Fragment-based approaches to enzyme inhibition.
Fragment-based approaches have provided a new paradigm for small-molecule drug discovery. The methodology is complementary to high-throughput screening approaches, starting from fragments of low molecular complexity and high ligand efficiency, and building up to more potent inhibitors. The approach, which depends heavily on a number of biophysical techniques, is now being taken up by more groups in both industry and academia. This article describes key aspects of the process and highlights recent developments and applications.
Ciulli
Alessio
A
University Chemical Laboratory, Lensfield Road, Cambridge CB2 1EW, United Kingdom. ca26@cam.ac.uk
Abell
Chris
C
D020650:Combinatorial Chemistry Techniques; D018360:Crystallography, X-Ray; D015195:Drug Design; D004345:Drug Industry / Q000379:methods; D004791:Enzyme Inhibitors / Q000737:chemistry*; D008024:Ligands; D015394:Molecular Structure; D013678:Technology, Pharmaceutical / Q000379:methods
D004791:Enzyme Inhibitors; D008024:Ligands