Drug Design, Development and Therapy

Exploring Fragment-Based Approaches in Drug Discovery

With the emergence of fragment-based drug discovery (FBDD), the field of drug discovery has undergone significant changes. Unlike traditional high-throughput screening techniques, FBDD is based on identifying low molecular weight compounds (fragments) with a low affinity to the biological target. These initial fragment hits are then developed into drug-like molecules through a range of techniques, including fragment merging, growing, and linking, to produce a lead with a higher affinity. FBDD has the capacity to streamline the drug discovery process by initiating a bottom-up process of combining fragments with high ligand efficiencies. Structural insights from X-ray crystallography have fostered hopes that fragments with strong local interaction networks could be extended to target a wider binding site. To help raise the profile of this important area of research, Drug Design, Development and Therapy is publishing a timely Article Collection on fragment-based drug discovery.