1ggn

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{{STRUCTURE_1ggn| PDB=1ggn | SCENE= }}
{{STRUCTURE_1ggn| PDB=1ggn | SCENE= }}
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'''Structures of glycogen phosphorylase-inhibitor complexes and the implications for structure-based drug design'''
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===Structures of glycogen phosphorylase-inhibitor complexes and the implications for structure-based drug design===
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==Overview==
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Glucopyranosylidene spirothiohydantoin (TH) has been identified as a potential inhibitor of both muscle and liver glycogen phosphorylase b (GPb) and a (GPa) and shown to diminish liver GPa activity in vitro. Kinetic experiments reported here show that TH inhibits muscle GPb competitively with respect to both substrates phosphate (K(i)=2.3 microM) and glycogen (K(i)=2.8 microM). The structure of the GPb-TH complex has been determined at a resolution of 2.26 A and refined to a crystallographic R value of 0.193 (R(free)=0.211). The structure of GPb-TH complex reveals that the inhibitor can be accommodated in the catalytic site of T-state GPb with very little change of the tertiary structure, and provides a basis of understanding potency and specificity of the inhibitor. The glucopyranose moiety makes the standard hydrogen bonds and van der Waals contacts as observed in the glucose complex, while the rigid thiohydantoin group is in a favourable electrostatic environment and makes additional polar contacts to the protein.
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(as it appears on PubMed at http://www.pubmed.gov), where 11741774 is the PubMed ID number.
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{{ABSTRACT_PUBMED_11741774}}
==About this Structure==
==About this Structure==
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[[Category: Inhibitor complex]]
[[Category: Inhibitor complex]]
[[Category: Transferase]]
[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 1 05:15:17 2008''

Revision as of 02:15, 1 July 2008

Image:1ggn.png

Template:STRUCTURE 1ggn

Structures of glycogen phosphorylase-inhibitor complexes and the implications for structure-based drug design

Template:ABSTRACT PUBMED 11741774

About this Structure

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

Reference

Kinetic and crystallographic studies of glucopyranosylidene spirothiohydantoin binding to glycogen phosphorylase B., Oikonomakos NG, Skamnaki VT, Osz E, Szilagyi L, Somsak L, Docsa T, Toth B, Gergely P, Bioorg Med Chem. 2002 Feb;10(2):261-8. PMID:11741774

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