Fragment-Based Lead Discovery Strategies in Antimicrobial Drug Discovery.
Antibiotics (Basel, Switzerland)(2023)
摘要
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 ~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.
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关键词
FBLD,STD NMR,antimicrobial,inhibitors of pathogenic bacterial enzymes,multidrug resistance,phenotypic screens
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