GPCR Signaling: Understanding the Pathway to Successful Drug Discovery

摘要: Modulators of G protein-coupled receptors (GPCRs) form a key area for the pharmaceutical industry, representing approximately 27% all Food and Drug Administration (FDA)-approved drugs. Consequently, there are wide variety in vitro plate-based screening technologies that enable measurement compound affinity, potency, efficacy almost every type GPCR. However, to maximize success it is prudent ensure (i) most suitable assay formats identified, (ii) they configured optimally detect desired activity, (iii) basis predicting clinical effects. To achieve this, an understanding pathways mechanisms receptor activation relevant disease mechanism, as well benefits and/or limitations specific techniques, key.