1sdv

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{{STRUCTURE_1sdv| PDB=1sdv | SCENE= }}
{{STRUCTURE_1sdv| PDB=1sdv | SCENE= }}
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'''Crystal structures of HIV protease V82A and L90M mutants reveal changes in indinavir binding site.'''
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===Crystal structures of HIV protease V82A and L90M mutants reveal changes in indinavir binding site.===
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==Overview==
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The crystal structures of the wild-type HIV-1 protease (PR) and the two resistant variants, PR(V82A) and PR(L90M), have been determined in complex with the antiviral drug, indinavir, to gain insight into the molecular basis of drug resistance. V82A and L90M correspond to an active site mutation and nonactive site mutation, respectively. The inhibition (K(i)) of PR(V82A) and PR(L90M) was 3.3- and 0.16-fold, respectively, relative to the value for PR. They showed only a modest decrease, of 10-15%, in their k(cat)/K(m) values relative to PR. The crystal structures were refined to resolutions of 1.25-1.4 A to reveal critical features associated with inhibitor resistance. PR(V82A) showed local changes in residues 81-82 at the site of the mutation, while PR(L90M) showed local changes near Met90 and an additional interaction with indinavir. These structural differences concur with the kinetic data.
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{{ABSTRACT_PUBMED_15066177}}
==About this Structure==
==About this Structure==
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[[Category: Drug resistance]]
[[Category: Drug resistance]]
[[Category: Hiv-1 protease]]
[[Category: Hiv-1 protease]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 08:35:23 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 12:41:48 2008''

Revision as of 09:41, 28 July 2008

Image:1sdv.png

Template:STRUCTURE 1sdv

Crystal structures of HIV protease V82A and L90M mutants reveal changes in indinavir binding site.

Template:ABSTRACT PUBMED 15066177

About this Structure

1SDV is a Single protein structure of sequence from Human immunodeficiency virus 1. Full crystallographic information is available from OCA.

Reference

Crystal structures of HIV protease V82A and L90M mutants reveal changes in the indinavir-binding site., Mahalingam B, Wang YF, Boross PI, Tozser J, Louis JM, Harrison RW, Weber IT, Eur J Biochem. 2004 Apr;271(8):1516-24. PMID:15066177

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