2geb

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{{STRUCTURE_2geb| PDB=2geb | SCENE= }}
{{STRUCTURE_2geb| PDB=2geb | SCENE= }}
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'''Crystal structure of the Thermoanaerobacter tengcongensis hypoxanthine-guanine phosphoribosyltransferase L160I mutant: insights into the inhibitor design'''
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===Crystal structure of the Thermoanaerobacter tengcongensis hypoxanthine-guanine phosphoribosyltransferase L160I mutant: insights into the inhibitor design===
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==Overview==
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Hypoxanthine-guanine phosphoribosyltransferase (HGPRT) is a potential target for structure-based inhibitor design for the treatment of parasitic diseases. We created point mutants of Thermoanaerobacter tengcongensis HGPRT and tested their activities to identify side chains that were important for function. Mutating residues Leu160 and Lys133 substantially diminished the activity of HGPRT, confirming their importance in catalysis. All 11 HGPRT mutants were subject to crystallization screening. The crystal structure of one mutant, L160I, was determined at 1.7 A resolution. Surprisingly, the active site is occupied by a peptide from the N-terminus of a neighboring tetramer. These crystal contacts suggest an alternate strategy for structure-based inhibitor design.
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(as it appears on PubMed at http://www.pubmed.gov), where 17662107 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17662107}}
==About this Structure==
==About this Structure==
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[[Category: Selectivity]]
[[Category: Selectivity]]
[[Category: Transferase]]
[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 05:00:21 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 08:23:32 2008''

Revision as of 05:23, 28 July 2008

Image:2geb.png

Template:STRUCTURE 2geb

Crystal structure of the Thermoanaerobacter tengcongensis hypoxanthine-guanine phosphoribosyltransferase L160I mutant: insights into the inhibitor design

Template:ABSTRACT PUBMED 17662107

About this Structure

2GEB is a Single protein structure of sequence from Thermoanaerobacter tengcongensis. Full crystallographic information is available from OCA.

Reference

Crystal structure of Thermoanaerobacter tengcongensis hypoxanthine-guanine phosphoribosyl transferase L160I mutant--insights into inhibitor design., Chen Q, You D, Liang Y, Su X, Gu X, Luo M, Zheng X, FEBS J. 2007 Sep;274(17):4408-15. Epub 2007 Jul 27. PMID:17662107

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