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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7BVQ
 | | Structure of human beta1 adrenergic receptor bound to carazolol | | 分子名称: | (2S)-1-(9H-Carbazol-4-yloxy)-3-(isopropylamino)propan-2-ol, (2S)-2,3-dihydroxypropyl (7Z)-tetradec-7-enoate, CHOLESTEROL, ... | | 著者 | Xu, X, Kaindl, J, Clark, M, Hubner, H, Hirata, K, Sunahara, R, Gmeiner, P, Kobilka, B.K, Liu, X. | | 登録日 | 2020-04-11 | | 公開日 | 2020-12-02 | | 最終更新日 | 2023-11-29 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | Binding pathway determines norepinephrine selectivity for the human beta 1 AR over beta 2 AR.
Cell Res., 31, 2021
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7SBF
 | | PZM21 bound Mu Opioid Receptor-Gi Protein Complex | | 分子名称: | 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, Guanine nucleotide-binding protein G(i) subunit alpha-1, ... | | 著者 | Huang, W, Qu, Q, Wang, H, Skiniotis, G, Kobilka, B. | | 登録日 | 2021-09-24 | | 公開日 | 2022-04-20 | | 最終更新日 | 2022-07-06 | | 実験手法 | ELECTRON MICROSCOPY (2.9 Å) | | 主引用文献 | Structure-Based Evolution of G Protein-Biased mu-Opioid Receptor Agonists.
Angew.Chem.Int.Ed.Engl., 61, 2022
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7XK9
 | | Structure of human beta2 adrenergic receptor bound to constrained isoproterenol | | 分子名称: | (5R,6R)-6-(propan-2-ylamino)-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 (3.4 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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7BTS
 | | Structure of human beta1 adrenergic receptor bound to epinephrine and nanobody 6B9 | | 分子名称: | (2S)-2,3-dihydroxypropyl (7Z)-tetradec-7-enoate, 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID, CHOLESTEROL, ... | | 著者 | Xu, X, Kaindl, J, Clark, M, Hubner, H, Hirata, K, Sunahara, R, Gmeiner, P, Kobilka, B.K, Liu, X. | | 登録日 | 2020-04-02 | | 公開日 | 2020-12-02 | | 最終更新日 | 2023-11-29 | | 実験手法 | X-RAY DIFFRACTION (3.13 Å) | | 主引用文献 | Binding pathway determines norepinephrine selectivity for the human beta 1 AR over beta 2 AR.
Cell Res., 31, 2021
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3UON
 | | Structure of the human M2 muscarinic acetylcholine receptor bound to an antagonist | | 分子名称: | (3R)-1-azabicyclo[2.2.2]oct-3-yl hydroxy(diphenyl)acetate, CHLORIDE ION, Human M2 muscarinic acetylcholine, ... | | 著者 | Haga, K, Kruse, A.C, Asada, H, Yurugi-Kobayashi, T, Shiroishi, M, Zhang, C, Weis, W.I, Okada, T, Kobilka, B.K, Haga, T, Kobayashi, T. | | 登録日 | 2011-11-16 | | 公開日 | 2012-02-01 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (3 Å) | | 主引用文献 | Structure of the human M2 muscarinic acetylcholine receptor bound to an antagonist.
Nature, 482, 2012
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7BU6
 | | Structure of human beta1 adrenergic receptor bound to norepinephrine and nanobody 6B9 | | 分子名称: | (2S)-2,3-dihydroxypropyl octanoate, 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID, CHOLESTEROL, ... | | 著者 | Xu, X, Kaindl, J, Clark, M, Hubner, H, Hirata, K, Sunahara, R, Gmeiner, P, Kobilka, B.K, Liu, X. | | 登録日 | 2020-04-04 | | 公開日 | 2020-12-02 | | 最終更新日 | 2023-11-29 | | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | | 主引用文献 | Binding pathway determines norepinephrine selectivity for the human beta 1 AR over beta 2 AR.
Cell Res., 31, 2021
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7SCG
 | | FH210 bound Mu Opioid Receptor-Gi Protein Complex | | 分子名称: | (2E)-N-[(2S)-2-(dimethylamino)-3-(4-hydroxyphenyl)propyl]-3-(naphthalen-1-yl)prop-2-enamide, 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 | Wang, H, Kobilka, B. | | 登録日 | 2021-09-28 | | 公開日 | 2022-04-20 | | 最終更新日 | 2022-07-06 | | 実験手法 | ELECTRON MICROSCOPY (3 Å) | | 主引用文献 | Structure-Based Evolution of G Protein-Biased mu-Opioid Receptor Agonists.
Angew.Chem.Int.Ed.Engl., 61, 2022
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6OIJ
 | | Muscarinic acetylcholine receptor 1-G11 protein complex | | 分子名称: | 4-(4,5-dihydro-1,2-oxazol-3-yloxy)-N,N,N-trimethylbut-2-yn-1-aminium, Antibody fragment, CHOLESTEROL HEMISUCCINATE, ... | | 著者 | Maeda, S, Qianhui, Q, Skiniotis, G, Kobilka, B. | | 登録日 | 2019-04-09 | | 公開日 | 2019-05-08 | | 最終更新日 | 2020-01-08 | | 実験手法 | ELECTRON MICROSCOPY (3.3 Å) | | 主引用文献 | Structures of the M1 and M2 muscarinic acetylcholine receptor/G-protein complexes.
Science, 364, 2019
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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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4LDE
 | | Structure of beta2 adrenoceptor bound to BI167107 and an engineered nanobody | | 分子名称: | (2S)-2,3-dihydroxypropyl (7Z)-tetradec-7-enoate, 8-[(1R)-2-{[1,1-dimethyl-2-(2-methylphenyl)ethyl]amino}-1-hydroxyethyl]-5-hydroxy-2H-1,4-benzoxazin-3(4H)-one, 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 (2.79 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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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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3VW7
 | | Crystal structure of human protease-activated receptor 1 (PAR1) bound with antagonist vorapaxar at 2.2 angstrom | | 分子名称: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, CHLORIDE ION, Proteinase-activated receptor 1, ... | | 著者 | Zhang, C, Srinivasan, Y, Arlow, D.H, Fung, J.J, Palmer, D, Zheng, Y, Green, H.F, Pandey, A, Dror, R.O, Shaw, D.E, Weis, W.I, Coughlin, S.R, Kobilka, B.K. | | 登録日 | 2012-08-07 | | 公開日 | 2012-12-12 | | 最終更新日 | 2023-11-08 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | High-resolution crystal structure of human protease-activated receptor 1
Nature, 492, 2012
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4QKX
 | | Structure of beta2 adrenoceptor bound to a covalent agonist and an engineered nanobody | | 分子名称: | 4-[(1R)-1-hydroxy-2-({2-[3-methoxy-4-(2-sulfanylethoxy)phenyl]ethyl}amino)ethyl]benzene-1,2-diol, Beta-2 adrenergic receptor, R9 protein, ... | | 著者 | Weichert, D, Kruse, A.C, Manglik, A, Hiller, C, Zhang, C, Huebner, H, Kobilka, B.K, Gmeiner, P. | | 登録日 | 2014-06-10 | | 公開日 | 2014-07-23 | | 最終更新日 | 2017-06-28 | | 実験手法 | X-RAY DIFFRACTION (3.3 Å) | | 主引用文献 | Covalent agonists for studying G protein-coupled receptor activation.
Proc.Natl.Acad.Sci.USA, 111, 2014
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7T90
 | | Cryo-EM structure of ACh-bound M2R-Go signaling complex in S2 state | | 分子名称: | ACETYLCHOLINE, 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 | Xu, J, Wang, Q, Du, Y, Kobilka, B.K. | | 登録日 | 2021-12-17 | | 公開日 | 2023-01-25 | | 最終更新日 | 2024-02-07 | | 実験手法 | ELECTRON MICROSCOPY (3.32 Å) | | 主引用文献 | Structural and dynamic insights into supra-physiological activation and allosteric modulation of a muscarinic acetylcholine receptor.
Nat Commun, 14, 2023
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7T8X
 | | Cryo-EM structure of ACh-bound M2R-Go signaling complex in S1 state | | 分子名称: | ACETYLCHOLINE, Antibody fragment, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | Xu, J, Wang, Q, Du, Y, Kobilka, B.K. | | 登録日 | 2021-12-17 | | 公開日 | 2023-01-25 | | 最終更新日 | 2024-02-07 | | 実験手法 | ELECTRON MICROSCOPY (3.21 Å) | | 主引用文献 | Structural and dynamic insights into supra-physiological activation and allosteric modulation of a muscarinic acetylcholine receptor.
Nat Commun, 14, 2023
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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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4MQT
 | | Structure of active human M2 muscarinic acetylcholine receptor bound to the agonist iperoxo and allosteric modulator LY2119620 | | 分子名称: | 3-amino-5-chloro-N-cyclopropyl-4-methyl-6-[2-(4-methylpiperazin-1-yl)-2-oxoethoxy]thieno[2,3-b]pyridine-2-carboxamide, 4-(4,5-dihydro-1,2-oxazol-3-yloxy)-N,N,N-trimethylbut-2-yn-1-aminium, Muscarinic acetylcholine receptor M2, ... | | 著者 | Kruse, A.C, Ring, A.M, Manglik, A, Hu, J, Hu, K, Eitel, K, Huebner, H, Pardon, E, Valant, C, Sexton, P.M, Christopoulos, A, Felder, C.C, Gmeiner, P, Steyaert, J, Weis, W.I, Garcia, K.C, Wess, J, Kobilka, B.K. | | 登録日 | 2013-09-16 | | 公開日 | 2013-11-27 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (3.7 Å) | | 主引用文献 | Activation and allosteric modulation of a muscarinic acetylcholine receptor.
Nature, 504, 2013
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4JQI
 | | Structure of active beta-arrestin1 bound to a G protein-coupled receptor phosphopeptide | | 分子名称: | 1,2-ETHANEDIOL, Beta-arrestin-1, CHLORIDE ION, ... | | 著者 | Shukla, A.K, Manglik, A, Kruse, A.C, Xiao, K, Reis, R.I, Tseng, W.C, Staus, D.P, Hilger, D, Uysal, S, Huang, L.H, Paduch, M, Shukla, P.T, Koide, A, Koide, S, Weis, W.I, Kossiakoff, A.A, Kobilka, B.K, Lefkowitz, R.J. | | 登録日 | 2013-03-20 | | 公開日 | 2013-04-17 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | Structure of active beta-arrestin-1 bound to a G-protein-coupled receptor phosphopeptide.
Nature, 497, 2013
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6N48
 | | Structure of beta2 adrenergic receptor bound to BI167107, Nanobody 6B9, and a positive allosteric modulator | | 分子名称: | (2S)-2,3-dihydroxypropyl (7Z)-tetradec-7-enoate, 8-[(1R)-2-{[1,1-dimethyl-2-(2-methylphenyl)ethyl]amino}-1-hydroxyethyl]-5-hydroxy-2H-1,4-benzoxazin-3(4H)-one, Camelid Antibody Fragment, ... | | 著者 | Liu, X, Masoudi, A, Kahsai, A.W, Huang, L.Y, Pani, B, Hirata, K, Ahn, S, Lefkowitz, R.J, Kobilka, B.K. | | 登録日 | 2018-11-17 | | 公開日 | 2019-06-26 | | 最終更新日 | 2023-10-11 | | 実験手法 | X-RAY DIFFRACTION (3.2 Å) | | 主引用文献 | Mechanism of beta2AR regulation by an intracellular positive allosteric modulator.
Science, 364, 2019
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4GBR
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6OBA
 | | The beta2 adrenergic receptor bound to a negative allosteric modulator | | 分子名称: | (2S)-1-[(1-methylethyl)amino]-3-(2-prop-2-en-1-ylphenoxy)propan-2-ol, 6-bromo-N~2~-phenylquinazoline-2,4-diamine, Beta-2 adrenergic receptor,Lysozyme,Beta-2 adrenergic receptor, ... | | 著者 | Liu, X, Stobel, A, Kaindl, J, Dengler, D, ClarK, M, Mahoney, J, Korczynska, M, Matt, R.A, Hubner, H, Xu, X, Stanek, M, Hirata, K, Shoichet, B, Sunahara, R, Gmeiner, R, Kobilka, B.K. | | 登録日 | 2019-03-20 | | 公開日 | 2020-03-25 | | 最終更新日 | 2023-10-11 | | 実験手法 | X-RAY DIFFRACTION (3.1 Å) | | 主引用文献 | An allosteric modulator binds to a conformational hub in the beta2adrenergic receptor.
Nat.Chem.Biol., 16, 2020
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5ZKB
 | | Crystal structure of rationally thermostabilized M2 muscarinic acetylcholine receptor bound with AF-DX 384 | | 分子名称: | Muscarinic acetylcholine receptor M2,Apo-cytochrome b562,Muscarinic acetylcholine receptor M2, N-[2-[(2S)-2-[(dipropylamino)methyl]piperidin-1-yl]ethyl]-6-oxidanylidene-5H-pyrido[2,3-b][1,4]benzodiazepine-11-carboxamide | | 著者 | Suno, R, Maeda, S, Yasuda, S, Yamashita, K, Hirata, K, Horita, S, Tawaramoto, M.S, Tsujimoto, H, Murata, T, Kinoshita, M, Yamamoto, M, Kobilka, B.K, Iwata, S, Kobayashi, T. | | 登録日 | 2018-03-23 | | 公開日 | 2018-11-21 | | 最終更新日 | 2022-03-23 | | 実験手法 | X-RAY DIFFRACTION (2.95 Å) | | 主引用文献 | Structural insights into the subtype-selective antagonist binding to the M2muscarinic receptor
Nat. Chem. Biol., 14, 2018
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7T2G
 | | CryoEM structure of mu-opioid receptor - Gi protein complex bound to mitragynine pseudoindoxyl (MP) | | 分子名称: | CHOLESTEROL, 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 | Seven, A.B, Qu, Q, Robertson, M.J, Wang, H, Kobilka, B.K, Skiniotis, G. | | 登録日 | 2021-12-04 | | 公開日 | 2022-12-07 | | 最終更新日 | 2023-02-15 | | 実験手法 | ELECTRON MICROSCOPY (2.5 Å) | | 主引用文献 | Insights into distinct signaling profiles of the mu OR activated by diverse agonists.
Nat.Chem.Biol., 2022
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7T2H
 | | CryoEM structure of mu-opioid receptor - Gi protein complex bound to lofentanil (LFT) | | 分子名称: | 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, Guanine nucleotide-binding protein G(i) subunit alpha-1, ... | | 著者 | Seven, A.B, Qu, Q, Huang, W, Robertson, M.J, Kobilka, B.K, Skiniotis, G. | | 登録日 | 2021-12-04 | | 公開日 | 2022-12-07 | | 最終更新日 | 2022-12-14 | | 実験手法 | ELECTRON MICROSCOPY (3.2 Å) | | 主引用文献 | Insights into distinct signaling profiles of the mu OR activated by diverse agonists.
Nat.Chem.Biol., 2022
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