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Structural basis for pore blockade of human voltage-gated calcium channel Ca1.3 by motion sickness drug cinnarizine.

作者信息

Yao Xia, Gao Shuai, Yan Nieng

机构信息

Department of Molecular Biology, Princeton University, Princeton, NJ, USA.

出版信息

Cell Res. 2022 Oct;32(10):946-948. doi: 10.1038/s41422-022-00663-5. Epub 2022 Apr 27.

DOI:10.1038/s41422-022-00663-5
PMID:35477996
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9525318/
Abstract
摘要
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b449/9525318/40117d515fde/41422_2022_663_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b449/9525318/40117d515fde/41422_2022_663_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b449/9525318/40117d515fde/41422_2022_663_Fig1_HTML.jpg

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本文引用的文献

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Closed-state inactivation and pore-blocker modulation mechanisms of human Ca2.2.人类 Ca2.2 通道的失活关闭状态和孔阻塞调节剂作用机制。
Cell Rep. 2021 Nov 2;37(5):109931. doi: 10.1016/j.celrep.2021.109931.
2
Structure of human Ca2.2 channel blocked by the painkiller ziconotide.人类钙通道 2.2 型被痛觉阻断剂 ziconotide 阻断的结构。
Nature. 2021 Aug;596(7870):143-147. doi: 10.1038/s41586-021-03699-6. Epub 2021 Jul 7.
3
Structural Basis of the Modulation of the Voltage-Gated Calcium Ion Channel Ca 1.1 by Dihydropyridine Compounds*.
Proc Natl Acad Sci U S A. 2025 Jun 10;122(23):e2424387122. doi: 10.1073/pnas.2424387122. Epub 2025 Jun 3.
4
Deciphering Ca permeation and valence selectivity in Ca1: Molecular dynamics simulations reveal the three-ion knock-on mechanism.解析Ca1中的钙渗透和价态选择性:分子动力学模拟揭示三离子撞击机制。
Proc Natl Acad Sci U S A. 2025 Jun 3;122(22):e2424694122. doi: 10.1073/pnas.2424694122. Epub 2025 May 29.
5
Calcium channels as pharmacological targets for cancer therapy.钙通道作为癌症治疗的药理学靶点。
Clin Exp Med. 2025 Mar 25;25(1):94. doi: 10.1007/s10238-025-01632-z.
6
Electrosome assembly: Structural insights from high voltage-activated calcium channel (CaV)-chaperone interactions.电小体组装:来自高电压激活钙通道(CaV)-伴侣蛋白相互作用的结构见解。
Biochem Soc Trans. 2025 Feb 6;53(1):BST20240422. doi: 10.1042/BST20240422.
7
Autism-Linked Mutations in αδ-1 and αδ-3 Reduce Protein Membrane Expression but Affect Neither Calcium Channels nor Trans-Synaptic Signaling.αδ-1和αδ-3中与自闭症相关的突变会降低蛋白质膜表达,但既不影响钙通道也不影响跨突触信号传导。
Pharmaceuticals (Basel). 2024 Nov 28;17(12):1608. doi: 10.3390/ph17121608.
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Structural biology and molecular pharmacology of voltage-gated ion channels.电压门控离子通道的结构生物学与分子药理学
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A Single Amino Acid Determines the Selectivity and Efficacy of Selective Negative Allosteric Modulators of Ca1.3 L-Type Calcium Channels.单一氨基酸决定了 Ca1.3 L 型钙通道选择性负变构调节剂的选择性和效力。
ACS Chem Biol. 2020 Sep 18;15(9):2539-2550. doi: 10.1021/acschembio.0c00577. Epub 2020 Sep 3.
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Molecular Basis for Ligand Modulation of a Mammalian Voltage-Gated Ca Channel.哺乳动物电压门控钙通道配体调节的分子基础。
Cell. 2019 May 30;177(6):1495-1506.e12. doi: 10.1016/j.cell.2019.04.043.
6
The Physiology, Pathology, and Pharmacology of Voltage-Gated Calcium Channels and Their Future Therapeutic Potential.电压门控钙通道的生理学、病理学和药理学及其未来的治疗潜力。
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Pharmacology of L-type Calcium Channels: Novel Drugs for Old Targets?L型钙通道的药理学:针对旧靶点的新型药物?
Curr Mol Pharmacol. 2015;8(2):110-22. doi: 10.2174/1874467208666150507105845.
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Modest CaV1.342-selective inhibition by compound 8 is β-subunit dependent.化合物8对CaV1.3 42亚基的适度抑制作用依赖于β亚基。
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Pyrimidine-2,4,6-triones are a new class of voltage-gated L-type Ca2+ channel activators.嘧啶-2,4,6-三酮是一类新型的电压门控L型钙离子通道激活剂。
Nat Commun. 2014 Jun 19;5:3897. doi: 10.1038/ncomms4897.
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CaV1.3-selective L-type calcium channel antagonists as potential new therapeutics for Parkinson's disease. Cav1.3 选择性 L 型钙通道拮抗剂有望成为帕金森病的新型治疗药物。
Nat Commun. 2012;3:1146. doi: 10.1038/ncomms2149.