Research ArticleGPCR SIGNALING

CCR5 adopts three homodimeric conformations that control cell surface delivery

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Sci. Signal.  08 May 2018:
Vol. 11, Issue 529, eaal2869
DOI: 10.1126/scisignal.aal2869

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CCR5 delivery to the cell surface

The chemokine receptor CCR5 is a class A GPCR and co-receptor for HIV-1 infection. How class A GPCRs dimerize and how it affects their function are unclear. Jin et al. analyzed the structures of related receptors and identified CCR5 residues that mediated homodimerization. Cross-linking and energy transfer experiments and monitoring the release of receptors from the endoplasmic reticulum identified two dimeric CCR5 conformations that directed its delivery to the plasma membrane. A third CCR5 homodimer was stabilized by maraviroc, a clinically used inhibitor that binds to CCR5 and inhibits its interaction with HIV-1. These data increase our understanding of class A GPCR dimerization and provide insight into the mechanisms of inhibiting HIV-1 entry.