Robert Lefkowitz

G Protein Coupled Receptors


Abstract

Seven transmembrane receptors (7TMRs), aka G protein coupled receptors (GPCRs) represent by far the largest, most versatile, and most ubiquitous of the several families of plasma membrane receptors. They regulate virtually all known physiological processes in humans, and are the commonest target of therapeutic drugs. As recently as 40-50 years ago, the very existence of cellular receptors for drugs and hormones was highly controversial, and there were no direct means of studying them. Today, the family of GPCRs is known to number approximately 1,000, and crystal structures have recently been solved for dozens of the members of the family and even of a receptor-G protein complex. I will briefly review how the field has evolved over the past 50 years emphasizing how basic research has reshaped the process of drug discovery.


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