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Fragment-based lead discovery strategies in antimicrobial drug discovery

DOI: 10.3390/antibiotics12020315 DOI Help

Authors: Monika I. Konaklieva (American University) , Balbina J. Plotkin (Midwestern University)
Co-authored by industrial partner: No

Type: Journal Paper
Journal: Antibiotics , VOL 12

State: Published (Approved)
Published: February 2023

Open Access Open Access

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 (KD ~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.

Journal Keywords: FBLD; antimicrobial; multidrug resistance; inhibitors of pathogenic bacterial enzymes; phenotypic screens; STD NMR

Diamond Keywords: Bacteria

Subject Areas: Medicine, Biology and Bio-materials

Diamond Offline Facilities: XChem
Instruments: NONE-No attached Diamond beamline

Added On: 08/02/2023 09:28


Discipline Tags:

Pathogens Antibiotic Resistance Health & Wellbeing Drug Discovery Life Sciences & Biotech

Technical Tags:

Diffraction Macromolecular Crystallography (MX) Fragment Screening