1z6p

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{{STRUCTURE_1z6p| PDB=1z6p | SCENE= }}
{{STRUCTURE_1z6p| PDB=1z6p | SCENE= }}
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'''Glycogen phosphorylase AMP site inhibitor complex'''
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===Glycogen phosphorylase AMP site inhibitor complex===
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==Overview==
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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.
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The line below this paragraph, {{ABSTRACT_PUBMED_15214781}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 15214781 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15214781}}
==About this Structure==
==About this Structure==
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[[Category: Glycogen phosphorylase b]]
[[Category: Glycogen phosphorylase b]]
[[Category: Inhibition]]
[[Category: Inhibition]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 17:14:32 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 13:13:02 2008''

Revision as of 10:13, 29 July 2008

Image:1z6p.png

Template:STRUCTURE 1z6p

Glycogen phosphorylase AMP site inhibitor complex

Template:ABSTRACT PUBMED 15214781

About this Structure

1Z6P 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

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