학술논문
Hydroxyethylene isostere inhibitors of human immunodeficiency virus-1 protease: structure-activity analysis using enzyme kinetics, x-ray crystallography, and infected T-cell assays
Document Type
Academic Journal
Author
Source
Biochemistry. July 28, 1992, Vol. 31 Issue 29, p6646, 14 p.
Subject
Language
ISSN
0006-2960
Abstract
Peptide analogues containing hydroxyethylene dipeptide isosteres were synthesized and their inhibition of HIV-1 protease in two different infected cell systems was examined. The enzyme inhibition constants in the two sytems were determined and compared. Virological assays that assess their ability to inhibit both assembly of infectious virions and infection of uninfectedd T-cells were also performed. Inaddition, enzyme-kinetics and X-ray crystallography were used to analyze the structure-activity relationship of these inhibitors.