2uy0
From Proteopedia
TWO-CARBON-ELONGATED HIV-1 PROTEASE INHIBITORS WITH A TERTIARY-ALCOHOL-CONTAINING TRANSITION-STATE MIMIC
Overview
A new generation of HIV-1 protease inhibitors encompassing a tertiary-alcohol-based transition-state mimic has been developed. By elongation of the core structure of recently reported inhibitors with two carbon atoms and by varying the P1' group of the compounds, efficient inhibitors were obtained with Ki down to 2.3 nM and EC50 down to 0.17 microM. Two inhibitor-enzyme X-ray structures are reported.
About this Structure
2UY0 is a Single protein structure of sequence from Human immunodeficiency virus 1. Full crystallographic information is available from OCA.
Reference
Two-carbon-elongated HIV-1 protease inhibitors with a tertiary-alcohol-containing transition-state mimic., Wu X, Ohrngren P, Ekegren JK, Unge J, Unge T, Wallberg H, Samuelsson B, Hallberg A, Larhed M, J Med Chem. 2008 Feb 28;51(4):1053-7. Epub 2008 Jan 24. PMID:18215014 Page seeded by OCA on Thu May 22 21:38:09 2008
