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NEUROTRANSMITTER RECEPTORS

Structural insights

Nature Reviews Neuroscience volume 22, page 195 (2021)Cite this article

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Aberrant dopaminergic signalling has been implicated in various brain disorders and a need exists to further develop drugs that target dopamine receptors. Among these G protein-coupled receptors, D1 and D2 dopamine receptors (D1Rs and D2Rs) are the most widely found in the CNS. Although some structures for D2R have been reported, there has been a lack of structures reported for D1R, impeding structure-based drug design efforts. Now, two studies using cryoelectron microscopy provide structural insights in D1R and D2R signalling complexes. Xiao et al. report five structures for human D1R coupled to its G protein (Gs); in four of these structures, D1R is in complex with an agonist, whereas in the other, the receptor is in a complex with an allosteric modulator. Zhuang et al. also report three structures for human D1R-Gs in complex with agonists, and they describe a structure for agonist-bound human D2R coupled to its G protein, Gi. Collectively, the studies provide structural insights into D1R activation and allosteric regulation of this receptor, as well as ligand and G protein selectively for D1R and D2R.

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References

Original articles

  • Zhuang, Y. et al. Structural insights into the human D1 and D2 dopamine receptor signalling complexes. Cell 184, 931–942 (2021)

    Article  CAS  Google Scholar 

  • Xiao, P. et al. Ligand recognition and allosteric regulation of DRD1-Gs signalling complexes. Cell 184, 943–956 (2021)

    Article  CAS  Google Scholar 

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  1. Nature Reviews Neuroscience http://www.nature.com/nrn/

    Darran Yates

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  1. Darran Yates
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Correspondence to Darran Yates.

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Yates, D. Structural insights. Nat Rev Neurosci 22, 195 (2021). https://doi.org/10.1038/s41583-021-00453-9

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