EMDB/PDB/SASBDBから引用されている文献のデータベース

キーワード
構造解析手法	All X線回折 NMR 電子顕微鏡小角散乱中性子線回折線維回折粉末回折赤外分光 EPR FRET 理論モデルハイブリッド
著者・登録者
ジャーナル
IF	>30 >20 >10 >5 all

タイトル	Structural mechanism of the agonist binding on human TRPC3 channel.
ジャーナル・号・ページ	Nat Commun, Vol. 16, Issue 1, Page 9343, Year 2025
掲載日	2025年10月22日
著者	Yikun Chen / Jiahe Zang / Wenjun Guo / Jiaxuan Xu / Miao Wei / Li Quan / Min Zhu / Xiaole Zhao / Hailin Peng / Yakun Wan / Lei Chen /
PubMed 要旨	TRPC3/6/7 channels are cation channels that are directly activated by the second messenger diacylglycerol (DAG). These channels play crucial physiological roles and are implicated in various disease ...TRPC3/6/7 channels are cation channels that are directly activated by the second messenger diacylglycerol (DAG). These channels play crucial physiological roles and are implicated in various disease conditions; however, the binding mechanism of DAG to these channels remains incompletely understood. In this study, we present the structures of human TRPC3 in complex with DAG or synthetic activators, 4n and GSK1702934A. The structural analysis reveals that DAG binds at the L2 site, located near the pore on the extracellular side of TRPC3. Functional assays confirmed that the L2 site serves as the activating site for DAG. Notably, both 4n and GSK1702934A competitively bind to the same site, facilitating channel activation. Moreover, based on the pharmacophore identified from the DAG-bound structure, we found that monoacylglycerols (MAGs) are endogenous activators of TRPC3/6/7 channels, providing new insights into their regulatory mechanisms.
リンク	Nat Commun / PubMed:41125595 / PubMed Central
手法	EM (単粒子)
解像度	2.25 - 3.34 Å
構造データ	62268 9kdb EMDB-62268, PDB-9kdb: Structure of hTRPC3 in complex with Nb1-25 at 2.67 angstrom 手法: EM (単粒子) / 解像度: 2.67 Å 62269 9kdc EMDB-62269, PDB-9kdc: Structure of hTRPC3 in complex with Nb3-37 at 3.01 angstrom 手法: EM (単粒子) / 解像度: 3.01 Å 62270 9kdd EMDB-62270, PDB-9kdd: Structure of GSK1702934A-bound TRPC3 at 3.3 angstrom 手法: EM (単粒子) / 解像度: 2.7 Å 62271 9kde EMDB-62271, PDB-9kde: Structure of 4n-bound TRPC3 at 3.3 angstrom 手法: EM (単粒子) / 解像度: 3.34 Å 63868 9u5c EMDB-63868, PDB-9u5c: Structure of hTRPC3 in complex with Nb1-94 at 2.25 angstrom 手法: EM (単粒子) / 解像度: 2.25 Å
化合物	ChemComp-ZN: Unknown entry ChemComp-CA: Unknown entry / カルシウムジカチオン PDB-1l5i: 30-CONFORMER NMR ENSEMBLE OF THE N-TERMINAL, DNA-BINDING DOMAIN OF THE REPLICATION INITIATION PROTEIN FROM A GEMINIVIRUS (TOMATO YELLOW LEAF CURL VIRUS-SARDINIA) PDB-1l5p: Crystal Structure of Trichomonas vaginalis Ferredoxin PDB-1l5q: Human liver glycogen phosphorylase a complexed with caffeine, N-Acetyl-beta-D-glucopyranosylamine, and CP-403700 ChemComp-HOH: WATER
由来	homo sapiens (ヒト) camelus (哺乳類)
キーワード	METAL TRANSPORT / TRPC3 / DAG / Nb1-25 / nanobody / Nb3-37 / MOG / 4n / Nb1-94