1a5x: Difference between revisions
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Revision as of 15:40, 30 October 2007
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ASV INTEGRASE CORE DOMAIN WITH HIV-1 INTEGRASE INHIBITOR Y3
OverviewOverview
The x-ray structures of an inhibitor complex of the catalytic core domain, of avian sarcoma virus integrase (ASV IN) were solved at 1.9- to 2.0-A, resolution at two pH values, with and without Mn2+ cations. This inhibitor, (Y-3), originally identified in a screen for inhibitors of the catalytic, activity of HIV type 1 integrase (HIV-1 IN), was found in the present, study to be active against ASV IN as well as HIV-1 IN. The Y-3 molecule is, located in close proximity to the enzyme active site, interacts with the, flexible loop, alters loop conformation, and affects the conformations of, active site residues. As crystallized, a Y-3 molecule stacks against its, symmetry-related mate. Preincubation of IN with metal cations does not, prevent inhibition, and Y-3 binding does not prevent binding ... [(full description)]
About this StructureAbout this Structure
1A5X is a [Single protein] structure of sequence from [Rous sarcoma virus] with Y3 as [ligand]. Active as [RNA-directed DNA polymerase], with EC number [2.7.7.49]. Structure known Active Site: ACT. Full crystallographic information is available from [OCA].
ReferenceReference
Structure of the catalytic domain of avian sarcoma virus integrase with a bound HIV-1 integrase-targeted inhibitor., Lubkowski J, Yang F, Alexandratos J, Wlodawer A, Zhao H, Burke TR Jr, Neamati N, Pommier Y, Merkel G, Skalka AM, Proc Natl Acad Sci U S A. 1998 Apr 28;95(9):4831-6. PMID:9560188
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