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Structural insights into the agonist activity of the nonpeptide modulator JR14a on C3aR.

作者信息

Luo Ping, Xin Wenwen, Guo Shimeng, Li Xin, Zhang Qing, Xu Youwei, He Xinheng, Wang Yue, Fan Wenjia, Yuan Qingning, Wu Kai, Hu Wen, Zhuang Youwen, Xu H Eric, Xie Xin

机构信息

State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China.

University of Chinese Academy of Sciences, Beijing, China.

出版信息

Cell Discov. 2025 Jan 10;11(1):7. doi: 10.1038/s41421-024-00765-x.

DOI:10.1038/s41421-024-00765-x
PMID:39788969
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11718183/
Abstract
摘要
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ff59/11718183/f4136b144b34/41421_2024_765_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ff59/11718183/f4136b144b34/41421_2024_765_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ff59/11718183/f4136b144b34/41421_2024_765_Fig1_HTML.jpg

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本文引用的文献

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Functional profiling of the G protein-coupled receptor C3aR1 reveals ligand-mediated biased agonism.G 蛋白偶联受体 C3aR1 的功能分析揭示了配体介导的偏激动效应。
J Biol Chem. 2024 Jan;300(1):105549. doi: 10.1016/j.jbc.2023.105549. Epub 2023 Dec 10.
2
Molecular basis of anaphylatoxin binding, activation, and signaling bias at complement receptors.补体受体上过敏毒素结合、激活和信号转导偏倚的分子基础。
Cell. 2023 Oct 26;186(22):4956-4973.e21. doi: 10.1016/j.cell.2023.09.020. Epub 2023 Oct 17.
3
A method for structure determination of GPCRs in various states.
一种用于确定各种状态下 G 蛋白偶联受体结构的方法。
Nat Chem Biol. 2024 Jan;20(1):74-82. doi: 10.1038/s41589-023-01389-0. Epub 2023 Aug 14.
4
Revealing the signaling of complement receptors C3aR and C5aR1 by anaphylatoxins.揭示过敏毒素 C3aR 和 C5aR1 的信号转导。
Nat Chem Biol. 2023 Nov;19(11):1351-1360. doi: 10.1038/s41589-023-01339-w. Epub 2023 May 11.
5
Complement Receptors and Their Role in Leukocyte Recruitment and Phagocytosis.补体受体及其在白细胞募集和吞噬作用中的作用。
Front Cell Dev Biol. 2021 Feb 11;9:624025. doi: 10.3389/fcell.2021.624025. eCollection 2021.
6
Complement C3a receptor-mediated vascular dysfunction: a complex interplay between aging and neurodegeneration.补体 C3a 受体介导的血管功能障碍：衰老和神经退行性变之间的复杂相互作用。
J Clin Invest. 2021 Jan 4;131(1). doi: 10.1172/JCI144348.
7
Potent Thiophene Antagonists of Human Complement C3a Receptor with Anti-Inflammatory Activity.强效噻吩类人补体 C3a 受体拮抗剂，具有抗炎活性。
J Med Chem. 2020 Jan 23;63(2):529-541. doi: 10.1021/acs.jmedchem.9b00927. Epub 2020 Jan 7.
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Complement System Part I - Molecular Mechanisms of Activation and Regulation.补体系统 第一部分——激活与调节的分子机制
Front Immunol. 2015 Jun 2;6:262. doi: 10.3389/fimmu.2015.00262. eCollection 2015.
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Complement System Part II: Role in Immunity.补体系统第二部分：在免疫中的作用。
Front Immunol. 2015 May 26;6:257. doi: 10.3389/fimmu.2015.00257. eCollection 2015.
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Potent heterocyclic ligands for human complement c3a receptor.强效杂环配体用于人补体 C3a 受体。
J Med Chem. 2014 Oct 23;57(20):8459-70. doi: 10.1021/jm500956p. Epub 2014 Oct 8.