Interdependence of Inhibitor Recognition in HIV-1 Protease

Interdependence of Inhibitor Recognition in HIV-1 Protease

Molecular recognition is a highly interdependent process. Subsite couplings within the active site of proteases are most often revealed through conditional amino acid preferences in substrate recognition. However, the potential effect of these couplings on inhibition and thus inhibitor design is largely unexplored. The present study examines the interdependency of subsites in HIV-1 protease usi...

Effect of Biomolecular Conformation on Docking Simulation: A Case Study on a Potent HIV-1 Protease Inhibitor

Human immunodeficiency virus infection / acquired immunodeficiency syndrome (HIV/AIDS) is a disease pertained to the human immune system. Given its crucial role in viral replication, HIV-1 protease (HIV-1 PR) is a prime therapeutic target in AIDS therapy. In this regard, the dynamic aspects of ligand-enzyme interactions may indicate an important role of conformational variability in HIV-1 PR in...

HIV-1 protease mutations and protease inhibitor cross-resistance.

The effects of many protease inhibitor (PI)-selected mutations on the susceptibility to individual PIs are unknown. We analyzed in vitro susceptibility test results on 2,725 HIV-1 protease isolates. More than 2,400 isolates had been tested for susceptibility to fosamprenavir, indinavir, nelfinavir, and saquinavir; 2,130 isolates had been tested for susceptibility to lopinavir; 1,644 isolates ha...

Changes in Glycosylation of Alpha-1-Protease Inhibitor in Inflammation (Rheumatoid Arthritis and Crohn\'s Disease)

Alpha-1-proteinase inhibitor (API) is one of the acute phase proteins. Following an inflammatory stimuli the concentration of API increased up to four folds. Accompanying these quantitative changes, there is qualitative alterations in the structure of carbohydrate moiety (glycosylation). To determine the alterations in the glycosylation of API in inflammation, API was isolated from the sera of...

HIV Protease Inhibitor : Past