5UZ7
 
 | | Volta phase plate cryo-electron microscopy structure of a calcitonin receptor-heterotrimeric Gs protein complex | | 分子名称: | Calcitonin 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 | Liang, Y.L, Khoshouei, M, Radjainia, M, Zhang, Y, Glukhova, A, Tarrasch, J, Thal, D.M, Furness, S.G.B, Christopoulos, G, Coudrat, T, Danev, R, Baumeister, W, Miller, L.J, Christopoulos, A, Kobilka, B.K, Wootten, D, Skiniotis, G, Sexton, P.M. | | 登録日 | 2017-02-24 | | 公開日 | 2017-05-03 | | 最終更新日 | 2018-07-18 | | 実験手法 | ELECTRON MICROSCOPY (4.1 Å) | | 主引用文献 | Phase-plate cryo-EM structure of a class B GPCR-G-protein complex.
Nature, 546, 2017
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7LD3
 | | Cryo-EM structure of the human adenosine A1 receptor-Gi2-protein complex bound to its endogenous agonist and an allosteric ligand | | 分子名称: | ADENOSINE, Chimera protein of Muscarinic acetylcholine receptor M4 and Adenosine receptor A1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | Draper-Joyce, C.J, Danev, R, Thal, D.M, Christopoulos, A, Glukhova, A. | | 登録日 | 2021-01-12 | | 公開日 | 2021-09-08 | | 最終更新日 | 2021-10-13 | | 実験手法 | ELECTRON MICROSCOPY (3.2 Å) | | 主引用文献 | Positive allosteric mechanisms of adenosine A 1 receptor-mediated analgesia.
Nature, 597, 2021
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7LD4
 | | Cryo-EM structure of the human adenosine A1 receptor-Gi2-protein complex bound to its endogenous agonist | | 分子名称: | ADENOSINE, Chimera protein of Muscarinic acetylcholine receptor M4 and Adenosine receptor A1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | Draper-Joyce, C.J, Danev, R, Thal, D.M, Christopoulos, A, Glukhova, A. | | 登録日 | 2021-01-12 | | 公開日 | 2021-09-08 | | 最終更新日 | 2021-10-13 | | 実験手法 | ELECTRON MICROSCOPY (3.3 Å) | | 主引用文献 | Positive allosteric mechanisms of adenosine A 1 receptor-mediated analgesia.
Nature, 597, 2021
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6NIY
 | | A high-resolution cryo-electron microscopy structure of a calcitonin receptor-heterotrimeric Gs protein complex | | 分子名称: | Calcitonin, Calcitonin receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | dal Maso, E, Glukhova, A, Zhu, Y, Garcia-Nafria, J, Tate, C.G, Atanasio, S, Reynolds, C.A, Ramirez-Aportela, E, Carazo, J.-M, Hick, C.A, Furness, S.G.B, Hay, D.L, Liang, Y.-L, Miller, L.J, Christopoulos, A, Wang, M.-W, Wootten, D, Sexton, P.M. | | 登録日 | 2019-01-02 | | 公開日 | 2019-01-23 | | 最終更新日 | 2020-04-08 | | 実験手法 | ELECTRON MICROSCOPY (3.34 Å) | | 主引用文献 | The Molecular Control of Calcitonin Receptor Signaling.
Acs Pharmacol Transl Sci, 2, 2019
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6B3J
 | | 3.3 angstrom phase-plate cryo-EM structure of a biased agonist-bound human GLP-1 receptor-Gs complex | | 分子名称: | Exendin-P5, Glucagon-like peptide 1 receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | Liang, Y.L, Khoshouei, M, Glukhova, A, Furness, S.G.B, Koole, C, Zhao, P, Clydesdale, L, Thal, D.M, Radjainia, M, Danev, R, Baumeister, W, Wang, M.W, Miller, L.J, Christopoulos, A, Sexton, P.M, Wootten, D. | | 登録日 | 2017-09-22 | | 公開日 | 2018-02-21 | | 最終更新日 | 2020-01-15 | | 実験手法 | ELECTRON MICROSCOPY (3.3 Å) | | 主引用文献 | Phase-plate cryo-EM structure of a biased agonist-bound human GLP-1 receptor-Gs complex.
Nature, 555, 2018
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5DSG
 | | Structure of the M4 muscarinic acetylcholine receptor (M4-mT4L) bound to tiotropium | | 分子名称: | (1R,2R,4S,5S,7S)-7-{[hydroxy(dithiophen-2-yl)acetyl]oxy}-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.0~2,4~]nonane, (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 1-(2-METHOXY-ETHOXY)-2-{2-[2-(2-METHOXY-ETHOXY]-ETHOXY}-ETHANE, ... | | 著者 | Thal, D.M, Kobilka, B.K, Sexton, P.M, Christopoulos, A. | | 登録日 | 2015-09-17 | | 公開日 | 2016-03-16 | | 最終更新日 | 2024-03-13 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | Crystal structures of the M1 and M4 muscarinic acetylcholine receptors.
Nature, 531, 2016
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2MPM
 | | Structural Basis of Receptor Sulfotyrosine Recognition by a CC Chemokine: the N-terminal Region of CCR3 Bound to CCL11/Eotaxin-1 | | 分子名称: | CCR3, Eotaxin | | 著者 | Millard, C.J, Ludeman, J.P, Canals, M, Bridgford, J.L, Hinds, M.G, Clayton, D.J, Christopoulos, A, Payne, R.J, Stone, M.J. | | 登録日 | 2014-05-26 | | 公開日 | 2014-12-10 | | 実験手法 | SOLUTION NMR | | 主引用文献 | Structural Basis of Receptor Sulfotyrosine Recognition by a CC Chemokine: The N-Terminal Region of CCR3 Bound to CCL11/Eotaxin-1.
Structure, 22, 2014
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4MQS
 | | Structure of active human M2 muscarinic acetylcholine receptor bound to the agonist iperoxo | | 分子名称: | 4-(4,5-dihydro-1,2-oxazol-3-yloxy)-N,N,N-trimethylbut-2-yn-1-aminium, Muscarinic acetylcholine receptor M2, Nanobody 9-8 | | 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 (3.5 Å) | | 主引用文献 | Activation and allosteric modulation of a muscarinic acetylcholine receptor.
Nature, 504, 2013
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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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6E3Y
 | | Cryo-EM structure of the active, Gs-protein complexed, human CGRP receptor | | 分子名称: | Calcitonin gene-related peptide 1, Calcitonin gene-related peptide type 1 receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | Liang, Y.L, Khoshouei, M, Deganutti, G, Glukhova, A, Koole, C, Peat, T.S, Radjainia, M, Plitzko, J.M, Baumeister, W, Miller, L.J, Hay, D.L, Christopoulos, A, Reynolds, C.A, Wootten, D, Sexton, P.M. | | 登録日 | 2018-07-16 | | 公開日 | 2018-09-19 | | 最終更新日 | 2020-01-15 | | 実験手法 | ELECTRON MICROSCOPY (3.3 Å) | | 主引用文献 | Cryo-EM structure of the active, Gs-protein complexed, human CGRP receptor.
Nature, 561, 2018
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6D9H
 | | Cryo-EM structure of the human adenosine A1 receptor-Gi2-protein complex bound to its endogenous agonist | | 分子名称: | ADENOSINE, Chimera protein of Muscarinic acetylcholine receptor M4 and Adenosine receptor A1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | Draper-Joyce, C.J, Khoshouei, M, Thal, D.M, Liang, Y.-L, Nguyen, A.T.N, Furness, S.G.B, Venugopal, H, Baltos, J, Plitzko, J.M, Danev, R, Baumeister, W, May, L.T, Wootten, D, Sexton, P, Glukhova, A, Christopoulos, A. | | 登録日 | 2018-04-29 | | 公開日 | 2018-06-20 | | 最終更新日 | 2018-07-11 | | 実験手法 | ELECTRON MICROSCOPY (3.6 Å) | | 主引用文献 | Structure of the adenosine-bound human adenosine A1receptor-Gicomplex.
Nature, 558, 2018
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5UEN
 | | Crystal structure of the human adenosine A1 receptor A1AR-bRIL in complex with the covalent antagonist DU172 at 3.2A resolution | | 分子名称: | 4-{[3-(8-cyclohexyl-2,6-dioxo-1-propyl-1,2,6,7-tetrahydro-3H-purin-3-yl)propyl]carbamoyl}benzene-1-sulfonyl fluoride, Adenosine receptor A1,Soluble cytochrome b562,Adenosine receptor A1, OLEIC ACID | | 著者 | Glukhova, A, Thal, D.M, Nguyen, A.T, Vecchio, E.A, Jorg, M, Scammells, P.J, May, L.T, Sexton, P.M, Christopoulos, A. | | 登録日 | 2017-01-03 | | 公開日 | 2017-03-01 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (3.2 Å) | | 主引用文献 | Structure of the Adenosine A1 Receptor Reveals the Basis for Subtype Selectivity.
Cell, 168, 2017
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6OL9
 | | Structure of the M5 muscarinic acetylcholine receptor (M5-T4L) bound to tiotropium | | 分子名称: | (1R,2R,4S,5S,7S)-7-{[hydroxy(dithiophen-2-yl)acetyl]oxy}-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.0~2,4~]nonane, (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 3,6,9,12,15,18-HEXAOXAICOSANE-1,20-DIOL, ... | | 著者 | Vuckovic, Z, Christopoulos, A, Thal, D.M. | | 登録日 | 2019-04-16 | | 公開日 | 2019-12-11 | | 最終更新日 | 2023-10-11 | | 実験手法 | X-RAY DIFFRACTION (2.541 Å) | | 主引用文献 | Crystal structure of the M5muscarinic acetylcholine receptor.
Proc.Natl.Acad.Sci.USA, 116, 2019
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9BKK
 | | Cholecystokinin 1 receptor (CCK1R) sterol 7M mutant, Gq chimera (mGsqi) complex | | 分子名称: | Cholecystokinin receptor type A, Cholecystokinin-8, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | Harikumar, K.G, Zhao, P, Cary, B.P, Xu, X, Desai, A.J, Mobbs, J.I, Toufaily, C, Furness, S.G.B, Christopoulos, A, Belousoff, M.J, Wootten, D, Sexton, P.M, Miller, L.J. | | 登録日 | 2024-04-29 | | 公開日 | 2024-05-22 | | 実験手法 | ELECTRON MICROSCOPY (2.51 Å) | | 主引用文献 | Cholesterol-dependent dynamic changes in the conformation of the type 1 cholecystokinin receptor affect ligand binding and G protein coupling
To Be Published
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9BKJ
 | | Cholecystokinin 1 receptor (CCK1R) Y140A mutant, Gq chimera (mGsqi) complex | | 分子名称: | AMINO GROUP, Cholecystokinin receptor type A, Cholecystokinin-8, ... | | 著者 | Cary, B.P, Harikumar, K.G, Zhao, P, Desai, A.J, Mobbs, J.M, Toufaily, C, Furness, S.G.B, Christopoulos, A, Belousoff, M.J, Wootten, D, Sexton, P.M, Miller, L.J. | | 登録日 | 2024-04-29 | | 公開日 | 2024-05-22 | | 実験手法 | ELECTRON MICROSCOPY (2.59 Å) | | 主引用文献 | Cholesterol-dependent dynamic changes in the conformation of the type 1 cholecystokinin receptor affect ligand binding and G protein coupling
To Be Published
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8FX5
 | | Human M4 muscarinic acetylcholine receptor complex with Gi1 and xanomeline | | 分子名称: | Antibody fragment scFv16, 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 | Vuckovic, Z, Mobbs, J.I, Glukhova, A, Sexton, P.M, Danev, R, Thal, D.M. | | 登録日 | 2023-01-23 | | 公開日 | 2023-09-13 | | 実験手法 | ELECTRON MICROSCOPY (2.45 Å) | | 主引用文献 | Xanomeline displays concomitant orthosteric and allosteric binding modes at the M 4 mAChR.
Nat Commun, 14, 2023
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7MBX
 | | Human Cholecystokinin 1 receptor (CCK1R) Gs complex | | 分子名称: | CHOLESTEROL HEMISUCCINATE, Cholecystokinin receptor type A, Cholecystokinin-8, ... | | 著者 | Mobbs, J.I, Belousoff, M.J, Danev, R, Thal, D.M, Sexton, P.M. | | 登録日 | 2021-04-01 | | 公開日 | 2021-05-26 | | 最終更新日 | 2021-07-14 | | 実験手法 | ELECTRON MICROSCOPY (1.95 Å) | | 主引用文献 | Structures of the human cholecystokinin 1 (CCK1) receptor bound to Gs and Gq mimetic proteins provide insight into mechanisms of G protein selectivity.
Plos Biol., 19, 2021
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7MBY
 | | Human Cholecystokinin 1 receptor (CCK1R) Gq chimera (mGsqi) complex | | 分子名称: | CHOLESTEROL HEMISUCCINATE, Cholecystokinin receptor type A, Cholecystokinin-8, ... | | 著者 | Mobbs, J.I, Belousoff, M.J, Danev, R, Thal, D.M, Sexton, P.M. | | 登録日 | 2021-04-01 | | 公開日 | 2021-05-26 | | 最終更新日 | 2021-07-14 | | 実験手法 | ELECTRON MICROSCOPY (2.44 Å) | | 主引用文献 | Structures of the human cholecystokinin 1 (CCK1) receptor bound to Gs and Gq mimetic proteins provide insight into mechanisms of G protein selectivity.
Plos Biol., 19, 2021
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6P9X
 | | CRF1 Receptor Gs GPCR protein complex with CRF1 peptide | | 分子名称: | Corticoliberin, Corticotropin-releasing factor receptor 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | Belousoff, M.J, Liang, Y.L, Sexton, P, Danev, R. | | 登録日 | 2019-06-10 | | 公開日 | 2020-02-05 | | 最終更新日 | 2020-02-19 | | 実験手法 | ELECTRON MICROSCOPY (2.91 Å) | | 主引用文献 | Toward a Structural Understanding of Class B GPCR Peptide Binding and Activation.
Mol.Cell, 77, 2020
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6P9Y
 | | PAC1 GPCR Receptor 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(s) subunit alpha isoforms short, ... | | 著者 | Belousoff, M.J, Liang, Y.L, Sexton, P, Danev, R. | | 登録日 | 2019-06-10 | | 公開日 | 2020-02-05 | | 最終更新日 | 2020-02-19 | | 実験手法 | ELECTRON MICROSCOPY (3.01 Å) | | 主引用文献 | Toward a Structural Understanding of Class B GPCR Peptide Binding and Activation.
Mol.Cell, 77, 2020
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6X19
 | | Non peptide agonist CHU-128, bound to Glucagon-Like peptide-1 (GLP-1) Receptor | | 分子名称: | 3-{(1S)-1-[5-(2,2-dimethylmorpholin-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]butyl}-1,2,4-oxadiazol-5(4H)-one, Glucagon-like peptide 1 receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | Belousoff, M.J, Zhang, X, Danev, R. | | 登録日 | 2020-05-18 | | 公開日 | 2020-09-09 | | 最終更新日 | 2020-11-18 | | 実験手法 | ELECTRON MICROSCOPY (2.1 Å) | | 主引用文献 | Differential GLP-1R Binding and Activation by Peptide and Non-peptide Agonists.
Mol.Cell, 80, 2020
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6X18
 | | GLP-1 peptide hormone bound to Glucagon-Like peptide-1 (GLP-1) Receptor | | 分子名称: | Glucagon, Glucagon-like peptide 1 receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | Belousoff, M.J, Zhang, X, Danev, R. | | 登録日 | 2020-05-18 | | 公開日 | 2020-09-09 | | 最終更新日 | 2020-11-18 | | 実験手法 | ELECTRON MICROSCOPY (2.1 Å) | | 主引用文献 | Differential GLP-1R Binding and Activation by Peptide and Non-peptide Agonists.
Mol.Cell, 80, 2020
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6X1A
 | | Non peptide agonist PF-06882961, bound to Glucagon-Like peptide-1 (GLP-1) Receptor | | 分子名称: | 2-[(4-{6-[(4-cyano-2-fluorophenyl)methoxy]pyridin-2-yl}piperidin-1-yl)methyl]-1-{[(2S)-oxetan-2-yl]methyl}-1H-benzimidazole-6-carboxylic acid, Glucagon-like peptide 1 receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | Belousoff, M.J, Zhang, X, Danev, R. | | 登録日 | 2020-05-18 | | 公開日 | 2020-09-09 | | 最終更新日 | 2020-11-18 | | 実験手法 | ELECTRON MICROSCOPY (2.5 Å) | | 主引用文献 | Differential GLP-1R Binding and Activation by Peptide and Non-peptide Agonists.
Mol.Cell, 80, 2020
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7LLL
 | | Exendin-4-bound Glucagon-Like Peptide-1 (GLP-1) Receptor in complex with Gs protein | | 分子名称: | Exendin-4, Glucagon-like peptide 1 receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | Wootten, D, Sexton, P.M, Belousoff, M.J, Danev, R, Zhang, X, Khoshouei, M, Venugopal, H. | | 登録日 | 2021-02-04 | | 公開日 | 2022-01-12 | | 最終更新日 | 2022-01-26 | | 実験手法 | ELECTRON MICROSCOPY (3.7 Å) | | 主引用文献 | Dynamics of GLP-1R peptide agonist engagement are correlated with kinetics of G protein activation.
Nat Commun, 13, 2022
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7LLY
 | | Oxyntomodulin-bound Glucagon-Like Peptide-1 (GLP-1) Receptor in complex with Gs protein | | 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 | Wootten, D, Sexton, P.M, Belousoff, M.J, Danev, R, Zhang, X, Khoshouei, M, Venugopal, H. | | 登録日 | 2021-02-04 | | 公開日 | 2022-01-12 | | 最終更新日 | 2022-01-26 | | 実験手法 | ELECTRON MICROSCOPY (3.3 Å) | | 主引用文献 | Dynamics of GLP-1R peptide agonist engagement are correlated with kinetics of G protein activation.
Nat Commun, 13, 2022
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