Fragment-Based Lead Discovery Strategies in Antimicrobial Drug Discovery.

ABSTRACT: Fragment-based lead discovery (FBLD) is a powerful application for developing ligands as modulators of disease targets. This approach strategy involves identification of interactions between low-molecular weight compounds (100-300 Da) and their putative targets, often with low affinity (K_D ~0.1-1 mM) interactions. The focus of this screening methodology is to optimize and streamline identification of fragments with higher ligand efficiency (LE) than typical high-throughput screening. The focus of this review is on the last half decade of fragment-based drug discovery strategies that have been used for antimicrobial drug discovery.

SUBMITTER: Konaklieva MI 

PROVIDER: S-EPMC9951956 | biostudies-literature | 2023 Feb

REPOSITORIES: biostudies-literature