Fragment-Based Drug Discovery: Concepts & Technologies

This lecture covers the concepts and technologies related to fragment-based drug discovery (FBDD). It discusses the evolution of FBDD, the 'rule of three' in drug discovery, hit identification, and lead optimization. Various screening methods, such as absorbance, fluorescence, and bioluminescence, are explored. The lecture also delves into the application of FBDD in both druggable and less druggable targets, showcasing examples like Pexidartinib and Navitoclax. Additionally, it addresses the challenges and strategies in targeting traditionally undruggable sites. By the end, students will gain insights into the advantages of FBDD over conventional high-throughput screening methods and the potential of FBDD in accessing non-classical drug targets.