BioCentury
ARTICLE | Cover Story

Deep pockets

August 22, 2013 7:00 AM UTC

The B class of GPCRs is brimming with therapeutic targets, but thus far, development of small molecule drugs has been stymied. New studies reporting the first-ever crystal structures of members of the family could change that and open up new therapeutic real estate.1,2

GPCRs are versatile chemical sensors that coordinate cellular responses to a variety of extracellular stimuli and are the largest target class of FDA-approved drugs.3 Despite years of research and numerous approvals, predicting the relationship between ligands and GPCRs remains challenging because of a deficiency in molecular-level information about these interactions and the complexity of downstream biological effects...