
Fragment-based screening is now recognised as a powerful method for the design of novel potent molecules against therapeutic protein targets including challenging targets. Here, the main concepts used in the fragment-based drug design approach are reviewed, together with the reasons for its success. Methods and strategies used to identify, validate and select fragments are discussed. Future challenges and developments that are expected for the next decade are presented.
LIGAND SPECIFICITY, [CHIM.ANAL] Chemical Sciences/Analytical chemistry, Binding Sites, IDENTIFICATION, Molecular Structure, Drug Evaluation, Preclinical, SITE, Ligands, NMR, PROTEIN DRUGGABILITY, Molecular Weight, Structure-Activity Relationship, LEAD DISCOVERY, Drug Design, Animals, Humans, Molecular Targeted Therapy, Nuclear Magnetic Resonance, Biomolecular, Forecasting, Protein Binding
LIGAND SPECIFICITY, [CHIM.ANAL] Chemical Sciences/Analytical chemistry, Binding Sites, IDENTIFICATION, Molecular Structure, Drug Evaluation, Preclinical, SITE, Ligands, NMR, PROTEIN DRUGGABILITY, Molecular Weight, Structure-Activity Relationship, LEAD DISCOVERY, Drug Design, Animals, Humans, Molecular Targeted Therapy, Nuclear Magnetic Resonance, Biomolecular, Forecasting, Protein Binding
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