High-throughput lead finding and optimisation for GPCR targets.
Driven by past successes and the detailed knowledge of signalling cascades and physiological processes, G-protein-coupled receptors are taking a prominent place in the portfolios of many pharmaceutical companies. To successfully address this target class, scientists need not only a good understanding of the specific receptor under investigation, but also the right tools from assay technology, reagent production to a hit-to-lead process that acknowledges the importance of parameters beyond potency and embraces the gain in knowledge of the last decade. This manuscripts attempts to summarise some of the changes and progress made across the pharmaceutical industry to design an efficient and effective strategy for finding and optimising small molecules modulating the activity of GPCRs.
Sewing
A
A
Primary Pharmacology Group, Pfizer PDGRD, IPC 580, Ramsgate Road, CT13 9NJ Sandwich, UK. Andreas.Sewing@pfizer.com
Cawkill
D
D
D000818:Animals; D001665:Binding Sites; D020650:Combinatorial Chemistry Techniques; D015195:Drug Design; D006801:Humans; D008024:Ligands; D008958:Models, Molecular; D011487:Protein Conformation; D021281:Quantitative Structure-Activity Relationship; D043562:Receptors, G-Protein-Coupled / Q000737:chemistry* / Q000378:metabolism
D008024:Ligands; D043562:Receptors, G-Protein-Coupled