7X8S
 
 | | Cryo-EM structure of the WB4-24-bound hGLP-1R-Gs complex | | 分子名称: | 2,4-bis(3-methoxy-4-thiophen-2-ylcarbonyloxy-phenyl)-1,3-bis[[4-(2-methylpropanoylamino)phenyl]carbonylamino]cyclobutane-1,3-dicarboxylic acid, Glucagon-like peptide 1 receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | Cong, Z.T, Zhou, Q.T, Li, Y, Chen, L.N, Zhang, Z.C, Liang, A.Y, Liu, Q, Wu, X.Y, Dai, A.T, Xia, T, Wu, W, Zhang, Y, Yang, D.H, Wang, M.W. | | 登録日 | 2022-03-14 | | 公開日 | 2022-06-29 | | 実験手法 | ELECTRON MICROSCOPY (3.09 Å) | | 主引用文献 | Structural basis of peptidomimetic agonism revealed by small- molecule GLP-1R agonists Boc5 and WB4-24.
Proc.Natl.Acad.Sci.USA, 119, 2022
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8THL
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3RZE
 | | Structure of the human histamine H1 receptor in complex with doxepin | | 分子名称: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (3E)-3-(dibenzo[b,e]oxepin-11(6H)-ylidene)-N,N-dimethylpropan-1-amine, (3Z)-3-(dibenzo[b,e]oxepin-11(6H)-ylidene)-N,N-dimethylpropan-1-amine, ... | | 著者 | Shimamura, T, Han, G.W, Shiroishi, M, Weyand, S, Tsujimoto, H, Winter, G, Katritch, V, Abagyan, R, Cherezov, V, Liu, W, Kobayashi, T, Stevens, R, Iwata, S, GPCR Network (GPCR) | | 登録日 | 2011-05-11 | | 公開日 | 2011-06-15 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (3.1 Å) | | 主引用文献 | Structure of the human histamine H1 receptor complex with doxepin.
Nature, 475, 2011
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3OE8
 | | Crystal structure of the CXCR4 chemokine receptor in complex with a small molecule antagonist IT1t in P1 spacegroup | | 分子名称: | (6,6-dimethyl-5,6-dihydroimidazo[2,1-b][1,3]thiazol-3-yl)methyl N,N'-dicyclohexylimidothiocarbamate, C-X-C chemokine receptor type 4, Lysozyme Chimera | | 著者 | Wu, B, Mol, C.D, Han, G.W, Katritch, V, Chien, E.Y.T, Liu, W, Cherezov, V, Stevens, R.C, Accelerated Technologies Center for Gene to 3D Structure (ATCG3D), GPCR Network (GPCR) | | 登録日 | 2010-08-12 | | 公開日 | 2010-10-27 | | 最終更新日 | 2021-10-06 | | 実験手法 | X-RAY DIFFRACTION (3.1 Å) | | 主引用文献 | Structures of the CXCR4 chemokine GPCR with small-molecule and cyclic peptide antagonists.
Science, 330, 2010
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6XOX
 | | cryo-EM of human GLP-1R bound to non-peptide agonist LY3502970 | | 分子名称: | 3-[(1S,2S)-1-(5-[(4S)-2,2-dimethyloxan-4-yl]-2-{(4S)-2-(4-fluoro-3,5-dimethylphenyl)-3-[3-(4-fluoro-1-methyl-1H-indazol-5-yl)-2-oxo-2,3-dihydro-1H-imidazol-1-yl]-4-methyl-2,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-carbonyl}-1H-indol-1-yl)-2-methylcyclopropyl]-1,2,4-oxadiazol-5(4H)-one, Alpha subunit of Gs with N-terminus swapped with equivalent residues in Gi,Guanine nucleotide-binding protein G(s) subunit alpha isoforms XLas, Glucagon-like peptide 1 receptor, ... | | 著者 | Sun, B, Kobilka, B.K, Sloop, K.W, Feng, D, Kobilka, T.S. | | 登録日 | 2020-07-07 | | 公開日 | 2020-11-18 | | 最終更新日 | 2020-12-09 | | 実験手法 | ELECTRON MICROSCOPY (3.1 Å) | | 主引用文献 | Structural basis for GLP-1 receptor activation by LY3502970, an orally active nonpeptide agonist.
Proc.Natl.Acad.Sci.USA, 117, 2020
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4LDL
 | | Structure of beta2 adrenoceptor bound to hydroxybenzylisoproterenol and an engineered nanobody | | 分子名称: | (2S)-2,3-dihydroxypropyl (7Z)-tetradec-7-enoate, 4-[(1R)-1-hydroxy-2-{[1-(4-hydroxyphenyl)-2-methylpropan-2-yl]amino}ethyl]benzene-1,2-diol, Camelid Antibody Fragment, ... | | 著者 | Ring, A.M, Manglik, A, Kruse, A.C, Enos, M.D, Weis, W.I, Garcia, K.C, Kobilka, B.K. | | 登録日 | 2013-06-24 | | 公開日 | 2013-09-25 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (3.1 Å) | | 主引用文献 | Adrenaline-activated structure of beta 2-adrenoceptor stabilized by an engineered nanobody.
Nature, 502, 2013
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5ZHP
 | | M3 muscarinic acetylcholine receptor in complex with a selective antagonist | | 分子名称: | (1R,2R,4S,5S,7s)-7-({[4-fluoro-2-(thiophen-2-yl)phenyl]carbamoyl}oxy)-9,9-dimethyl-3-oxa-9-azatricyclo[3.3.1.0~2,4~]nonan-9-ium, CITRIC ACID, HEXAETHYLENE GLYCOL, ... | | 著者 | Liu, H, Hofmann, J, Fish, I, Schaake, B, Eitel, K, Bartuschat, A, Kaindl, J, Rampp, H, Banerjee, A, Hubner, H, Clark, M.J, Vincent, S.G, Fisher, J, Heinrich, M, Hirata, K, Liu, X, Sunahara, R.K, Shoichet, B.K, Kobilka, B.K, Gmeiner, P. | | 登録日 | 2018-03-13 | | 公開日 | 2018-11-28 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (3.1 Å) | | 主引用文献 | Structure-guided development of selective M3 muscarinic acetylcholine receptor antagonists
Proc. Natl. Acad. Sci. U.S.A., 115, 2018
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3OE9
 | | Crystal structure of the chemokine CXCR4 receptor in complex with a small molecule antagonist IT1t in P1 spacegroup | | 分子名称: | (6,6-dimethyl-5,6-dihydroimidazo[2,1-b][1,3]thiazol-3-yl)methyl N,N'-dicyclohexylimidothiocarbamate, C-X-C chemokine receptor type 4, Lysozyme Chimera | | 著者 | Wu, B, Mol, C.D, Han, G.W, Katritch, V, Chien, E.Y.T, Liu, W, Cherezov, V, Stevens, R.C, Accelerated Technologies Center for Gene to 3D Structure (ATCG3D), GPCR Network (GPCR) | | 登録日 | 2010-08-12 | | 公開日 | 2010-10-27 | | 最終更新日 | 2021-10-06 | | 実験手法 | X-RAY DIFFRACTION (3.1 Å) | | 主引用文献 | Structures of the CXCR4 chemokine GPCR with small-molecule and cyclic peptide antagonists.
Science, 330, 2010
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7XKA
 | | Structure of human beta2 adrenergic receptor bound to constrained epinephrine | | 分子名称: | (5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol, Camelid Antibody Fragment, Endolysin,Beta-2 adrenergic receptor, ... | | 著者 | Xu, X, Shonberg, J, Kaindl, J, Clark, M, Stobel, A, Maul, L, Mayer, D, Hubner, H, Venkatakrishnan, A, Dror, R, Kobilka, B.K, Sunahara, R, Liu, X, Gmeiner, P. | | 登録日 | 2022-04-19 | | 公開日 | 2023-04-26 | | 最終更新日 | 2023-11-29 | | 実験手法 | X-RAY DIFFRACTION (3.1 Å) | | 主引用文献 | Constrained catecholamines gain beta 2 AR selectivity through allosteric effects on pocket dynamics.
Nat Commun, 14, 2023
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6KK7
 | | Structure of thermal-stabilised(M6) human GLP-1 receptor transmembrane domain | | 分子名称: | Glucagon-like peptide 1 receptor,Endolysin,Glucagon-like peptide 1 receptor, N-{4-[(R)-(3,3-dimethylcyclobutyl)({6-[4-(trifluoromethyl)-1H-imidazol-1-yl]pyridin-3-yl}amino)methyl]benzene-1-carbonyl}-beta-alanine | | 著者 | Song, G. | | 登録日 | 2019-07-23 | | 公開日 | 2019-11-13 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (3.1 Å) | | 主引用文献 | Mutagenesis facilitated crystallization of GLP-1R.
Iucrj, 6, 2019
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4RWS
 | | Crystal structure of CXCR4 and viral chemokine antagonist vMIP-II complex (PSI Community Target) | | 分子名称: | C-X-C chemokine receptor type 4/Endolysin chimeric protein, Viral macrophage inflammatory protein 2 | | 著者 | Qin, L, Kufareva, I, Holden, L, Wang, C, Zheng, Y, Wu, H, Fenalti, G, Han, G.W, Cherezov, V, Abagyan, R, Stevens, R.C, Handel, T.M, GPCR Network (GPCR) | | 登録日 | 2014-12-05 | | 公開日 | 2015-02-11 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (3.1 Å) | | 主引用文献 | Structural biology. Crystal structure of the chemokine receptor CXCR4 in complex with a viral chemokine.
Science, 347, 2015
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5CGC
 | | Structure of the human class C GPCR metabotropic glutamate receptor 5 transmembrane domain in complex with the negative allosteric modulator 3-chloro-4-fluoro-5-[6-(1H-pyrazol-1-yl)pyrimidin-4-yl]benzonitrile | | 分子名称: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, 3-chloro-4-fluoro-5-[6-(1H-pyrazol-1-yl)pyrimidin-4-yl]benzonitrile, Metabotropic glutamate receptor 5,Endolysin,Metabotropic glutamate receptor 5, ... | | 著者 | Christopher, J.A, Aves, S.J, Bennett, K.A, Dore, A.S, Errey, J.C, Jazayeri, A, Marshall, F.H, Okrasa, K, Serrano-Vega, M.J, Tehan, B.G, Wiggin, G.R, Congreve, M. | | 登録日 | 2015-07-09 | | 公開日 | 2015-08-12 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (3.101 Å) | | 主引用文献 | Fragment and Structure-Based Drug Discovery for a Class C GPCR: Discovery of the mGlu5 Negative Allosteric Modulator HTL14242 (3-Chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile).
J.Med.Chem., 58, 2015
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3NYA
 | | Crystal structure of the human beta2 adrenergic receptor in complex with the neutral antagonist alprenolol | | 分子名称: | (2S)-1-[(1-methylethyl)amino]-3-(2-prop-2-en-1-ylphenoxy)propan-2-ol, Beta-2 adrenergic receptor, Lysozyme, ... | | 著者 | Brown, M.A, Wacker, D, Fenalti, G, Katritch, V, Abagyan, R, Cherezov, V, Stevens, R.C, GPCR Network (GPCR) | | 登録日 | 2010-07-14 | | 公開日 | 2010-08-11 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (3.16 Å) | | 主引用文献 | Conserved Binding Mode of Human beta(2) Adrenergic Receptor Inverse Agonists and Antagonist Revealed by X-ray Crystallography
J.Am.Chem.Soc., 132, 2010
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5XF1
 | | Structure of the Full-length glucagon class B G protein-coupled receptor | | 分子名称: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, ... | | 著者 | Zhang, H, Qiao, A, Yang, D, Yang, L, Dai, A, de Graaf, C, Reedtz-Runge, S, Dharmarajan, V, Zhang, H, Han, G.W, Grant, T, Sierra, R, Weierstall, U, Nelson, G, Liu, W, Wu, Y, Ma, L, Cai, X, Lin, G, Wu, X, Geng, Z, Dong, Y, Song, G, Griffin, P, Lau, J, Cherezov, V, Yang, H, Hanson, M, Stevens, R, Jiang, H, Wang, M, Zhao, Q, Wu, B. | | 登録日 | 2017-04-06 | | 公開日 | 2017-05-24 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (3.19 Å) | | 主引用文献 | Structure of the full-length glucagon class B G-protein-coupled receptor.
Nature, 546, 2017
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4TN3
 | | Structure of the BBox-Coiled-coil region of Rhesus Trim5alpha | | 分子名称: | TRIM5/cyclophilin A fusion protein/T4 Lysozyme chimera, ZINC ION | | 著者 | Kirkpatrick, J.J, Stoye, J.P, Taylor, I.A, Goldstone, D.C. | | 登録日 | 2014-06-03 | | 公開日 | 2014-07-16 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (3.1989 Å) | | 主引用文献 | Structural studies of postentry restriction factors reveal antiparallel dimers that enable avid binding to the HIV-1 capsid lattice.
Proc.Natl.Acad.Sci.USA, 111, 2014
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6KPC
 | | Crystal structure of an agonist bound GPCR | | 分子名称: | 7-[(6aR,9R,10aR)-1-Hydroxy-9-(hydroxymethyl)-6,6-dimethyl-6a,7,8,9,10,10a-hexahydro-6H-benzo[c]chromen-3-yl]- 7-methyloctanenitrile, Cannabinoid receptor 2,Endolysin | | 著者 | Li, X.T, Hua, T, Wu, L.J, Makriyannis, A, Wu, M, Liu, Z.J. | | 登録日 | 2019-08-15 | | 公開日 | 2020-02-12 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (3.2 Å) | | 主引用文献 | Activation and Signaling Mechanism Revealed by Cannabinoid Receptor-GiComplex Structures.
Cell, 180, 2020
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5XSZ
 | | Crystal structure of zebrafish lysophosphatidic acid receptor LPA6 | | 分子名称: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, Lysophosphatidic acid receptor 6a,Endolysin,Lysophosphatidic acid receptor 6a | | 著者 | Taniguchi, R, Nishizawa, T, Ishitani, R, Nureki, O. | | 登録日 | 2017-06-16 | | 公開日 | 2017-08-16 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (3.2 Å) | | 主引用文献 | Structural insights into ligand recognition by the lysophosphatidic acid receptor LPA6
Nature, 548, 2017
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6J21
 | | Crystal structure of the human NK1 substance P receptor | | 分子名称: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 5-[[(2~{R},3~{S})-2-[(1~{R})-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholin-4-yl]methyl]-1,2-dihydro-1,2,4-triazol-3-one, Substance-P receptor,Endolysin | | 著者 | Chen, S, Lu, M, Zhang, H, Wu, B, Zhao, Q. | | 登録日 | 2018-12-30 | | 公開日 | 2019-03-06 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (3.2 Å) | | 主引用文献 | Human substance P receptor binding mode of the antagonist drug aprepitant by NMR and crystallography.
Nat Commun, 10, 2019
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3SN6
 | | Crystal structure of the beta2 adrenergic receptor-Gs protein complex | | 分子名称: | 8-[(1R)-2-{[1,1-dimethyl-2-(2-methylphenyl)ethyl]amino}-1-hydroxyethyl]-5-hydroxy-2H-1,4-benzoxazin-3(4H)-one, Camelid antibody VHH fragment, Endolysin,Beta-2 adrenergic receptor, ... | | 著者 | Rasmussen, S.G.F, DeVree, B.T, Zou, Y, Kruse, A.C, Chung, K.Y, Kobilka, T.S, Thian, F.S, Chae, P.S, Pardon, E, Calinski, D, Mathiesen, J.M, Shah, S.T.A, Lyons, J.A, Caffrey, M, Gellman, S.H, Steyaert, J, Skiniotis, G, Weis, W.I, Sunahara, R.K, Kobilka, B.K. | | 登録日 | 2011-06-28 | | 公開日 | 2011-07-20 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (3.2 Å) | | 主引用文献 | Crystal structure of the beta2 adrenergic receptor-Gs protein complex
Nature, 477, 2011
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3OE6
 | | Crystal structure of the CXCR4 chemokine receptor in complex with a small molecule antagonist IT1t in I222 spacegroup | | 分子名称: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (6,6-dimethyl-5,6-dihydroimidazo[2,1-b][1,3]thiazol-3-yl)methyl N,N'-dicyclohexylimidothiocarbamate, C-X-C chemokine receptor type 4, ... | | 著者 | Wu, B, Mol, C.D, Han, G.W, Katritch, V, Chien, E.Y.T, Liu, W, Cherezov, V, Stevens, R.C, Accelerated Technologies Center for Gene to 3D Structure (ATCG3D), GPCR Network (GPCR) | | 登録日 | 2010-08-12 | | 公開日 | 2010-10-27 | | 最終更新日 | 2021-10-06 | | 実験手法 | X-RAY DIFFRACTION (3.2 Å) | | 主引用文献 | Structures of the CXCR4 chemokine GPCR with small-molecule and cyclic peptide antagonists.
Science, 330, 2010
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4LDO
 | | Structure of beta2 adrenoceptor bound to adrenaline and an engineered nanobody | | 分子名称: | (2S)-2,3-dihydroxypropyl (7Z)-tetradec-7-enoate, Camelid Antibody Fragment, L-EPINEPHRINE, ... | | 著者 | Ring, A.M, Manglik, A, Kruse, A.C, Enos, M.D, Weis, W.I, Garcia, K.C, Kobilka, B.K. | | 登録日 | 2013-06-24 | | 公開日 | 2013-09-25 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (3.2 Å) | | 主引用文献 | Adrenaline-activated structure of beta 2-adrenoceptor stabilized by an engineered nanobody.
Nature, 502, 2013
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7RG9
 | | cryo-EM of human Glucagon-like peptide 1 receptor GLP-1R in apo form | | 分子名称: | Glucagon-like peptide 1 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, ... | | 著者 | Sun, B, Kobilka, B.K, Sloop, K.W, Feng, D, Kobilka, T.S. | | 登録日 | 2021-07-14 | | 公開日 | 2022-04-13 | | 実験手法 | ELECTRON MICROSCOPY (3.2 Å) | | 主引用文献 | Structural determinants of dual incretin receptor agonism by tirzepatide.
Proc.Natl.Acad.Sci.USA, 119, 2022
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5D6L
 | | beta2AR-T4L - CIM | | 分子名称: | (2S)-1-(9H-Carbazol-4-yloxy)-3-(isopropylamino)propan-2-ol, 1,4-BUTANEDIOL, ACETAMIDE, ... | | 著者 | Ma, P, Caffrey, M. | | 登録日 | 2015-08-12 | | 公開日 | 2016-08-17 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (3.2 Å) | | 主引用文献 | The cubicon method for concentrating membrane proteins in the cubic mesophase.
Nat Protoc, 12, 2017
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6LN2
 | | Crystal structure of full length human GLP1 receptor in complex with Fab fragment (Fab7F38) | | 分子名称: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Fab7F38_heavy chain, Fab7F38_light chain, ... | | 著者 | Wu, F, Yang, L, Hang, K, Laursen, M, Wu, L, Han, G.W, Ren, Q, Roed, N.K, Lin, G, Hanson, M, Jiang, H, Wang, M, Reedtz-Runge, S, Song, G, Stevens, R.C. | | 登録日 | 2019-12-28 | | 公開日 | 2020-03-18 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (3.2 Å) | | 主引用文献 | Full-length human GLP-1 receptor structure without orthosteric ligands.
Nat Commun, 11, 2020
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5JQH
 | | Structure of beta2 adrenoceptor bound to carazolol and inactive-state stabilizing nanobody, Nb60 | | 分子名称: | (2S)-1-(9H-Carbazol-4-yloxy)-3-(isopropylamino)propan-2-ol, CHOLESTEROL, Endolysin,Beta-2 adrenergic receptor, ... | | 著者 | Staus, D.P, Strachan, R.T, Manglik, A, Pani, B, Kahsai, A.W, Kim, T.H, Wingler, L.M, Ahn, S, Chatterjee, A, Masoudi, A, Kruse, A.C, Pardon, E, Steyaert, J, Weis, W.I, Prosser, R.S, Kobilka, B.K, Costa, T, Lefkowitz, R.J. | | 登録日 | 2016-05-05 | | 公開日 | 2016-07-13 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (3.2 Å) | | 主引用文献 | Allosteric nanobodies reveal the dynamic range and diverse mechanisms of G-protein-coupled receptor activation.
Nature, 535, 2016
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