Cryo-EM Structures of Class B GPCR Reveal the Activation Mechanism.

Caught in the act: Two-domain G-protein-coupled receptors of the class B family mediate peptide hormone signaling and play a pivotal role in diseases such as diabetes and obesity. Drug discovery for these GPCRs has been difficult, especially when agonists are needed. Now, the first structures of full-length active class B GPCRs have been solved, which illuminates the activation mechanism and could accelerate structure-based drug discovery for class B GPCRs.