain serum glucose levels and is a therapeutic target for, diabetes. HLGP is regulated by multiple interacting allosteric sites, each, of which is a potential drug binding site. We used surface plasmon, resonance (SPR) to screen for compounds that bind to the purine allosteric, inhibitor site. We determined the affinities of a series of compounds and, solved the crystal structures of three representative ligands with K(D), values from 17-550 microM. The crystal structures reveal that the, affinities are partly determined by ligand-specific water-mediated, hydrogen bonds and side chain movements. These effects could not be, predicted; both crystallographic and SPR studies were required to, understand the important features of binding and together provide a basis, for the design of new allosteric inhibitors targeting this site.
Disease
Known disease associated with this structure: Glycogen storage disease VI OMIM:[232700]
About this Structure
1L5R is a Single protein structure of sequence from Homo sapiens with , , , and as ligands. Active as Transferase, with EC number 2.4.4.1 Full crystallographic information is available from OCA.
Reference
Structure-activity analysis of the purine binding site of human liver glycogen phosphorylase., Ekstrom JL, Pauly TA, Carty MD, Soeller WC, Culp J, Danley DE, Hoover DJ, Treadway JL, Gibbs EM, Fletterick RJ, Day YS, Myszka DG, Rath VL, Chem Biol. 2002 Aug;9(8):915-24. PMID:12204691
Page seeded by OCA on Fri Feb 15 16:16:36 2008
Categories: Homo sapiens | Single protein | Transferase | Carty, M.D. | Culp, J. | Danley, D.E. | Day, Y.S.N. | Ekstrom, J.L. | Fletterick, R.J. | Gibbs, E.M. | Hoover, D.J. | Myszka, D.G. | Pauly, T.A. | Rath, V.L. | Soeller, W.C. | Treadway, J.L. | 700 | MRD | NBG | PLP | RBF | Phosphorylase | Purine site
