2g9q

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{{STRUCTURE_2g9q| PDB=2g9q | SCENE= }}
{{STRUCTURE_2g9q| PDB=2g9q | SCENE= }}
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'''The crystal structure of the glycogen phosphorylase b- 1AB complex'''
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===The crystal structure of the glycogen phosphorylase b- 1AB complex===
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==Overview==
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Iminosugars DAB (5), isofagomine (9), and several N-substituted derivatives have been identified as potent inhibitors of liver glycogen phosphorylase a (IC(50) = 0.4-1.2 microM) and of basal and glucagon-stimulated glycogenolysis (IC(50) = 1-3 microM). The X-ray structures of 5, 9, and its N-3-phenylpropyl analogue 8 in complex with rabbit muscle glycogen phosphorylase (GPb) shows that iminosugars bind tightly at the catalytic site in the presence of the substrate phosphate and induce conformational changes that characterize the R-state conformation of the enzyme. Charged nitrogen N1 is within hydrogen-bonding distance with the carbonyl oxygen of His377 (5) and in ionic contact with the substrate phosphate oxygen (8 and 9). Our findings suggest that the inhibitors function as oxocarbenium ion transition-state analogues. The conformational change to the R state provides an explanation for previous findings that 5, unlike inhibitors that favor the T state, promotes phosphorylation of GPb in hepatocytes with sequential inactivation of glycogen synthase.
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(as it appears on PubMed at http://www.pubmed.gov), where 16970395 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16970395}}
==About this Structure==
==About this Structure==
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[[Category: Rational inhibitor design]]
[[Category: Rational inhibitor design]]
[[Category: Structure]]
[[Category: Structure]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 04:51:35 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 14:33:44 2008''

Revision as of 11:33, 29 July 2008

Image:2g9q.png

Template:STRUCTURE 2g9q

The crystal structure of the glycogen phosphorylase b- 1AB complex

Template:ABSTRACT PUBMED 16970395

About this Structure

2G9Q is a Single protein structure of sequence from Oryctolagus cuniculus. Full crystallographic information is available from OCA.

Reference

Iminosugars as potential inhibitors of glycogenolysis: structural insights into the molecular basis of glycogen phosphorylase inhibition., Oikonomakos NG, Tiraidis C, Leonidas DD, Zographos SE, Kristiansen M, Jessen CU, Norskov-Lauritsen L, Agius L, J Med Chem. 2006 Sep 21;49(19):5687-701. PMID:16970395

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