Mechanism of dopamine binding and allosteric modulation of the human D1 dopamine receptor
Dear Editor,
Dopamine acts as an essential neurotransmitter whose signal-ing is conducted through five G protein-coupled receptors(GPCRs),dopamine D1 to D5 receptors (DRD1-DRD5).1 The D1-like receptors,comprising DRD1 and DRD5,primarily couple to the Gs family of G proteins to activate adenylyl cyclase and induce cAMP production.DRD1 is the most abundantly expressed dopamine receptor in the CNS.1 It is the central receptor mediating excitatory dopamine signaling in multiple dopaminer-gic pathways.Dysregulation of DRD1 signaling has been directly linked to Parkinson's disease (PD),schizophrenia,and drug abuse.1,2 Due to its fundamental functions in human diseases,DRD1 has long been the subject of intensive drug development efforts toward the treatment of neuropsychiatric diseases.3 A majority of DRD1 agonists,including the SKF compounds,targets the orthosteric pocket of DRD1,but none has passed clinical trials for neuropsychiatric symptoms to date.3
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2021-06-21（万方平台首次上网日期，不代表论文的发表时间）
共4页
593-596
