登録情報 データベース : EMDB / ID : EMD-32535 ダウンロードとリンクタイトル Structure of SUR1 in complex with mitiglinide マップデータ 詳細 試料複合体 : Sulfonylurea receptor 1タンパク質・ペプチド : ATP-sensitive inward rectifier potassium channel 11,ATP-binding cassette sub-family C member 8 isoform X1リガンド : ADENOSINE-5'-TRIPHOSPHATEリガンド : (2S)-4-[(3aR,7aS)-1,3,3a,4,5,6,7,7a-octahydroisoindol-2-yl]-4-oxidanylidene-2-(phenylmethyl)butanoic acid 詳細 キーワード SUR1 / KATP / channel / mitiglinide / MEMBRANE PROTEIN機能・相同性 機能・相同性情報分子機能 ドメイン・相同性 構成要素
ATP sensitive Potassium channels / ATP-activated inward rectifier potassium channel activity / Regulation of insulin secretion / ABC-family proteins mediated transport / Ion homeostasis / inward rectifying potassium channel / sulfonylurea receptor activity / inward rectifier potassium channel activity / regulation of monoatomic ion transmembrane transport / nervous system process ... ATP sensitive Potassium channels / ATP-activated inward rectifier potassium channel activity / Regulation of insulin secretion / ABC-family proteins mediated transport / Ion homeostasis / inward rectifying potassium channel / sulfonylurea receptor activity / inward rectifier potassium channel activity / regulation of monoatomic ion transmembrane transport / nervous system process / ankyrin binding / response to ATP / potassium ion import across plasma membrane / negative regulation of insulin secretion / ABC-type transporter activity / regulation of membrane potential / potassium ion transport / glucose metabolic process / transmembrane transporter binding / membrane => GO:0016020 / response to xenobiotic stimulus / ATP binding / plasma membrane 類似検索 - 分子機能 Potassium channel, inwardly rectifying, Kir6.2 / ATP-binding cassette subfamily C member 8 / Sulphonylurea receptor / Potassium channel, inwardly rectifying, transmembrane domain / Inward rectifier potassium channel transmembrane domain / Potassium channel, inwardly rectifying, Kir, cytoplasmic / Potassium channel, inwardly rectifying, Kir / Inward rectifier potassium channel, C-terminal / Inward rectifier potassium channel C-terminal domain / ABC transporter transmembrane region ... Potassium channel, inwardly rectifying, Kir6.2 / ATP-binding cassette subfamily C member 8 / Sulphonylurea receptor / Potassium channel, inwardly rectifying, transmembrane domain / Inward rectifier potassium channel transmembrane domain / Potassium channel, inwardly rectifying, Kir, cytoplasmic / Potassium channel, inwardly rectifying, Kir / Inward rectifier potassium channel, C-terminal / Inward rectifier potassium channel C-terminal domain / ABC transporter transmembrane region / ABC transporter type 1, transmembrane domain / ABC transporter integral membrane type-1 fused domain profile. / ABC transporter type 1, transmembrane domain superfamily / ABC transporter-like, conserved site / ABC transporters family signature. / ABC transporter / ABC transporter-like, ATP-binding domain / ATP-binding cassette, ABC transporter-type domain profile. / Immunoglobulin E-set / ATPases associated with a variety of cellular activities / AAA+ ATPase domain / P-loop containing nucleoside triphosphate hydrolase 類似検索 - ドメイン・相同性 ATP-binding cassette sub-family C member 8 isoform X1 / ATP-sensitive inward rectifier potassium channel 11 類似検索 - 構成要素生物種 Mesocricetus auratus (ネズミ)手法 単粒子再構成法 / クライオ電子顕微鏡法 / 解像度 : 3.21 Å 詳細 データ登録者Chen L / Wang MM 資金援助 中国, 1件 詳細 詳細を隠すOrganization Grant number 国 National Natural Science Foundation of China (NSFC) 91957201 and 31870833 中国
引用ジャーナル : Front Pharmacol / 年 : 2022タイトル : Structural Insights Into the High Selectivity of the Anti-Diabetic Drug Mitiglinide.著者 : Mengmeng Wang / Jing-Xiang Wu / Lei Chen / 要旨 : Mitiglinide is a highly selective fast-acting anti-diabetic drug that induces insulin secretion by inhibiting pancreatic K channels. However, how mitiglinide binds K channels remains unknown. Here, ... Mitiglinide is a highly selective fast-acting anti-diabetic drug that induces insulin secretion by inhibiting pancreatic K channels. However, how mitiglinide binds K channels remains unknown. Here, we show the cryo-EM structure of the SUR1 subunit complexed with mitiglinide. The structure reveals that mitiglinide binds inside the common insulin secretagogue-binding site of SUR1, which is surrounded by TM7, TM8, TM16, and TM17. Mitiglinide locks SUR1 in the NBD-separated inward-facing conformation. The detailed structural analysis of the mitiglinide-binding site uncovers the molecular basis of its high selectivity. 履歴 登録 2022年1月4日 - ヘッダ(付随情報) 公開 2022年11月16日 - マップ公開 2022年11月16日 - 更新 2024年6月26日 - 現状 2024年6月26日 処理サイト : PDBj / 状態 : 公開
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