6VCB
 
 | | Cryo-EM structure of the Glucagon-like peptide-1 receptor in complex with G protein, GLP-1 peptide and a positive allosteric modulator | | 分子名称: | 1-[(1R)-1-(2,6-dichloro-3-methoxyphenyl)ethyl]-6-{2-[(2R)-piperidin-2-yl]phenyl}-1H-benzimidazole, Glucagon-like peptide 1, Glucagon-like peptide 1 receptor, ... | | 著者 | Sun, B, Feng, D, Bueno, A, Kobilka, B, Sloop, K. | | 登録日 | 2019-12-20 | | 公開日 | 2020-07-22 | | 最終更新日 | 2020-09-30 | | 実験手法 | ELECTRON MICROSCOPY (3.3 Å) | | 主引用文献 | Structural insights into probe-dependent positive allosterism of the GLP-1 receptor.
Nat.Chem.Biol., 16, 2020
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7LCI
 | | PF 06882961 bound to the glucagon-like peptide-1 receptor (GLP-1R):Gs complex | | 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, Johnson, R.M, Drulyte, I, Yu, L, Kotecha, A, Danev, R, Wootten, D, Zhang, X, Sexton, P.M. | | 登録日 | 2021-01-11 | | 公開日 | 2021-01-20 | | 最終更新日 | 2021-09-15 | | 実験手法 | ELECTRON MICROSCOPY (2.9 Å) | | 主引用文献 | Evolving cryo-EM structural approaches for GPCR drug discovery.
Structure, 29, 2021
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7LCK
 | | PF 06882961 bound to the glucagon-like peptide-1 receptor (GLP-1R) | | 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 | | 著者 | Belousoff, M.J, Johnson, R.M, Drulyte, I, Yu, L, Kotecha, A, Danev, R, Wootten, D, Zhang, X, Sexton, P.M. | | 登録日 | 2021-01-11 | | 公開日 | 2021-01-20 | | 最終更新日 | 2021-09-15 | | 実験手法 | ELECTRON MICROSCOPY (3.24 Å) | | 主引用文献 | Evolving cryo-EM structural approaches for GPCR drug discovery.
Structure, 29, 2021
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7LCJ
 | | PF 06882961 bound to the glucagon-like peptide-1 receptor (GLP-1R):Gs complex | | 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 | | 著者 | Belousoff, M.J, Johnson, R.M, Drulyte, I, Yu, L, Kotecha, A, Danev, R, Wootten, D, Zhang, X, Sexton, P.M. | | 登録日 | 2021-01-11 | | 公開日 | 2021-01-20 | | 最終更新日 | 2021-09-15 | | 実験手法 | ELECTRON MICROSCOPY (2.82 Å) | | 主引用文献 | Evolving cryo-EM structural approaches for GPCR drug discovery.
Structure, 29, 2021
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5VEX
 | | Structure of the human GLP-1 receptor complex with NNC0640 | | 分子名称: | 4-{[(4-cyclohexylphenyl){[3-(methylsulfonyl)phenyl]carbamoyl}amino]methyl}-N-(1H-tetrazol-5-yl)benzamide, Glucagon-like peptide 1 receptor, Endolysin chimera | | 著者 | Song, G, Yang, D, Wang, Y, Graaf, C.D, Zhou, Q, Jiang, S, Liu, K, Cai, X, Dai, A, Lin, G, Liu, D, Wu, F, Wu, Y, Zhao, S, Ye, L, Han, G.W, Lau, J, Wu, B, Hanson, M.A, Liu, Z.-J, Wang, M.-W, Stevens, R.C. | | 登録日 | 2017-04-05 | | 公開日 | 2017-05-17 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (3 Å) | | 主引用文献 | Human GLP-1 receptor transmembrane domain structure in complex with allosteric modulators.
Nature, 546, 2017
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5VEW
 | | Structure of the human GLP-1 receptor complex with PF-06372222 | | 分子名称: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, Glucagon-like peptide 1 receptor,Endolysin chimera, 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, Yang, D, Wang, Y, Graaf, C.D, Zhou, Q, Jiang, S, Liu, K, Cai, X, Dai, A, Lin, G, Liu, D, Wu, F, Wu, Y, Zhao, S, Ye, L, Han, G.W, Lau, J, Wu, B, Hanson, M.A, Liu, Z.-J, Wang, M.-W, Stevens, R.C. | | 登録日 | 2017-04-05 | | 公開日 | 2017-05-24 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | | 主引用文献 | Human GLP-1 receptor transmembrane domain structure in complex with allosteric modulators.
Nature, 546, 2017
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2M5P
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2M5Q
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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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6KJV
 | | Structure of thermal-stabilised(M9) human GLP-1 receptor transmembrane domain | | 分子名称: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 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 (2.8 Å) | | 主引用文献 | Mutagenesis facilitated crystallization of GLP-1R.
Iucrj, 6, 2019
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3CZF
 | | Crystal structure of HLA-B*2709 complexed with the glucagon receptor (GR) peptide (residues 412-420) | | 分子名称: | BETA-2-MICROGLOBULIN, GLUCAGON RECEPTOR PEPTIDE, GLYCEROL, ... | | 著者 | Loll, B, Fiorillo, M.T, Rueckert, C, Saenger, W, Sorrentino, R, Ziegler, A, Uchanska-Ziegler, B. | | 登録日 | 2008-04-29 | | 公開日 | 2009-04-07 | | 最終更新日 | 2023-08-30 | | 実験手法 | X-RAY DIFFRACTION (1.2 Å) | | 主引用文献 | Conformational Plasticity of HLA-B27 Molecules Correlates Inversely With Efficiency of Negative T Cell Selection.
Front Immunol, 11, 2020
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8TJT
 | | The Fab fragment of an anti-glucagon receptor (GCGR) antibody | | 分子名称: | anti-GCGR Fab heavy chain, anti-GCGR Fab light chain | | 著者 | Dai, J, Carter, P.J, Sudhamsu, J, Kung, J. | | 登録日 | 2023-07-24 | | 公開日 | 2024-02-14 | | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | | 主引用文献 | Variable domain mutational analysis to probe the molecular mechanisms of high viscosity of an IgG 1 antibody.
Mabs, 16, 2024
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8GJI
 | | De novo design of high-affinity protein binders to bioactive helical peptides | | 分子名称: | GCG binder, Glucagon | | 著者 | Torres, S.V, Leung, P.J.Y, Bera, A.K, Baker, D, Kang, A. | | 登録日 | 2023-03-15 | | 公開日 | 2024-01-10 | | 最終更新日 | 2024-02-14 | | 実験手法 | X-RAY DIFFRACTION (1.81 Å) | | 主引用文献 | De novo design of high-affinity binders of bioactive helical peptides.
Nature, 626, 2024
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6MQ3
 | | Structure of Cysteine-free Human Insulin-Degrading Enzyme in complex with Substrate-selective Macrocycle Inhibitor 63 | | 分子名称: | 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID, Insulin-degrading enzyme, {(8R,9S,10S)-9-(2',3'-dimethyl[1,1'-biphenyl]-4-yl)-6-[(1-methyl-1H-imidazol-2-yl)sulfonyl]-1,6-diazabicyclo[6.2.0]decan-10-yl}methanol | | 著者 | Tan, G.A, Seeliger, M.A, Welsh, A.J, Maianti, J.P, Liu, D.R. | | 登録日 | 2018-10-09 | | 公開日 | 2019-04-03 | | 最終更新日 | 2023-10-11 | | 実験手法 | X-RAY DIFFRACTION (3.569147 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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7RA3
 | | cryo-EM of human Gastric inhibitory polypeptide receptor GIPR bound to GIP | | 分子名称: | Gastric inhibitory polypeptide, Gastric inhibitory polypeptide receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | Sun, B, Kobilka, B.K, Sloop, K.W, Feng, D, Kobilka, T.S. | | 登録日 | 2021-06-29 | | 公開日 | 2022-04-13 | | 実験手法 | ELECTRON MICROSCOPY (3.24 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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7C2E
 | | GLP-1R-Gs complex structure with a small molecule full agonist | | 分子名称: | 2-[[4-[6-[(4-cyano-2-fluoranyl-phenyl)methoxy]pyridin-2-yl]-3,6-dihydro-2~{H}-pyridin-1-yl]methyl]-3-[[(2~{S})-oxetan-2-yl]methyl]imidazo[4,5-b]pyridine-5-carboxylic acid, Glucagon-like peptide 1 receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | Ma, H, Yuan, D.P, Huang, W, Wenge, Z, Xu, E. | | 登録日 | 2020-05-07 | | 公開日 | 2020-08-26 | | 最終更新日 | 2020-12-16 | | 実験手法 | ELECTRON MICROSCOPY (4.2 Å) | | 主引用文献 | Structural insights into the activation of GLP-1R by a small molecule agonist.
Cell Res., 30, 2020
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7RBT
 | | cryo-EM structure of human Gastric inhibitory polypeptide receptor GIPR bound to tirzepatide | | 分子名称: | 2-fluoro-4-[(1R)-6-methoxy-1-methyl-2-{(1S)-1-[4-(propan-2-yl)phenyl]ethyl}-1,2,3,4-tetrahydroisoquinolin-5-yl]-6-[(2-methylpropyl)amino]phenol, Gastric inhibitory polypeptide receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | Sun, B, Kobilka, B.K, Sloop, K.W, Feng, D, Kobilka, T.S. | | 登録日 | 2021-07-06 | | 公開日 | 2022-04-13 | | 実験手法 | ELECTRON MICROSCOPY (3.08 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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6BYZ
 | | Structure of Cysteine-free Human Insulin-Degrading Enzyme in complex with Substrate-selective Macrocyclic Inhibitor 37 | | 分子名称: | 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID, ALA-ALA-ALA, Insulin-degrading enzyme, ... | | 著者 | Tan, G.A, Seeliger, M.A, Maianti, J.P, Liu, D.R. | | 登録日 | 2017-12-21 | | 公開日 | 2019-04-03 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (2.95624852 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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2QKH
 | | Crystal structure of the extracellular domain of human GIP receptor in complex with the hormone GIP | | 分子名称: | Cyclic 2,3-di-O-methyl-alpha-D-glucopyranose-(1-4)-2-O-methyl-alpha-D-glucopyranose-(1-4)-2,6-di-O-methyl-alpha-D-glucopyranose-(1-4)-2-O-methyl-alpha-D-glucopyranose-(1-4)-alpha-D-glucopyranose-(1-4)-alpha-D-glucopyranose-(1-4)-3-O-methyl-alpha-D-glucopyranose, D(-)-TARTARIC ACID, Glucose-dependent insulinotropic polypeptide, ... | | 著者 | Parthier, C, Kleinschmidt, M, Neumann, P, Rudolph, R, Manhart, S, Schlenzig, D, Fanghanel, J, Rahfeld, J.-U, Demuth, H.-U, Stubbs, M.T. | | 登録日 | 2007-07-11 | | 公開日 | 2007-08-14 | | 最終更新日 | 2020-07-29 | | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | | 主引用文献 | Crystal structure of the incretin-bound extracellular domain of a G protein-coupled receptor
Proc.Natl.Acad.Sci.Usa, 104, 2007
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2RRI
 | | NMR structure of vasoactive intestinal peptide in DPC Micelle | | 分子名称: | Vasoactive intestinal peptide | | 著者 | Umetsu, Y, Tenno, T, Goda, N, Shirakawa, M, Ikegami, T, Hiroaki, H. | | 登録日 | 2010-12-21 | | 公開日 | 2011-04-06 | | 最終更新日 | 2024-05-15 | | 実験手法 | SOLUTION NMR | | 主引用文献 | Structural difference of vasoactive intestinal peptide in two distinct membrane-mimicking environments
Biochim.Biophys.Acta, 1814, 2011
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2RRH
 | | NMR structure of vasoactive intestinal peptide in Methanol | | 分子名称: | VIP peptides | | 著者 | Umetsu, Y, Tenno, T, Goda, N, Ikegami, T, Hiroaki, H. | | 登録日 | 2010-11-12 | | 公開日 | 2011-04-06 | | 最終更新日 | 2024-05-01 | | 実験手法 | SOLUTION NMR | | 主引用文献 | Structural difference of vasoactive intestinal peptide in two distinct membrane-mimicking environments.
Biochim.Biophys.Acta, 1814, 2011
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6LPB
 | | Cryo-EM structure of the human PAC1 receptor coupled to an engineered heterotrimeric G protein | | 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,Guanine nucleotide-binding protein G(s) subunit alpha isoforms short, ... | | 著者 | Kobayashi, K, Shihoya, W, Nishizawa, T, Nureki, O. | | 登録日 | 2020-01-09 | | 公開日 | 2020-03-11 | | 最終更新日 | 2020-03-25 | | 実験手法 | ELECTRON MICROSCOPY (3.9 Å) | | 主引用文献 | Cryo-EM structure of the human PAC1 receptor coupled to an engineered heterotrimeric G protein.
Nat.Struct.Mol.Biol., 27, 2020
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1U8E
 | | HUMAN DIPEPTIDYL PEPTIDASE IV/CD26 MUTANT Y547F | | 分子名称: | 2-acetamido-2-deoxy-alpha-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, ... | | 著者 | Bjelke, J.R, Christensen, J, Branner, S, Wagtmann, N, Olsen, C, Kanstrup, A.B, Rasmussen, H.B. | | 登録日 | 2004-08-05 | | 公開日 | 2004-08-17 | | 最終更新日 | 2021-10-20 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | Tyrosine 547 constitutes an essential part of the catalytic mechanism of dipeptidyl peptidase IV
J.Biol.Chem., 279, 2004
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2MJ9
 | | Designed Exendin-4 analogues | | 分子名称: | Exendin-4 | | 著者 | Rovo, P, Farkas, V, Straner, P, Szabo, M, Jermendy, A, Hegyi, O, Toth, G.K, Perczel, A. | | 登録日 | 2013-12-30 | | 公開日 | 2014-06-04 | | 最終更新日 | 2023-06-14 | | 実験手法 | SOLUTION NMR | | 主引用文献 | Rational design of alpha-helix-stabilized exendin-4 analogues.
Biochemistry, 53, 2014
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8WA3
 | | Cryo-EM structure of peptide free and Gs-coupled GIPR | | 分子名称: | Gastric inhibitory polypeptide receptor,Fusion protein, 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,O-antigen polymerase, ... | | 著者 | Cong, Z.T, Zhao, F.H, Li, Y, Luo, G, Zhou, Q.T, Yang, D.H, Wang, M.W. | | 登録日 | 2023-09-06 | | 公開日 | 2024-03-06 | | 実験手法 | ELECTRON MICROSCOPY (2.86 Å) | | 主引用文献 | Molecular features of the ligand-free GLP-1R, GCGR and GIPR in complex with G s proteins.
Cell Discov, 10, 2024
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