2geb

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[[Image:2geb.jpg|left|200px]]
[[Image:2geb.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2geb |SIZE=350|CAPTION= <scene name='initialview01'>2geb</scene>, resolution 1.70&Aring;
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The line below this paragraph, containing "STRUCTURE_2geb", 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=CA:CALCIUM+ION'>CA</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/Hypoxanthine_phosphoribosyltransferase Hypoxanthine phosphoribosyltransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.4.2.8 2.4.2.8] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= HGPRT, Hpt ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=119072 Thermoanaerobacter tengcongensis])
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|DOMAIN=
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{{STRUCTURE_2geb| PDB=2geb | SCENE= }}
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|RELATEDENTRY=[[1r3u|1R3U]], [[1yfz|1YFZ]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2geb FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2geb OCA], [http://www.ebi.ac.uk/pdbsum/2geb PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2geb RCSB]</span>
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'''Crystal structure of the Thermoanaerobacter tengcongensis hypoxanthine-guanine phosphoribosyltransferase L160I mutant: insights into the inhibitor design'''
'''Crystal structure of the Thermoanaerobacter tengcongensis hypoxanthine-guanine phosphoribosyltransferase L160I mutant: insights into the inhibitor design'''
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[[Category: Chen, Q.]]
[[Category: Chen, Q.]]
[[Category: Luo, M.]]
[[Category: Luo, M.]]
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[[Category: hgprt]]
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[[Category: Hgprt]]
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[[Category: inhibitor design]]
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[[Category: Inhibitor design]]
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[[Category: mutant]]
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[[Category: Mutant]]
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[[Category: selectivity]]
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[[Category: Selectivity]]
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[[Category: transferase]]
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[[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 Mar 31 03:15:29 2008''
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Revision as of 02:00, 4 May 2008

Image:2geb.jpg

Template:STRUCTURE 2geb

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


Overview

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.

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 Page seeded by OCA on Sun May 4 05:00:21 2008

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