Journal
ANTIBIOTICS-BASEL
Volume 12, Issue 2, Pages -Publisher
MDPI
DOI: 10.3390/antibiotics12020315
Keywords
FBLD; antimicrobial; multidrug resistance; inhibitors of pathogenic bacterial enzymes; phenotypic screens; STD NMR
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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.
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.
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