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 of ligand recognition and activation of the histamine receptor family.
ジャーナル・号・ページ	Nat Commun, Vol. 15, Issue 1, Page 8296, Year 2024
掲載日	2024年9月27日
著者	Xuan Zhang / Guibing Liu / Ya-Ni Zhong / Ru Zhang / Chuan-Cheng Yang / Canyang Niu / Xuanyu Pu / Jingjing Sun / Tianyao Zhang / Lejin Yang / Chao Zhang / Xiu Li / Xinyuan Shen / Peng Xiao / Jin-Peng Sun / Weimin Gong /
PubMed 要旨	Histamine is a biogenic amine that is critical in various physiological and pathophysiological processes, including but not limited to allergic reactions, wakefulness, gastric acid secretion and ...Histamine is a biogenic amine that is critical in various physiological and pathophysiological processes, including but not limited to allergic reactions, wakefulness, gastric acid secretion and neurotransmission. Here, we determine 9 cryo-electron microscopy (cryo-EM) structures of the 4 histamine receptors in complex with four different G protein subtypes, with endogenous or synthetic agonists bound. Inside the ligand pocket, we identify key motifs for the recognition of histamine, the distinct binding orientations of histamine and three subpockets that facilitate the design of specific ligands. In addition, we also identify key residues responsible for the selectivity of immethridine. Moreover, we reveal distinct structural features as determinants of Gq vs. Gs or Gs vs. Gi coupling differences among the histamine receptors. Our study provides a structural framework for understanding the ligand recognition and G protein coupling of all 4 histamine receptors, which may facilitate the rational design of ligands targeting these receptors.
リンク	Nat Commun / PubMed:39333117 / PubMed Central
手法	EM (単粒子)
解像度	2.3 - 2.97 Å
構造データ	39412 8yn2 EMDB-39412, PDB-8yn2: Cryo-EM structure of histamine H1 receptor in complex with histamine and miniGq 手法: EM (単粒子) / 解像度: 2.66 Å 39413 8yn3 EMDB-39413, PDB-8yn3: Cryo-EM structure of histamine H2 receptor in complex with histamine and miniGs 手法: EM (単粒子) / 解像度: 2.56 Å 39414 8yn4 EMDB-39414, PDB-8yn4: Cryo-EM structure of histamine H2 receptor in complex with histamine and miniGq 手法: EM (単粒子) / 解像度: 2.97 Å 39415 8yn5 EMDB-39415, PDB-8yn5: Cryo-EM structure of histamine H3 receptor in complex with histamine and Gi 手法: EM (単粒子) / 解像度: 2.7 Å 39416 8yn6 EMDB-39416, PDB-8yn6: Cryo-EM structure of histamine H3 receptor in complex with imetit and Gi 手法: EM (単粒子) / 解像度: 2.77 Å 39417 8yn7 EMDB-39417, PDB-8yn7: Cryo-EM structure of histamine H3 receptor in complex with immethridine and miniGo 手法: EM (単粒子) / 解像度: 2.77 Å 39418 8yn8 EMDB-39418, PDB-8yn8: Cryo-EM structure of histamine H3 receptor in complex with proxyfan and miniGo 手法: EM (単粒子) / 解像度: 2.77 Å 39419 8yn9 EMDB-39419, PDB-8yn9: Cryo-EM structure of histamine H4 receptor in complex with histamine and Gi 手法: EM (単粒子) / 解像度: 2.3 Å 39420 8yna EMDB-39420, PDB-8yna: Cryo-EM structure of histamine H4 receptor in complex with immepip and Gi 手法: EM (単粒子) / 解像度: 2.63 Å
化合物	ChemComp-HSM: HISTAMINE / ヒスタミン / 神経伝達物質, ホルモンYM ChemComp-CLR: CHOLESTEROL / コレステロ-ル ChemComp-ITF: 2-(1~{H}-imidazol-5-yl)ethyl carbamimidothioate / イメチット PDB-1ly2: Crystal structure of unliganded human CD21 SCR1-SCR2 (Complement receptor type 2) PDB-1ly3: ANALYSIS OF QUINAZOLINE AND PYRIDOPYRIMIDINE N9-C10 REVERSED BRIDGE ANTIFOLATES IN COMPLEX WITH NADP+ AND PNEUMOCYSTIS CARINII DIHYDROFOLATE REDUCTASE ChemComp-HOH: WATER PDB-1ly4*: Analysis of quinazoline and PYRIDO[2,3D]PYRIMIDINE N9-C10 reversed bridge antifolates in complex with NADP+ and Pneumocystis carinii dihydrofolate reductase
由来	homo sapiens (ヒト) synthetic construct (人工物)
キーワード	SIGNALING PROTEIN / GPCR