This old version of Proteopedia is provided for student assignments while the new version is undergoing repairs. Content and edits done in this old version of Proteopedia after March 1, 2026 will eventually be lost when it is retired in about June of 2026.
Apply for new accounts at the new Proteopedia. Your logins will work in both the old and new versions.
1a5v
From Proteopedia
|
ASV INTEGRASE CORE DOMAIN WITH HIV-1 INTEGRASE INHIBITOR Y3 AND MN CATION
Overview
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 Structure
1A5V is a [Single protein] structure of sequence from [Rous sarcoma virus] with MN and Y3 as [ligands]. Active as [[1]], with EC number [2.7.7.49]. Full crystallographic information is available from [OCA].
Reference
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
Page seeded by OCA on Mon Oct 29 20:27:11 2007
