1z6q

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[[Image:1z6q.jpg|left|200px]]
[[Image:1z6q.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 1z6q |SIZE=350|CAPTION= <scene name='initialview01'>1z6q</scene>, resolution 2.03&Aring;
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The line below this paragraph, containing "STRUCTURE_1z6q", 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=195:4-{2,4-BIS[(3-NITROBENZOYL)AMINO]PHENOXY}PHTHALIC+ACID'>195</scene>, <scene name='pdbligand=LLP:2-LYSINE(3-HYDROXY-2-METHYL-5-PHOSPHONOOXYMETHYL-PYRIDIN-4-YLMETHANE)'>LLP</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_1z6q| PDB=1z6q | SCENE= }}
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|RELATEDENTRY=[[1z6p|1Z6P]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1z6q FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1z6q OCA], [http://www.ebi.ac.uk/pdbsum/1z6q PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1z6q RCSB]</span>
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}}
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'''Glycogen phosphorylase with inhibitor in the AMP site'''
'''Glycogen phosphorylase with inhibitor in the AMP site'''
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[[Category: Kristiansen, M.]]
[[Category: Kristiansen, M.]]
[[Category: Westergaard, N.]]
[[Category: Westergaard, N.]]
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[[Category: allosteric]]
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[[Category: Allosteric]]
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[[Category: glycogen metabolism]]
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[[Category: Glycogen metabolism]]
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[[Category: glycogen phosphorylase b]]
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[[Category: Glycogen phosphorylase b]]
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[[Category: inhibition]]
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[[Category: Inhibition]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 17:14:41 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 01:30:14 2008''
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Revision as of 14:14, 3 May 2008

Image:1z6q.jpg

Template:STRUCTURE 1z6q

Glycogen phosphorylase with inhibitor in the AMP site


Overview

Inhibition of glycogen phosphorylase (GP) has attracted considerable attention during the last five to 10 years as a means of treating the elevated hepatic glucose production seen in patients with type 2 diabetes. Several different GP inhibitors binding to various binding sites of the GP enzyme have been reported in the literature. In this paper we report on a novel class of compounds that have been identified as potent GP inhibitors. Their synthesis, mode of binding to the allosteric AMP site as well as in vitro data on GP inhibition are shown. The most potent inhibitor was found to be 4-[2,4-bis-(3-nitrobenzoylamino)phenoxy]phthalic acid (4j) with an IC(50) value of 74 nM. This compound together with a closely related analogue was further characterized by enzyme kinetics and in primary rat hepatocytes.

About this Structure

1Z6Q is a Single protein structure of sequence from Oryctolagus cuniculus. Full crystallographic information is available from OCA.

Reference

Identification, synthesis, and characterization of new glycogen phosphorylase inhibitors binding to the allosteric AMP site., Kristiansen M, Andersen B, Iversen LF, Westergaard N, J Med Chem. 2004 Jul 1;47(14):3537-45. PMID:15214781 Page seeded by OCA on Sat May 3 17:14:41 2008

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