1sdt: Difference between revisions

Revision as of 11:33, 28 July 2008

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File:1sdt.png

Template:STRUCTURE 1sdt

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

Template:ABSTRACT PUBMED 15066177

About this StructureAbout this Structure

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

ReferenceReference

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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Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)

OCA

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-'''Crystal structures of HIV protease V82A and L90M mutants reveal changes in indinavir binding site.'''
+===Crystal structures of HIV protease V82A and L90M mutants reveal changes in indinavir binding site.===
-==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.
+The line below this paragraph, {{ABSTRACT_PUBMED_15066177}}, adds the Publication Abstract to the page
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 [[Category: Drug resistance]]
 [[Category: Hiv-1]]
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