登録情報 データベース : PDB / ID : 6k41 構造の表示 ダウンロードとリンクタイトル cryo-EM structure of alpha2BAR-GoA complex 要素(Guanine nucleotide-binding protein ...) x 3 Alpha-2A adrenergic receptor,Endolysin,Alpha-2B adrenergic receptor,Alpha-2B adrenergic receptor scFv 単鎖可変領域フラグメント 詳細キーワード MEMBRANE PROTEIN (膜タンパク質) / GPCR (Gタンパク質共役受容体) / Complex / cryo-EM (低温電子顕微鏡法)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
Activation of the phototransduction cascade / Sensory perception of sweet, bitter, and umami (glutamate) taste / regulation of vascular associated smooth muscle contraction / Olfactory Signaling Pathway / adenylate cyclase-inhibiting adrenergic receptor signaling pathway / phospholipase C-activating adrenergic receptor signaling pathway / alpha2-adrenergic receptor activity / Adrenaline signalling through Alpha-2 adrenergic receptor / G beta:gamma signalling through PLC beta / Presynaptic function of Kainate receptors ... Activation of the phototransduction cascade / Sensory perception of sweet, bitter, and umami (glutamate) taste / regulation of vascular associated smooth muscle contraction / Olfactory Signaling Pathway / adenylate cyclase-inhibiting adrenergic receptor signaling pathway / phospholipase C-activating adrenergic receptor signaling pathway / alpha2-adrenergic receptor activity / Adrenaline signalling through Alpha-2 adrenergic receptor / G beta:gamma signalling through PLC beta / Presynaptic function of Kainate receptors / alpha-2C adrenergic receptor binding / receptor transactivation / epinephrine binding / Prostacyclin signalling through prostacyclin receptor / G alpha (z) signalling events / Glucagon-type ligand receptors / G beta:gamma signalling through PI3Kgamma / G beta:gamma signalling through CDC42 / Synthesis, secretion, and inactivation of Glucagon-like Peptide-1 (GLP-1) / G beta:gamma signalling through BTK / Adrenaline,noradrenaline inhibits insulin secretion / ADP signalling through P2Y purinoceptor 12 / Cooperation of PDCL (PhLP1) and TRiC/CCT in G-protein beta folding / Thromboxane signalling through TP receptor / positive regulation of uterine smooth muscle contraction / negative regulation of norepinephrine secretion / Thrombin signalling through proteinase activated receptors (PARs) / positive regulation of epidermal growth factor-activated receptor activity / Activation of G protein gated Potassium channels / Inhibition of voltage gated Ca2+ channels via Gbeta/gamma subunits / G-protein activation / Ca2+ pathway / G alpha (s) signalling events / negative regulation of epinephrine secretion / G alpha (q) signalling events / Extra-nuclear estrogen signaling / G alpha (12/13) signalling events / heterotrimeric G-protein binding / Vasopressin regulates renal water homeostasis via Aquaporins / G alpha (i) signalling events / GPER1 signaling / regulation of smooth muscle contraction / dopaminergic synapse / Glucagon-like Peptide-1 (GLP1) regulates insulin secretion / ADP signalling through P2Y purinoceptor 1 / mu-type opioid receptor binding / phototransduction, visible light / corticotropin-releasing hormone receptor 1 binding / positive regulation of blood pressure / fear response / thioesterase binding / negative regulation of insulin secretion involved in cellular response to glucose stimulus / alkylglycerophosphoethanolamine phosphodiesterase activity / norepinephrine binding / アドレナリン受容体 / positive regulation of membrane protein ectodomain proteolysis / photoreceptor outer segment membrane / dopamine receptor signaling pathway / regulation of synaptic vesicle exocytosis / spectrin binding / positive regulation of wound healing / adrenergic receptor signaling pathway / plasma membrane => GO:0005886 / regulation of vasoconstriction / photoreceptor outer segment / G protein-coupled serotonin receptor binding / negative regulation of lipid catabolic process / adenylate cyclase-activating adrenergic receptor signaling pathway / viral release from host cell by cytolysis / cellular response to hormone stimulus / cardiac muscle cell apoptotic process / positive regulation of neuron differentiation / activation of protein kinase B activity / photoreceptor inner segment / peptidoglycan catabolic process / positive regulation of cytokine production / female pregnancy / muscle contraction / G protein-coupled receptor activity / positive regulation of MAP kinase activity / G-protein beta/gamma-subunit complex binding / adenylate cyclase-modulating G protein-coupled receptor signaling pathway / G beta:gamma signalling through PLC beta / Presynaptic function of Kainate receptors / Thromboxane signalling through TP receptor / G-protein activation / Activation of G protein gated Potassium channels / Inhibition of voltage gated Ca2+ channels via Gbeta/gamma subunits / Prostacyclin signalling through prostacyclin receptor / Glucagon signaling in metabolic regulation / G beta:gamma signalling through CDC42 / ADP signalling through P2Y purinoceptor 12 / G beta:gamma signalling through BTK / 凝固・線溶系 / Adrenaline,noradrenaline inhibits insulin secretion / Glucagon-type ligand receptors / Vasopressin regulates renal water homeostasis via Aquaporins / G alpha (z) signalling events / cellular response to catecholamine stimulus / Glucagon-like Peptide-1 (GLP1) regulates insulin secretion 類似検索 - 分子機能 Alpha 2B adrenoceptor / Alpha 2A adrenoceptor / Transducin (heterotrimeric G protein), gamma chain / G Protein Gi Gamma 2 / Adrenoceptor family / Rhopdopsin 7-helix transmembrane proteins / Rhodopsin 7-helix transmembrane proteins / YVTN repeat-like/Quinoprotein amine dehydrogenase / G-protein alpha subunit, group I / Endolysin T4 type ... Alpha 2B adrenoceptor / Alpha 2A adrenoceptor / Transducin (heterotrimeric G protein), gamma chain / G Protein Gi Gamma 2 / Adrenoceptor family / Rhopdopsin 7-helix transmembrane proteins / Rhodopsin 7-helix transmembrane proteins / YVTN repeat-like/Quinoprotein amine dehydrogenase / G-protein alpha subunit, group I / Endolysin T4 type / T4-type lysozyme / Glycoside hydrolase, family 24 / Lysozyme domain superfamily / Phage lysozyme / 7 Propeller / Methylamine Dehydrogenase; Chain H / Serpentine type 7TM GPCR chemoreceptor Srsx / G-alpha domain profile. / Guanine nucleotide binding protein (G-protein), alpha subunit / G protein alpha subunit, helical insertion / G-protein alpha subunit / G protein alpha subunit / G-protein, gamma subunit / G-protein gamma subunit domain profile. / GGL domain / G-protein gamma-like domain superfamily / G-protein gamma-like domain / GGL domain / G protein gamma subunit-like motifs / Guanine nucleotide-binding protein, beta subunit / G-protein, beta subunit / G-protein coupled receptors family 1 signature. / G protein-coupled receptor, rhodopsin-like / GPCR, rhodopsin-like, 7TM / G-protein coupled receptors family 1 profile. / 7 transmembrane receptor (rhodopsin family) / Few Secondary Structures / イレギュラー / Lysozyme-like domain superfamily / G-protein beta WD-40 repeat / WD40 repeat, conserved site / Trp-Asp (WD) repeats signature. / Trp-Asp (WD) repeats profile. / Trp-Asp (WD) repeats circular profile. / WD domain, G-beta repeat / WD40リピート / WD40リピート / WD40-repeat-containing domain superfamily / WD40/YVTN repeat-like-containing domain superfamily / Up-down Bundle / P-loop containing nucleoside triphosphate hydrolase / Mainly Beta / Mainly Alpha 類似検索 - ドメイン・相同性 Chem-CZX / Endolysin / Guanine nucleotide-binding protein G(o) subunit alpha / Alpha-2B adrenergic receptor / Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2 / Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1 / Alpha-2A adrenergic receptor 類似検索 - 構成要素生物種 Homo sapiens (ヒト)Mus musculus (ハツカネズミ)Bos taurus (ウシ) Enterobacteria phage RB59 (ファージ)手法 電子顕微鏡法 / 単粒子再構成法 / クライオ電子顕微鏡法 / 解像度 : 2.9 Å 詳細データ登録者 Yuan, D. / Liu, Z. / Wang, H.W. / Kobilka, B.K. 引用ジャーナル : Nat Chem Biol / 年 : 2020タイトル : Activation of the α adrenoceptor by the sedative sympatholytic dexmedetomidine.著者 : Daopeng Yuan / Zhongmin Liu / Jonas Kaindl / Shoji Maeda / Jiawei Zhao / Xiaoou Sun / Jun Xu / Peter Gmeiner / Hong-Wei Wang / Brian K Kobilka / 要旨 : The α adrenergic receptors (αARs) are G protein-coupled receptors (GPCRs) that respond to adrenaline and noradrenaline and couple to the Gi/o family of G proteins. αARs play important roles in ... The α adrenergic receptors (αARs) are G protein-coupled receptors (GPCRs) that respond to adrenaline and noradrenaline and couple to the Gi/o family of G proteins. αARs play important roles in regulating the sympathetic nervous system. Dexmedetomidine is a highly selective αAR agonist used in post-operative patients as an anxiety-reducing, sedative medicine that decreases the requirement for opioids. As is typical for selective αAR agonists, dexmedetomidine consists of an imidazole ring and a substituted benzene moiety lacking polar groups, which is in contrast to βAR-selective agonists, which share an ethanolamine group and an aromatic system with polar, hydrogen-bonding substituents. To better understand the structural basis for the selectivity and efficacy of adrenergic agonists, we determined the structure of the αAR in complex with dexmedetomidine and Go at a resolution of 2.9 Å by single-particle cryo-EM. The structure reveals the mechanism of αAR-selective activation and provides insights into Gi/o coupling specificity. 履歴 登録 2019年5月23日 登録サイト : PDBJ / 処理サイト : PDBJ改定 1.0 2020年4月15日 Provider : repository / タイプ : Initial release改定 1.1 2020年5月6日 Group : Database references / カテゴリ : citation / citation_authorItem : _citation.journal_volume / _citation.page_first ... _citation.journal_volume / _citation.page_first / _citation.page_last / _citation_author.identifier_ORCID 改定 1.2 2020年5月13日 Group : Structure summary / カテゴリ : audit_author / Item : _audit_author.name
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