Targeting HIV-1 Reverse Transcriptase Using a Fragment-Based Approach.

ABSTRACT: Human immunodeficiency virus type I (HIV-1) is a retrovirus that infects cells of the host's immune system leading to acquired immunodeficiency syndrome and potentially death. Although treatments are available to prevent its progression, HIV-1 remains a major burden on health resources worldwide. Continued emergence of drug-resistance mutations drives the need for novel drugs that can inhibit HIV-1 replication through new pathways. The viral protein reverse transcriptase (RT) plays a fundamental role in the HIV-1 replication cycle, and multiple approved medications target this enzyme. In this study, fragment-based drug discovery was used to optimize a previously identified hit fragment (compound B-1), which bound RT at a novel site. Three series of compounds were synthesized and eva

SUBMITTER: Mansouri M 

PROVIDER: S-EPMC10095864 | biostudies-literature | 2023 Mar

REPOSITORIES: biostudies-literature