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Vanilloid agonist-mediated activation of TRPV1 channels requires coordinated movement of the S1–S4 bundle rather than a quiescent state

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Science Bulletin 2022年第10期67卷 1062-1076,M0004页

作者： Meng-Yang Sun Xue Zhang Peng-Cheng Yu Di Liu Yang Yang Wen-Wen Cui Xiao-Na Yang Yun-Tao Lei Xing-Hua Li Wen-Hui Wang Peng Cao Heng-Shan Wang Michael X.Zhu Chang-Zhu Li Rui Wang Ying-Zhe Fan Ye Yu School of Life Sciences and Key Laboratory of Preclinical Study for New Drugs of Gansu Province School of Basic Medical SciencesLanzhou UniversityLanzhou 730000China State Key Laboratory of Utilization of Woody Oil Resource Hunan Academy of ForestryChangsha 410004China Department of Pharmacology and Chemical Biology Institute of Medical SciencesShanghai Jiao Tong University School of MedicineShanghai 200025China Department of Basic Medicine and Clinical Pharmacy China Pharmaceutical UniversityNanjing 210009China Putuo Hospital Shanghai University of Chinese Traditional MedicineShanghai 200062China College of Bioscience and Biotechnology Hunan Agricultural UniversityChangsha 410128China Hospital of Integrated Traditional Chinese and Western Medicine Nanjing University of Chinese MedicineNanjing 210023China State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources Collaborative Innovation Center for Guangxi Ethnic MedicineSchool of Chemistry and Pharmaceutical SciencesGuangxi Normal UniversityGuilin 541004China Department of Integrative Biology and Pharmacology McGovern Medical SchoolThe University of Texas Health Science Center at HoustonHoustonTX 77030USA

Transient receptor potential vanilloid 1(TRPV1)channel plays an important role in a wide range of physiological and pathological processes,and a comprehensive understanding of TRPV1 gating will create opportunities for therapeutic *** incredible advances in cryo-electron microscopy(cryo-EM)have yielded high-resolution structures of all TRPV subtypes(TRPV1-6)and all of them share highly conserved six transmembrane(TM)domains(S1-S6).As revealed by the open structures of TRPV1 in the presence of a bound vanilloid agonist(capsaicin or resiniferatoxin),TM helices S1 to S4 form a bundle that remains quiescent during channel activation,highlighting differences in the gating mechanism of TRPV1 and voltage-gated ion ***,however,we argue that the structural dynamics rather than quiescence of S1-S4 domains is necessary for capsaicin-mediated activation of *** fluorescent unnatural amino acid(flUAA)incorporation and voltage-clamp fluorometry(VCF)analysis,we directly observed allostery of the S1-S4 bundle upon capsaicin *** occupation of VCF-identified sites,single-channel recording,cell apoptosis analysis,and exploration of the role of PSFL828,a novel non-vanilloid agonist we identified,have collectively confirmed the essential role of this coordinated S1-S4 motility in capsaicin-mediated activation of *** study concludes that,in contrast to cryo-EM structural studies,vanilloid agonists are also required for S1-S4 movement during TRPV1 *** the gating process of vanilloid agonists and the discovery of new non-vanilloid agonists will allow the evaluation of new strategies aimed at the development of TRPV1 modulators.

关键词： Ligand-gated ion channels TRPV1 Allostery voltage-clamp fluorometry Vanilloid agonist

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Emerging approaches to probing ion channel structure and function

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Neuroscience Bulletin 2012年第4期28卷 351-374页

作者： Wei-Guang Li Tian-Le Xu Neuroscience Division Department of Biochemistry and Molecular Cell BiologyInstitute of Medical SciencesShanghaiJiao Tong University School of MedicineShanghai 200025China

Ion channels,as membrane proteins,are the sensors of the *** act as the first line of communication with the world beyond the plasma membrane and transduce changes in the external and internal environments into unique electrical signals to shape the responses of excitable *** of their importance in cellular communication,ion channels have been intensively studied at the structural and functional ***,we summarize the diverse approaches,including molecular and cellular,chemical,optical,biophysical,and computational,used to probe the structural and functional rearrangements that occur during channel activation（or sensitization）,inactivation（or desensitization）,and various forms of *** emerging insights into the structure and function of ion channels by multidisciplinary approaches allow the development of new pharmacotherapies as well as new tools useful in controlling cellular activity.

关键词： ion channel structure and function mutagenesis covalent modification voltage-clamp fluorometry computational chemistry

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