登録情報 データベース : EMDB / ID : EMD-9787 構造の表示 ダウンロードとリンクタイトル Structure of pancreatic ATP-sensitive potassium channel bound with repaglinide and ATPgammaS at 3.3A resolution マップデータthe sharpened map from cisTEM 詳細 試料複合体 : KATPタンパク質・ペプチド : ATP-sensitive inward rectifier potassium channel 11タンパク質・ペプチド : ATP-binding cassette sub-family C member 8 isoform X2リガンド : (2S)-3-(hexadecanoyloxy)-2-[(9Z)-octadec-9-enoyloxy]propyl 2-(trimethylammonio)ethyl phosphateリガンド : PHOSPHOTHIOPHOSPHORIC ACID-ADENYLATE ESTERリガンド : Digitoninリガンド : Repaglinideリガンド : PHOSPHATIDYLETHANOLAMINE 残り2件を表示 表示を減らす 詳細 キーワード KATP / channel / repaglinide / Kir / ABC transporter / SUR / MEMBRANE PROTEIN / diabetes / insulin secretagogue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 / response to resveratrol / ATP-activated inward rectifier potassium channel activity / glutamate secretion, neurotransmission / inward rectifying potassium channel / Regulation of insulin secretion / sulfonylurea receptor activity / ventricular cardiac muscle tissue development / cell body fiber / ABC-family proteins mediated transport ... ATP sensitive Potassium channels / response to resveratrol / ATP-activated inward rectifier potassium channel activity / glutamate secretion, neurotransmission / inward rectifying potassium channel / Regulation of insulin secretion / sulfonylurea receptor activity / ventricular cardiac muscle tissue development / cell body fiber / ABC-family proteins mediated transport / CAMKK-AMPK signaling cascade / voltage-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potential / inward rectifier potassium channel activity / ATPase-coupled monoatomic cation transmembrane transporter activity / Ion homeostasis / nervous system process / inorganic cation transmembrane transport / ankyrin binding / neuromuscular process / response to ATP / response to stress / potassium ion import across plasma membrane / potassium ion binding / response to testosterone / action potential / positive regulation of insulin secretion involved in cellular response to glucose stimulus / intercalated disc / axolemma / potassium channel activity / ABC-type transporter activity / cellular response to nutrient levels / negative regulation of insulin secretion / heat shock protein binding / T-tubule / acrosomal vesicle / response to ischemia / determination of adult lifespan / positive regulation of protein localization to plasma membrane / cellular response to glucose stimulus / ADP binding / cellular response to nicotine / glucose metabolic process / nuclear envelope / cellular response to tumor necrosis factor / response to estradiol / presynapse / presynaptic membrane / transmembrane transporter binding / response to hypoxia / endosome / response to xenobiotic stimulus / neuronal cell body / apoptotic process / glutamatergic synapse / ATP hydrolysis activity / ATP binding / plasma membrane / cytoplasm 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 / : ... 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 X2 / ATP-sensitive inward rectifier potassium channel 11 類似検索 - 構成要素生物種 Mus musculus (ハツカネズミ) / 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 : 3.3 Å 詳細 データ登録者Chen L / Ding D 資金援助 中国, 4件 詳細 詳細を隠すOrganization Grant number 国 Ministry of Science and Technology (China) 2016YFA0502004 中国 National Natural Science Foundation of China 31622021 中国 National Natural Science Foundation of China 31821091 中国 National Natural Science Foundation of China 31870833 中国
引用ジャーナル : Cell Rep / 年 : 2019タイトル : The Structural Basis for the Binding of Repaglinide to the Pancreatic K Channel.著者 : Dian Ding / Mengmeng Wang / Jing-Xiang Wu / Yunlu Kang / Lei Chen / 要旨 : Repaglinide (RPG) is a short-acting insulin secretagogue widely prescribed for the treatment of type 2 diabetes. It boosts insulin secretion by inhibiting the pancreatic ATP-sensitive potassium ... Repaglinide (RPG) is a short-acting insulin secretagogue widely prescribed for the treatment of type 2 diabetes. It boosts insulin secretion by inhibiting the pancreatic ATP-sensitive potassium channel (K). However, the mechanisms by which RPG binds to the K channel are poorly understood. Here, we describe two cryo-EM structures: the pancreatic K channel in complex with inhibitory RPG and adenosine-5'-(γ-thio)-triphosphate (ATPγS) at 3.3 Å and a medium-resolution structure of a RPG-bound mini SUR1 protein in which the N terminus of the inward-rectifying potassium channel 6.1 (Kir6.1) is fused to the ABC transporter module of the sulfonylurea receptor 1 (SUR1). These structures reveal the binding site of RPG in the SUR1 subunit. Furthermore, the high-resolution structure reveals the complex architecture of the ATP binding site, which is formed by both Kir6.2 and SUR1 subunits, and the domain-domain interaction interfaces. 履歴 登録 2019年1月25日 - ヘッダ(付随情報) 公開 2019年5月22日 - マップ公開 2019年5月22日 - 更新 2024年11月13日 - 現状 2024年11月13日 処理サイト : PDBj / 状態 : 公開
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