A novel substrate-based HIV-1 protease inhibitor drug resistance mechanism.

ABSTRACT:

Background

HIV protease inhibitor (PI) therapy results in the rapid selection of drug resistant viral variants harbouring one or two substitutions in the viral protease. To combat PI resistance development, two approaches have been developed. The first is to increase the level of PI in the plasma of the patient, and the second is to develop novel PI with high potency against the known PI-resistant HIV protease variants. Both approaches share the requirement for a considerable increase in the number of protease mutations to lead to clinical resistance, thereby increasing the genetic barrier. We investigated whether HIV could yet again find a way to become less susceptible to these novel inhibitors.

Methods and findings

We have performed in vitro selection experiments using a

SUBMITTER: Nijhuis M 

PROVIDER: S-EPMC1769415 | biostudies-literature | 2007 Jan

REPOSITORIES: biostudies-literature