Tanzania
Research Article
Inhibition of the Replication of Clinical Drug-Resistant HIV-1 Strains by Small Molecule Integrase Inhibitors M522 and M532
Author(s): Ibrahim S Abd-Elazem and Ru Chih C HuangIbrahim S Abd-Elazem and Ru Chih C Huang
Objective: Integrase (IN) is an enzyme essential for HIV-1 replication that has been a target of antiretroviral drug therapy. Since emerging HIV-1 variants have frequently become clinically resistant to antiretroviral agents, it is necessary to develop alternative IN inhibitors. Methods: We tested IN inhibitors, M522 and M532, against clinically resistant HIV-1 strains to antiretroviral drugs (AZT, non-nucleoside reverse transcriptase inhibitors, IN drug raltegravir, protease inhibitors); wild-type and clinical isolate from HIV-infected patients. We performed disintegration studies to show the interaction of M522 and M532 with the catalytic core domain of HIV-1 IN and time-of-drug-addition experiments to determine the inhibition step of viral replication. We tested selection of HIV-1 with M522 and M532 to examine the emergence of new drug resistant virus. CD4+ cell count was calculate.. Read More»
DOI:
10.4172/2155-6113.1000378
Journal of AIDS & Clinical Research received 5061 citations as per Google Scholar report