Crystal structure of dopamine receptor D4 bound to the subtype selective ligand, L745870.

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ID: 77660
2019
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Abstract
Multiple subtypes of dopamine receptors within the GPCR superfamily regulate neurological processes through various downstream signaling pathways. A crucial question about the dopamine receptor family is what structural features determine the subtype-selectivity of potential drugs. Here, we report the 3.5-angstrom crystal structure of mouse dopamine receptor D4 (DRD4) complexed with a subtype-selective antagonist, L745870. Our structure reveals a secondary binding pocket extended from the orthosteric ligand-binding pocket to a DRD4-specific crevice located between transmembrane helices 2 and 3. Additional mutagenesis studies suggest that the antagonist L745870 prevents DRD4 activation by blocking the relative movement between transmembrane helices 2 and 3. These results expand our knowledge of the molecular basis for the physiological functions of DRD4 and assist new drug design.
Reference Key
zhou2019crystalelife Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Zhou, Ye;Cao, Can;He, Lingli;Wang, Xianping;Zhang, Xuejun Cai;
Journal eLife
Year 2019
DOI
10.7554/eLife.48822
URL
Keywords
gpcr mouse molecular biophysics structural biology ligand binding dimerization antagonist drd4

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