1DQD
| CRYSTAL STRUCTURE OF FAB HGR-2 F6, A COMPETITIVE ANTAGONIST OF THE GLUCAGON RECEPTOR | 分子名称: | FAB HGR-2 F6 | 著者 | Wright, L.M, Brzozowski, A.M, Hubbard, R.E, Pike, A.C.W, Roberts, S.M, Skovgaard, R.N, Svendsen, I, Vissing, H, Bywater, R.P. | 登録日 | 2000-01-04 | 公開日 | 2000-05-10 | 最終更新日 | 2011-07-13 | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | 主引用文献 | Structure of Fab hGR-2 F6, a competitive antagonist of the glucagon receptor. Acta Crystallogr.,Sect.D, 56, 2000
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7S15
| GLP-1 receptor bound with Pfizer small molecule agonist | 分子名称: | 2-[(4-{6-[(2,4-difluorophenyl)methoxy]pyridin-2-yl}piperidin-1-yl)methyl]-1-[(1-ethyl-1H-imidazol-5-yl)methyl]-1H-benzimidazole-6-carboxylic acid, Glucagon-like peptide 1 receptor | 著者 | Liu, Y, Dias, J.M, Han, S. | 登録日 | 2021-09-01 | 公開日 | 2022-06-08 | 最終更新日 | 2022-07-06 | 実験手法 | ELECTRON MICROSCOPY (3.8 Å) | 主引用文献 | A Small-Molecule Oral Agonist of the Human Glucagon-like Peptide-1 Receptor. J.Med.Chem., 65, 2022
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6GDZ
| exendin-4 based dual GLP-1/glucagon receptor agonist | 分子名称: | (2~{S})-2-[[(4~{S})-4-(hexadecanoylamino)-5-oxidanyl-5-oxidanylidene-pentanoyl]amino]pentanedioic acid, Exendin-4 | 著者 | Evers, A, Kurz, M. | 登録日 | 2018-04-25 | 公開日 | 2018-06-20 | 最終更新日 | 2019-05-08 | 実験手法 | SOLUTION NMR | 主引用文献 | Dual Glucagon-like Peptide 1 (GLP-1)/Glucagon Receptor Agonists Specifically Optimized for Multidose Formulations. J. Med. Chem., 61, 2018
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7DUQ
| Cryo-EM structure of the compound 2 and GLP-1-bound human GLP-1 receptor-Gs complex | 分子名称: | CHOLESTEROL, Glucagon-like peptide 1, Glucagon-like peptide 1 receptor, ... | 著者 | Cong, Z, Chen, L, Ma, H, Zhou, Q, Zou, X, Ye, C, Dai, A, Liu, Q, Huang, W, Sun, X, Wang, X, Xu, P, Zhao, L, Xia, T, Zhong, W, Yang, D, Xu, H.E, Zhang, Y, Wang, M. | 登録日 | 2021-01-11 | 公開日 | 2021-07-14 | 実験手法 | ELECTRON MICROSCOPY (2.5 Å) | 主引用文献 | Molecular insights into ago-allosteric modulation of the human glucagon-like peptide-1 receptor. Nat Commun, 12, 2021
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4ZGM
| Crystal structure of Semaglutide peptide backbone in complex with the GLP-1 receptor extracellular domain | 分子名称: | 3,6,9,12,15,18-hexaoxahexacosan-1-ol, Glucagon-like peptide 1 receptor, Semaglutide peptide backbone; 8Aib,34R-GLP-1(7-37)-OH | 著者 | Reedtz-Runge, S. | 登録日 | 2015-04-23 | 公開日 | 2015-09-09 | 最終更新日 | 2024-01-10 | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | 主引用文献 | Discovery of the Once-Weekly Glucagon-Like Peptide-1 (GLP-1) Analogue Semaglutide. J.Med.Chem., 58, 2015
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7DUR
| Cryo-EM structure of the compound 2-bound human GLP-1 receptor-Gs complex | 分子名称: | CHOLESTEROL, Glucagon-like peptide 1 receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | 著者 | Cong, Z, Chen, L, Ma, H, Zhou, Q, Zou, X, Ye, C, Dai, A, Liu, Q, Huang, W, Sun, X, Wang, X, Xu, P, Zhao, L, Xia, T, Zhong, W, Yang, D, Xu, H.E, Zhang, Y, Wang, M. | 登録日 | 2021-01-11 | 公開日 | 2021-08-11 | 実験手法 | ELECTRON MICROSCOPY (3.3 Å) | 主引用文献 | Molecular insights into ago-allosteric modulation of the human glucagon-like peptide-1 receptor. Nat Commun, 12, 2021
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7E14
| Compound2_GLP-1R_OWL833_Gs complex structure | 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, CHOLESTEROL, G protein, ... | 著者 | Cong, Z.T, Chen, L.N, Ma, H.L, Yang, D.H, Xu, H.E, Zhang, Y, Wang, M.W. | 登録日 | 2021-01-30 | 公開日 | 2021-07-07 | 最終更新日 | 2024-03-27 | 実験手法 | ELECTRON MICROSCOPY (2.9 Å) | 主引用文献 | Molecular insights into ago-allosteric modulation of the human glucagon-like peptide-1 receptor. Nat Commun, 12, 2021
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5NIQ
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6ORV
| Non-peptide agonist (TT-OAD2) bound to the Glucagon-Like peptide-1 (GLP-1) Receptor | 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 | Belousoff, M.J, Liang, Y.L, Danev, R. | 登録日 | 2019-05-01 | 公開日 | 2020-01-08 | 最終更新日 | 2020-01-29 | 実験手法 | ELECTRON MICROSCOPY (3 Å) | 主引用文献 | Activation of the GLP-1 receptor by a non-peptidic agonist. Nature, 577, 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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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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6WPW
| GCGR-Gs signaling complex bound to a designed glucagon derivative | 分子名称: | Glucagon derivative ZP3780, Glucagon receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | 著者 | Hilger, D, Krishna Kumar, K, Hu, H, Mathiesen, J.M, Skiniotis, G, Kobilka, B.K. | 登録日 | 2020-04-28 | 公開日 | 2020-08-12 | 実験手法 | ELECTRON MICROSCOPY (3.1 Å) | 主引用文献 | Structural insights into differences in G protein activation by family A and family B GPCRs. Science, 369, 2020
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7KI1
| Taspoglutide-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 | Zhang, X, Belousoff, M.J, Danev, R, Sexton, P.M, Wootten, D. | 登録日 | 2020-10-22 | 公開日 | 2021-08-04 | 実験手法 | ELECTRON MICROSCOPY (2.5 Å) | 主引用文献 | Structure and dynamics of semaglutide- and taspoglutide-bound GLP-1R-Gs complexes. Cell Rep, 36, 2021
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7RGP
| cryo-EM of human Glucagon-like peptide 1 receptor GLP-1R bound to tirzepatide | 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 | 2021-07-15 | 公開日 | 2022-04-13 | 実験手法 | ELECTRON MICROSCOPY (2.9 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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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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7S3I
| Ex4-D-Ala bound to the glucagon-like peptide-1 receptor/g protein complex (conformer 2) | 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 | Belousoff, M.J, Piper, S.J, Danev, R. | 登録日 | 2021-09-07 | 公開日 | 2022-01-05 | 最終更新日 | 2022-03-16 | 実験手法 | ELECTRON MICROSCOPY (2.51 Å) | 主引用文献 | Structural and functional diversity among agonist-bound states of the GLP-1 receptor. Nat.Chem.Biol., 18, 2022
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2NAV
| NMR solution structure of Ex-4[1-16]/pl14a | 分子名称: | Exendin-4, Alpha/kappa-conotoxin pl14a chimera | 著者 | Schroeder, C.I, Swedberg, J.E, Craik, D.J. | 登録日 | 2016-01-11 | 公開日 | 2016-05-04 | 最終更新日 | 2016-08-17 | 実験手法 | SOLUTION NMR | 主引用文献 | Truncated Glucagon-like Peptide-1 and Exendin-4 alpha-Conotoxin pl14a Peptide Chimeras Maintain Potency and alpha-Helicity and Reveal Interactions Vital for cAMP Signaling in Vitro. J.Biol.Chem., 291, 2016
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2NAW
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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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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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7KI0
| Semaglutide-bound Glucagon-Like Peptide-1 (GLP-1) Receptor in Complex with Gs protein | 分子名称: | 17-amino-10-oxo-3,6,12,15-tetraoxa-9-azaheptadecan-1-oic acid, Glucagon-like peptide 1 receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | 著者 | Zhang, X, Belousoff, M.J, Danev, R, Sexton, P.M, Wootten, D. | 登録日 | 2020-10-22 | 公開日 | 2021-08-04 | 実験手法 | ELECTRON MICROSCOPY (2.5 Å) | 主引用文献 | Structure and dynamics of semaglutide- and taspoglutide-bound GLP-1R-Gs complexes. Cell Rep, 36, 2021
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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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7S1M
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6EDS
| Structure of Cysteine-free Human Insulin-Degrading Enzyme in complex with Glucagon and Substrate-selective Macrocyclic Inhibitor 63 | 分子名称: | 1,4-DIETHYLENE DIOXIDE, 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID, DI(HYDROXYETHYL)ETHER, ... | 著者 | Tan, G.A, Seeliger, M.A, Maianti, J.P, Liu, D.R, Welsh, A.J. | 登録日 | 2018-08-10 | 公開日 | 2019-04-03 | 最終更新日 | 2023-10-11 | 実験手法 | X-RAY DIFFRACTION (3.18071723 Å) | 主引用文献 | Substrate-selective inhibitors that reprogram the activity of insulin-degrading enzyme. Nat.Chem.Biol., 15, 2019
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8JIS
| Cryo-EM structure of the GLP-1R/GCGR dual agonist peptide15-bound human GLP-1R-Gs complex | 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 | Yang, L, Zhou, Q.T, Dai, A.T, Zhao, F.H, Chang, R.L, Ying, T.L, Wu, B.L, Yang, D.H, Wang, M.W, Cong, Z.T. | 登録日 | 2023-05-27 | 公開日 | 2023-11-08 | 実験手法 | ELECTRON MICROSCOPY (2.46 Å) | 主引用文献 | Structural analysis of the dual agonism at GLP-1R and GCGR. Proc.Natl.Acad.Sci.USA, 120, 2023
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