Fragment-Based Lead Discovery Strategies in Antimicrobial Drug Discovery

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 similar to 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.

Automated summary

Fragment-based lead discovery (FBLD) is an effective approach used to develop ligands as modulators of disease targets. This method focuses on identifying interactions between low-molecular weight compounds and their potential targets, with low affinity interactions. The review focuses on the past five years of fragment-based drug discovery strategies for antimicrobial drug development.