登録情報 データベース : EMDB / ID : EMD-30067 構造の表示 ダウンロードとリンクタイトル Structure of RyR1 (Ca2+/Caffeine/ATP/CaM1234/CHL) マップデータRyR1 Ca2 /ATP/caffeine/CaM1234/CHL 詳細 試料複合体 : RyR1 Ca2 /ATP/caffeine/CaM1234/CHL複合体 : RyR1タンパク質・ペプチド : Ryanodine receptor 1,Ryanodine receptor 1,Ryanodine receptor 1,Ryanodine receptor 1,Ryanodine receptor 1,Ryanodine receptor 1,Ryanodine receptor 1複合体 : FKBP12.6 and CAM1234タンパク質・ペプチド : Peptidyl-prolyl cis-trans isomerase FKBP1Bタンパク質・ペプチド : Calmodulin-1リガンド : CAFFEINEリガンド : CALCIUM IONリガンド : ADENOSINE-5'-TRIPHOSPHATEリガンド : ZINC IONリガンド : 5-bromanyl-N-[4-chloranyl-2-methyl-6-(methylcarbamoyl)phenyl]-2-(3-chloranylpyridin-2-yl)pyrazole-3-carboxamide 残り2件を表示 表示を減らす 詳細 キーワード Rabbit / Ryanodine receptor1 / CHL. / 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-gated ion channel activity / positive regulation of sequestering of calcium ion / cyclic nucleotide binding / negative regulation of calcium-mediated signaling / negative regulation of insulin secretion involved in cellular response to glucose stimulus / negative regulation of release of sequestered calcium ion into cytosol / neuronal action potential propagation / terminal cisterna / insulin secretion involved in cellular response to glucose stimulus / ryanodine receptor complex ... ATP-gated ion channel activity / positive regulation of sequestering of calcium ion / cyclic nucleotide binding / negative regulation of calcium-mediated signaling / negative regulation of insulin secretion involved in cellular response to glucose stimulus / negative regulation of release of sequestered calcium ion into cytosol / neuronal action potential propagation / terminal cisterna / insulin secretion involved in cellular response to glucose stimulus / ryanodine receptor complex / CaM pathway / ryanodine-sensitive calcium-release channel activity / Cam-PDE 1 activation / Sodium/Calcium exchangers / Calmodulin induced events / release of sequestered calcium ion into cytosol by sarcoplasmic reticulum / Reduction of cytosolic Ca++ levels / response to redox state / Activation of Ca-permeable Kainate Receptor / CREB1 phosphorylation through the activation of CaMKII/CaMKK/CaMKIV cascasde / Loss of phosphorylation of MECP2 at T308 / ossification involved in bone maturation / CREB1 phosphorylation through the activation of Adenylate Cyclase / 'de novo' protein folding / PKA activation / CaMK IV-mediated phosphorylation of CREB / negative regulation of high voltage-gated calcium channel activity / negative regulation of heart rate / Glycogen breakdown (glycogenolysis) / CLEC7A (Dectin-1) induces NFAT activation / Activation of RAC1 downstream of NMDARs / negative regulation of calcium ion export across plasma membrane / organelle localization by membrane tethering / mitochondrion-endoplasmic reticulum membrane tethering / skin development / autophagosome membrane docking / FK506 binding / presynaptic endocytosis / regulation of cardiac muscle cell action potential / positive regulation of axon regeneration / positive regulation of ryanodine-sensitive calcium-release channel activity / Synthesis of IP3 and IP4 in the cytosol / organelle membrane / regulation of cell communication by electrical coupling involved in cardiac conduction / Phase 0 - rapid depolarisation / cellular response to caffeine / Negative regulation of NMDA receptor-mediated neuronal transmission / negative regulation of ryanodine-sensitive calcium-release channel activity / Unblocking of NMDA receptors, glutamate binding and activation / RHO GTPases activate PAKs / calcineurin-mediated signaling / intracellularly gated calcium channel activity / outflow tract morphogenesis / Ion transport by P-type ATPases / Uptake and function of anthrax toxins / Long-term potentiation / Calcineurin activates NFAT / protein phosphatase activator activity / Regulation of MECP2 expression and activity / regulation of ryanodine-sensitive calcium-release channel activity / DARPP-32 events / smooth muscle contraction / response to vitamin E / Smooth Muscle Contraction / catalytic complex / toxic substance binding / detection of calcium ion / regulation of cardiac muscle contraction / RHO GTPases activate IQGAPs / voltage-gated calcium channel activity / regulation of cardiac muscle contraction by regulation of the release of sequestered calcium ion / smooth endoplasmic reticulum / presynaptic cytosol / calcium channel inhibitor activity / striated muscle contraction / cellular response to interferon-beta / Protein methylation / Activation of AMPK downstream of NMDARs / T cell proliferation / skeletal muscle fiber development / Ion homeostasis / regulation of release of sequestered calcium ion into cytosol by sarcoplasmic reticulum / eNOS activation / regulation of calcium-mediated signaling / Tetrahydrobiopterin (BH4) synthesis, recycling, salvage and regulation / titin binding / muscle contraction / voltage-gated potassium channel complex / sarcoplasmic reticulum membrane / release of sequestered calcium ion into cytosol / calcium channel regulator activity / sperm midpiece / substantia nigra development / calcium channel complex / calyx of Held / FCERI mediated Ca+2 mobilization / Ras activation upon Ca2+ influx through NMDA receptor / protein maturation / FCGR3A-mediated IL10 synthesis / adenylate cyclase activator activity 類似検索 - 分子機能 Ryanodine receptor, SPRY domain 2 / : / Ryanodine receptor junctional solenoid repeat / Ryanodine Receptor TM 4-6 / Ryanodine receptor / Ryanodine receptor, SPRY domain 1 / Ryanodine receptor, SPRY domain 3 / Ryanodine Receptor TM 4-6 / Ryanodine receptor Ryr / RyR domain ... Ryanodine receptor, SPRY domain 2 / : / Ryanodine receptor junctional solenoid repeat / Ryanodine Receptor TM 4-6 / Ryanodine receptor / Ryanodine receptor, SPRY domain 1 / Ryanodine receptor, SPRY domain 3 / Ryanodine Receptor TM 4-6 / Ryanodine receptor Ryr / RyR domain / : / RyR/IP3 receptor binding core, RIH domain superfamily / RyR/IP3R Homology associated domain / Inositol 1,4,5-trisphosphate/ryanodine receptor / RIH domain / RyR and IP3R Homology associated / Inositol 1,4,5-trisphosphate/ryanodine receptor / RIH domain / : / MIR motif / MIR domain / MIR domain profile. / Domain in ryanodine and inositol trisphosphate receptors and protein O-mannosyltransferases / Mir domain superfamily / SPRY domain / B30.2/SPRY domain / B30.2/SPRY domain profile. / B30.2/SPRY domain superfamily / Domain in SPla and the RYanodine Receptor. / SPRY domain / FKBP-type peptidyl-prolyl cis-trans isomerase / FKBP-type peptidyl-prolyl cis-trans isomerase domain / FKBP-type peptidyl-prolyl cis-trans isomerase domain profile. / Peptidyl-prolyl cis-trans isomerase domain superfamily / : / EF-hand domain pair / EF-hand, calcium binding motif / EF-Hand 1, calcium-binding site / EF-hand calcium-binding domain. / EF-hand calcium-binding domain profile. / EF-hand domain / Ion transport domain / Ion transport protein / EF-hand domain pair / Concanavalin A-like lectin/glucanase domain superfamily 類似検索 - ドメイン・相同性 Calmodulin-1 / Ryanodine receptor 1 / Peptidyl-prolyl cis-trans isomerase FKBP1B 類似検索 - 構成要素生物種 Oryctolagus cuniculus (ウサギ) / Homo sapiens (ヒト)手法 単粒子再構成法 / クライオ電子顕微鏡法 / 解像度 : 3.8 Å 詳細 データ登録者Ma R / Haji-Ghassemi O 資金援助 中国, カナダ, 4件 詳細 詳細を隠すOrganization Grant number 国 National Natural Science Foundation of China (NSFC) 31972287 中国 Ministry of Science and Technology (MoST, China) 2017YFD0201400 中国 Ministry of Science and Technology (MoST, China) 2017YFD0201403 中国 Canadian Institutes of Health Research (CIHR) PJT-159601 カナダ
引用ジャーナル : Nat Chem Biol / 年 : 2020タイトル : Structural basis for diamide modulation of ryanodine receptor.著者: Ruifang Ma / Omid Haji-Ghassemi / Dan Ma / Heng Jiang / Lianyun Lin / Li Yao / Arthur Samurkas / Yuxin Li / Yiwen Wang / Peng Cao / Shian Wu / Yan Zhang / Takashi Murayama / Bernard Moussian ... 著者 : Ruifang Ma / Omid Haji-Ghassemi / Dan Ma / Heng Jiang / Lianyun Lin / Li Yao / Arthur Samurkas / Yuxin Li / Yiwen Wang / Peng Cao / Shian Wu / Yan Zhang / Takashi Murayama / Bernard Moussian / Filip Van Petegem / Zhiguang Yuchi / 要旨 : The diamide insecticide class is one of the top-selling insecticides globally. They are used to control a wide range of pests by targeting their ryanodine receptors (RyRs). Here, we report the ... The diamide insecticide class is one of the top-selling insecticides globally. They are used to control a wide range of pests by targeting their ryanodine receptors (RyRs). Here, we report the highest-resolution cryo-electron microscopy (cryo-EM) structure of RyR1 in the open state, in complex with the anthranilic diamide chlorantraniliprole (CHL). The 3.2-Å local resolution map facilitates unambiguous assignment of the CHL binding site. The molecule induces a conformational change by affecting the S4-S5 linker, triggering channel opening. The binding site is further corroborated by mutagenesis data, which reveal how diamide insecticides are selective to the Lepidoptera group of insects over honeybee or mammalian RyRs. Our data reveal that several pests have developed resistance via two mechanisms, steric hindrance and loss of contact. Our results provide a foundation for the development of highly selective pesticides aimed at overcoming resistance and therapeutic molecules to treat human myopathies. 履歴 登録 2020年3月1日 - ヘッダ(付随情報) 公開 2020年9月2日 - マップ公開 2020年9月2日 - 更新 2024年3月27日 - 現状 2024年3月27日 処理サイト : PDBj / 状態 : 公開
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