1l7x

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[[Image:1l7x.gif|left|200px]]
[[Image:1l7x.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1l7x |SIZE=350|CAPTION= <scene name='initialview01'>1l7x</scene>, resolution 2.30&Aring;
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The line below this paragraph, containing "STRUCTURE_1l7x", 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=700:[5-CHLORO-1H-INDOL-2-CARBONYL-PHENYLALANINYL]-AZETIDINE-3-CARBOXYLIC+ACID'>700</scene>, <scene name='pdbligand=CFF:CAFFEINE'>CFF</scene>, <scene name='pdbligand=MRD:(4R)-2-METHYLPENTANE-2,4-DIOL'>MRD</scene>, <scene name='pdbligand=NBG:1-N-ACETYL-BETA-D-GLUCOSAMINE'>NBG</scene>, <scene name='pdbligand=PLP:PYRIDOXAL-5&#39;-PHOSPHATE'>PLP</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_1l7x| PDB=1l7x | SCENE= }}
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|RELATEDENTRY=[[1l5q|1L5Q]], [[1l5r|1L5R]], [[1l5s|1L5S]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1l7x FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1l7x OCA], [http://www.ebi.ac.uk/pdbsum/1l7x PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1l7x RCSB]</span>
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}}
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'''Human liver glycogen phosphorylase b complexed with caffeine, N-acetyl-beta-D-glucopyranosylamine, and CP-403,700'''
'''Human liver glycogen phosphorylase b complexed with caffeine, N-acetyl-beta-D-glucopyranosylamine, and CP-403,700'''
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[[Category: Soeller, W C.]]
[[Category: Soeller, W C.]]
[[Category: Treadway, J L.]]
[[Category: Treadway, J L.]]
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[[Category: phosphorylase]]
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[[Category: Phosphorylase]]
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[[Category: purine site]]
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[[Category: Purine site]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 23:38:46 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 21:59:18 2008''
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Revision as of 20:38, 2 May 2008

Image:1l7x.gif

Template:STRUCTURE 1l7x

Human liver glycogen phosphorylase b complexed with caffeine, N-acetyl-beta-D-glucopyranosylamine, and CP-403,700


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.

About this Structure

1L7X is a Single protein structure of sequence from Homo sapiens. 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 May 2 23:38:46 2008

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OCA

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