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4篇 您的检索式:作者名="Bryan L.Roth"
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1Mechanism of dopamine binding and allosteric modulation of the human D1 dopamine receptor显示文摘Dear Editor,Dopamine acts as an essential neurotransmitter whose signaling 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 dopaminergic pathways.Dysregulation of DRD1 signaling has been directly linked to Parkinson’s disease(PD),schizophrenia,and drug abuse.Youwen Zhuang Brian Krumm Huibing Zhang X.Edward Zhou Yue Wang Xi-Ping Huang Yongfeng Liu Xi Cheng Yi Jiang Hualiang Jiang Cheng Zhang Wei Yi Bryan L.Roth Yan Zhang H.Eric Xu 2021Cell Research2021,31,5:2
2五羟色胺2C受体结构揭示GPCR多重药理学特性的结构基础显示文摘文章简介有些药物往往需要作用于多个靶点,即多重药理学作用发挥其疗效。目前,针对多种血清素受体的药物,包括5-HT2C受体,对治疗肥胖、药物滥用和精神分裂症意义重大。彭瑶 John D.McCorvy Kasper Harpsoe Katherine Lansu Shuguang Yuan Petr Popov Lu Qu Mengchen Pu Tao Che Louise F.Nikolajsen Xi-Ping Huang Yiran Wu Ling Shen Walden E.Bjorn-Yoshimoto Kang Ding Daniel Wacker Gye Won Han Jianjun Cheng Vsevolod Katritch Anders A.Jensen Michael A.Hanson Suwen Zhao David E.Gloriam Bryan L.Roth Raymond C.Stevens 刘志杰 2019科学新闻2019,0,2:0
3Sensing unsaturated fatty acids:insights from GPR120 signaling显示文摘GPR120 is a receptor that plays a crucial role in mediating the beneficial effects of free fatty acids(FAs),particularlyω-3 FAs,on metabolic and inflammatory pathways,making it an important therapeutic target for metabolic diseases.Recently,Mao et al.report the cryo-EM structures of GPR120 in complex with anω-3 FA as well as other three endogenous FAs and a synthetic agonist,along with pharmacological investigations and molecular dynamics simulations,thereby providing comprehensive insights into the molecular recognition and biased signaling of GPR120 via various agonists.Shicheng Zhang Bryan L.Roth 2023Cell Research2023,33,9:0
4Structural genomics of the human dopamine receptor system显示文摘The dopaminergic system,including five dopamine receptors(D1R to D5R),plays essential roles in the central nervous system(CNS);and ligands that activate dopamine receptors have been used to treat many neuropsychiatric disorders,including Parkinson’s Disease(PD)and schizophrenia.Here,we report cryo-EM structures of all five subtypes of human dopamine receptors in complex with G protein and bound to the pan-agonist,rotigotine,which is used to treat PD and restless legs syndrome.The structures reveal the basis of rotigotine recognition in different dopamine receptors.Structural analysis together with functional assays illuminate determinants of ligand polypharmacology and selectivity.The structures also uncover the mechanisms of dopamine receptor activation,unique structural features among the five receptor subtypes,and the basis of G protein coupling specificity.Our work provides a comprehensive set of structural templates for the rational design of specific ligands to treat CNS diseases targeting the dopaminergic system.Peiyu Xu Sijie Huang Brian E.Krumm Youwen Zhuang Chunyou Mao Yumu Zhang Yue Wang Xi-Ping Huang Yong-Feng Liu Xinheng He Huadong Li Wanchao Yin Yi Jiang Yan Zhang Bryan L.Roth H.Eric Xu 2023Cell Research2023,33,8:0
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