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 basis for the subtype-selective activation of K3.1 channels.
ジャーナル・号・ページ	Structure, Year 2026
掲載日	2026年5月14日
著者	Alena Ramanishka / Joshua A Nasburg / Yang Xu / Xinyi Ma / Reza Mehvar / Meng Cui / Young-Woo Nam / Heike Wulff / Miao Zhang /
PubMed 要旨	The intermediate-conductance (K3.1) and the small-conductance (K2.2) Ca-activated K channels share a Ca-calmodulin dependent gating mechanism. We report cryo-electron microscopy structures of K3.1 ...The intermediate-conductance (K3.1) and the small-conductance (K2.2) Ca-activated K channels share a Ca-calmodulin dependent gating mechanism. We report cryo-electron microscopy structures of K3.1 and K2.2 in complex with two benzothiazole-type activators. While SKA-31 is only moderately selective (∼7.3-fold), its derivative SKA-111 exhibits ∼70-fold selectivity for K3.1 over K2.2. SKA-31 and SKA-111 both bind in a pocket at the interface between the SA helix and calmodulin where they allosterically modulate the inner gate of the two channels. SKA-31 binds with comparable energies in the two channels, consistent with its moderate selectivity for K3.1 over K2.2. In the K3.1 structure, the calmodulin helix IV is positioned outward, forming a pocket that more readily accommodates the bulkier SKA-111 that sits deeper inside calmodulin's N-lobe in K3.1 than in K2.2. The resulting higher binding energy explains the improved selectivity of SKA-111 for K3.1 compared to the less selective SKA-31.
リンク	Structure / PubMed:42140186
手法	EM (単粒子)
解像度	2.77 - 3.67 Å
構造データ	74531 9zpo EMDB-74531, PDB-9zpo: Cryo-EM structure of KCa3.1_I/calmodulin channel in complex with SKA31. 手法: EM (単粒子) / 解像度: 3.67 Å 74533 9zpt EMDB-74533, PDB-9zpt: Cryo-EM structure of KCa3.1_II/calmodulin channel in complex with SKA31. 手法: EM (単粒子) / 解像度: 3.39 Å 74625 9zrk EMDB-74625, PDB-9zrk: Cryo-EM structure of KCa3.1_I/calmodulin channel in complex with SKA111. 手法: EM (単粒子) / 解像度: 2.99 Å 74626 9zrl EMDB-74626, PDB-9zrl: Cryo-EM structure of KCa3.1_II/calmodulin channel in complex with SKA111. 手法: EM (単粒子) / 解像度: 3.38 Å 74627 9zrq EMDB-74627, PDB-9zrq: Cryo-EM structure of KCa2.2/calmodulin channel in complex with SKA31. 手法: EM (単粒子) / 解像度: 2.77 Å 74628 9zrr EMDB-74628, PDB-9zrr: Cryo-EM structure of KCa2.2/calmodulin channel in complex with SKA111. 手法: EM (単粒子) / 解像度: 3.31 Å
化合物	PDB-1c3q: CRYSTAL STRUCTURE OF NATIVE THIAZOLE KINASE IN THE MONOCLINIC FORM ChemComp-CA: Unknown entry ChemComp-K: Unknown entry PDB-1c3u: T. MARITIMA ADENYLOSUCCINATE LYASE ChemComp-HOH: WATER
由来	homo sapiens (ヒト)
キーワード	MEMBRANE PROTEIN / Intermediate conductance calcium-activated potassium channel / Ion channel / Calmodulin binding protein / TRANSPORT PROTEIN