Septerna

There are hundreds of G protein–coupled receptors (GPCRs) in the human genome, regulating just about every physiological system. While roughly a third of marketed drugs target a GPCR, many of the receptors have remained out of reach for drug hunters, in part because of challenges involved in studying them . After the heyday of GPCR-targeting drugs in the 1990s and early 2000s, few medicines targeting these proteins have been introduced. But new technologies may be poised to change that. A few years ago, chemistry Nobel laureate Robert J. Lefkowitz was working with scientists in his lab at Duke University in North Carolina to develop a new way to isolate enzymatically active GPCRs. Halfway around the world, at Monash University in Melbourne, Australia, the eminent pharmacology duo Patrick Sexton and Arthur Christopoulos was simultaneously developing techniques to modulate GPCR signaling using structure-based drug design. And in San Francisco, Jeffrey Finer, a