G protein–coupled receptors

G protein-coupled receptors (GPCRs) are membrane proteins that are involved in a broad range of biological processes, and a large number of clinically used drugs elicit their biological effect(s) via a GPCR. Structural information about GPCRs was very limited until 2007, and papers describing new GPCR structures and previously unseen conformational states have dramatically increased in the past few years. In this online special, we present a selection of recently published Nature papers that involve the structures of various GPCRs. Understanding the conformational changes that occur in these proteins when a ligand binds to and activates the receptor should facilitate the development of potential drugs with fewer side effects and more favorable pharmacological properties.

Credit: Kobilka et al.

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