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	Molecular basis of neurosteroid and anticonvulsant regulation of TRPM3.
ジャーナル・号・ページ	Nat Struct Mol Biol, Vol. 32, Issue 5, Page 828-840, Year 2025
掲載日	2025年1月14日
著者	Ying Yin / Cheon-Gyu Park / Shasha Feng / Ziqiang Guan / Hyuk-Joon Lee / Feng Zhang / Kedar Sharma / Mario J Borgnia / Wonpil Im / Seok-Yong Lee /
PubMed 要旨	Transient receptor potential channel subfamily M member 3 (TRPM3) is a Ca-permeable cation channel activated by the neurosteroid pregnenolone sulfate (PregS) or heat, serving as a nociceptor in the ...Transient receptor potential channel subfamily M member 3 (TRPM3) is a Ca-permeable cation channel activated by the neurosteroid pregnenolone sulfate (PregS) or heat, serving as a nociceptor in the peripheral sensory system. Recent discoveries of autosomal dominant neurodevelopmental disorders caused by gain-of-function mutations in TRPM3 highlight its role in the central nervous system. Notably, the TRPM3 inhibitor primidone, an anticonvulsant, has proven effective in treating patients with TRPM3-linked neurological disorders and in mouse models of thermal nociception. However, our understanding of neurosteroids, inhibitors and disease mutations on TRPM3 is limited. Here we present cryogenic electron microscopy structures of the mouse TRPM3 in complex with cholesteryl hemisuccinate, primidone and PregS with the synthetic agonist CIM 0216. Our studies identify the binding sites for the neurosteroid, synthetic agonist and inhibitor and offer insights into their effects and disease mutations on TRPM3 gating, aiding future drug development.
リンク	Nat Struct Mol Biol / PubMed:39809942 / PubMed Central
手法	EM (単粒子)
解像度	3.13 - 3.82 Å
構造データ	44100 9b28 EMDB-44100, PDB-9b28: Cryo-EM structure of the mouse TRPM3 alpha 2 channel in complex with primidone 手法: EM (単粒子) / 解像度: 3.24 Å 44101 9b29 EMDB-44101, PDB-9b29: Cryo-EM structure of the mouse TRPM3 alpha 2 channel in complex with cholesteryl hemisuccinate 手法: EM (単粒子) / 解像度: 3.13 Å 44102 9b2a EMDB-44102, PDB-9b2a: Cryo-EM structure of the mouse TRPM3 alpha 2 channel in complex with the neurosteroid pregnenolone sulfate and the synthetic agonist CIM 0216 手法: EM (単粒子) / 解像度: 3.82 Å
化合物	ChemComp-Y01: CHOLESTEROL HEMISUCCINATE ChemComp-6OU: [(2~{R})-1-[2-azanylethoxy(oxidanyl)phosphoryl]oxy-3-hexadecanoyloxy-propan-2-yl] (~{Z})-octadec-9-enoate / リン脂質YM PDB-1aia: STRUCTURAL BASIS FOR THE CATALYTIC ACTIVITY OF ASPARTATE AMINOTRANSFERASE K258H LACKING THE PYRIDOXAL-5'-PHOSPHATE BINDING LYSINE RESIDUE ChemComp-LBN: 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine / リン脂質YM ChemComp-PX2: 1,2-DILAUROYL-SN-GLYCERO-3-PHOSPHATE PDB-1aib: STRUCTURAL BASIS FOR THE CATALYTIC ACTIVITY OF ASPARTATE AMINOTRANSFERASE K258H LACKING THE PYRIDOXAL-5'-PHOSPHATE BINDING LYSINE RESIDUE ChemComp-A8W: Pregnenolone sulfate / 抗うつ薬*YM
由来	mus musculus (ハツカネズミ)
キーワード	TRANSPORT PROTEIN / Transient receptor potential channel / TRPM3 / neurosteroid / pregnenolone sulfate / neurodevelopmental disorders / anticonvulsant / primidone / neurological disorders / nociception / analgesic