8FEC
 
 | | Structure of J-PKAc chimera complexed with Aplithianine derivative | | 分子名称: | 6-[(6P)-6-(4-bromo-1-methyl-1H-imidazol-5-yl)-2,3-dihydro-4H-1,4-thiazin-4-yl]-7H-purine, DnaJ homolog subfamily B member 1,cAMP-dependent protein kinase catalytic subunit alpha, cAMP-dependent protein kinase inhibitor alpha | | 著者 | Du, L, Wilson, B.A.P, Li, N, Martinez Fiesco, J.A, Dalilian, M, Wang, D, Smith, E.A, Wamiru, A, Goncharova, E.I, Zhang, P, O'Keefe, B.R. | | 登録日 | 2022-12-06 | | 公開日 | 2023-10-18 | | 最終更新日 | 2024-05-01 | | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | | 主引用文献 | Discovery and Synthesis of a Naturally Derived Protein Kinase Inhibitor that Selectively Inhibits Distinct Classes of Serine/Threonine Kinases.
J.Nat.Prod., 86, 2023
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8FE2
 | | Structure of J-PKAc chimera complexed with Aplithianine A | | 分子名称: | 6-[(6M)-6-(1-methyl-1H-imidazol-5-yl)-2,3-dihydro-4H-1,4-thiazin-4-yl]-9H-purine, DnaJ homolog subfamily B member 1, cAMP-dependent protein kinase catalytic subunit alpha, ... | | 著者 | Du, L, Wilson, B.A.P, Li, N, Dalilian, M, Wang, D, Martinez Fiesco, J.A, Smith, E.A, Wamiru, A, Goncharova, E.I, Zhang, P, O'Keefe, B.R. | | 登録日 | 2022-12-05 | | 公開日 | 2023-10-18 | | 最終更新日 | 2024-05-01 | | 実験手法 | X-RAY DIFFRACTION (2.34 Å) | | 主引用文献 | Discovery and Synthesis of a Naturally Derived Protein Kinase Inhibitor that Selectively Inhibits Distinct Classes of Serine/Threonine Kinases.
J.Nat.Prod., 86, 2023
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8FE5
 | | Structure of J-PKAc chimera complexed with Aplithianine B | | 分子名称: | 6-[(6P)-6-(1-methyl-1H-imidazol-5-yl)-2,3-dihydro-4H-1,4-thiazin-4-yl]-7,9-dihydro-8H-purin-8-one, DnaJ homolog subfamily B member 1,cAMP-dependent protein kinase catalytic subunit alpha, cAMP-dependent protein kinase inhibitor alpha | | 著者 | Du, L, Wilson, B.A.P, Li, N, Martinez Fiesco, J.A, Dalilian, M, Wang, D, Smith, E.A, Wamiru, A, Goncharova, E.I, Zhang, P, O'Keefe, B.R. | | 登録日 | 2022-12-05 | | 公開日 | 2023-10-18 | | 最終更新日 | 2024-05-01 | | 実験手法 | X-RAY DIFFRACTION (2.51 Å) | | 主引用文献 | Discovery and Synthesis of a Naturally Derived Protein Kinase Inhibitor that Selectively Inhibits Distinct Classes of Serine/Threonine Kinases.
J.Nat.Prod., 86, 2023
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3L9M
 | | Crystal structure of PKAB3 (pka triple mutant V123A, L173M, Q181K) with compound 18 | | 分子名称: | (2S)-N~1~-[5-(3-methyl-1H-indazol-5-yl)-1,3,4-thiadiazol-2-yl]-3-(4-methylphenyl)propane-1,2-diamine, cAMP-dependent protein kinase catalytic subunit alpha, cAMP-dependent protein kinase inhibitor alpha | | 著者 | Huang, X. | | 登録日 | 2010-01-05 | | 公開日 | 2011-01-19 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | | 主引用文献 | Azole-based inhibitors of AKT/PKB for the treatment of cancer.
Bioorg.Med.Chem.Lett., 20, 2010
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6N43
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3L9N
 | | crystal structure of PKAB3 (pka triple mutant V123A, L173M, Q181K) with compound 27 | | 分子名称: | (2S)-N~1~-[5-(1H-indazol-5-yl)-1,3,4-thiadiazol-2-yl]-3-(4-methylphenyl)propane-1,2-diamine, cAMP-dependent protein kinase catalytic subunit alpha, cAMP-dependent protein kinase inhibitor alpha | | 著者 | Huang, X. | | 登録日 | 2010-01-05 | | 公開日 | 2011-01-19 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Azole-based inhibitors of AKT/PKB for the treatment of cancer.
Bioorg.Med.Chem.Lett., 20, 2010
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8G59
 | | Cryo-EM structure of the TUG891 bound GPR120-Giq complex | | 分子名称: | 3-{4-[(4-fluoro-4'-methyl[1,1'-biphenyl]-2-yl)methoxy]phenyl}propanoic acid, Free fatty acid receptor 4, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | Mao, C, Xiao, P, Tao, X, Qin, J, He, Q, Zhang, C, Yu, X, Zhang, Y, Sun, J. | | 登録日 | 2023-02-12 | | 公開日 | 2023-03-08 | | 最終更新日 | 2023-04-19 | | 実験手法 | ELECTRON MICROSCOPY (2.64 Å) | | 主引用文献 | Unsaturated bond recognition leads to biased signal in a fatty acid receptor.
Science, 380, 2023
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6N42
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3L9L
 | | Crystal structure of pka with compound 36 | | 分子名称: | 5-[2-({(2S)-2-amino-3-[4-(trifluoromethyl)phenyl]propyl}amino)-1,3-thiazol-5-yl]-1,3-dihydro-2H-indol-2-one, cAMP-dependent protein kinase catalytic subunit alpha, cAMP-dependent protein kinase inhibitor alpha | | 著者 | Huang, X. | | 登録日 | 2010-01-05 | | 公開日 | 2011-01-19 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Azole-based inhibitors of AKT/PKB for the treatment of cancer.
Bioorg.Med.Chem.Lett., 20, 2010
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8FLR
 | | Human PTH1R in complex with PTHrP and Gs | | 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 | Cary, B.P, Belousoff, M.J, Piper, S.J, Wootten, D, Sexton, P.M. | | 登録日 | 2022-12-22 | | 公開日 | 2023-04-26 | | 最終更新日 | 2023-06-14 | | 実験手法 | ELECTRON MICROSCOPY (2.94 Å) | | 主引用文献 | Molecular insights into peptide agonist engagement with the PTH receptor.
Structure, 31, 2023
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8FLQ
 | | Human PTH1R in complex with PTH(1-34) and Gs | | 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 | Cary, B.P, Belousoff, M.J, Piper, S.J, Wootten, D, Sexton, P.M. | | 登録日 | 2022-12-22 | | 公開日 | 2023-04-26 | | 最終更新日 | 2023-06-14 | | 実験手法 | ELECTRON MICROSCOPY (2.55 Å) | | 主引用文献 | Molecular insights into peptide agonist engagement with the PTH receptor.
Structure, 31, 2023
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8FLS
 | | Human PTH1R in complex with Abaloparatide and Gs | | 分子名称: | Abaloparatide, 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 | Cary, B.P, Belousoff, M.J, Piper, S.J, Wootten, D, Sexton, P.M. | | 登録日 | 2022-12-22 | | 公開日 | 2023-04-26 | | 最終更新日 | 2023-06-14 | | 実験手法 | ELECTRON MICROSCOPY (3.09 Å) | | 主引用文献 | Molecular insights into peptide agonist engagement with the PTH receptor.
Structure, 31, 2023
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8FLU
 | | Human PTH1R in complex with LA-PTH and Gs | | 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 | Cary, B.P, Belousoff, M.J, Piper, S.J, Wootten, D, Sexton, P.M. | | 登録日 | 2022-12-22 | | 公開日 | 2023-04-26 | | 最終更新日 | 2023-06-14 | | 実験手法 | ELECTRON MICROSCOPY (2.76 Å) | | 主引用文献 | Molecular insights into peptide agonist engagement with the PTH receptor.
Structure, 31, 2023
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8FLT
 | | Human PTH1R in complex with M-PTH(1-14) and Gs | | 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 | Cary, B.P, Belousoff, M.J, Piper, S.J, Wootten, D, Sexton, P.M. | | 登録日 | 2022-12-22 | | 公開日 | 2023-04-26 | | 最終更新日 | 2023-06-14 | | 実験手法 | ELECTRON MICROSCOPY (3.03 Å) | | 主引用文献 | Molecular insights into peptide agonist engagement with the PTH receptor.
Structure, 31, 2023
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1M51
 | | PEPCK complex with a GTP-competitive inhibitor | | 分子名称: | 1,2-ETHANEDIOL, ACETATE ION, MANGANESE (II) ION, ... | | 著者 | Foley, L.H, Wang, P, Dunten, P, Wertheimer, S.J. | | 登録日 | 2002-07-06 | | 公開日 | 2003-09-30 | | 最終更新日 | 2024-02-14 | | 実験手法 | X-RAY DIFFRACTION (2.25 Å) | | 主引用文献 | X-ray Structures of two xanthine inhibitors bound to PEPCK and N-3 modifications of substituted 1,8-Dibenzylxanthines
Bioorg.Med.Chem.Lett., 13, 2003
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6NI3
 | | B2V2R-Gs protein subcomplex of a GPCR-G protein-beta-arrestin mega-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, Endolysin,Beta-2 adrenergic receptor chimera, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | Nguyen, A.H, Thomsen, A.R.B, Cahill, T.J, des Georges, A, Lefkowitz, R.J. | | 登録日 | 2018-12-26 | | 公開日 | 2019-11-20 | | 最終更新日 | 2019-12-18 | | 実験手法 | ELECTRON MICROSCOPY (3.8 Å) | | 主引用文献 | Structure of an endosomal signaling GPCR-G protein-beta-arrestin megacomplex.
Nat.Struct.Mol.Biol., 26, 2019
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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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6NO7
 | | Crystal Structure of the full-length wild-type PKA RIa Holoenzyme | | 分子名称: | ADENOSINE-5'-TRIPHOSPHATE, MAGNESIUM ION, cAMP-dependent protein kinase catalytic subunit alpha, ... | | 著者 | Lu, T, Wu, J, Taylor, S.S. | | 登録日 | 2019-01-15 | | 公開日 | 2019-07-24 | | 最終更新日 | 2023-10-11 | | 実験手法 | X-RAY DIFFRACTION (3.55 Å) | | 主引用文献 | Two PKA RI alpha holoenzyme states define ATP as an isoform-specific orthosteric inhibitor that competes with the allosteric activator, cAMP.
Proc.Natl.Acad.Sci.USA, 116, 2019
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1N1M
 | | Human Dipeptidyl Peptidase IV/CD26 in complex with an inhibitor | | 分子名称: | 2-AMINO-3-METHYL-1-PYRROLIDIN-1-YL-BUTAN-1-ONE, 2-acetamido-2-deoxy-alpha-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-alpha-D-glucopyranose-(1-4)-[alpha-L-fucopyranose-(1-6)]2-acetamido-2-deoxy-beta-D-glucopyranose, ... | | 著者 | Rasmussen, H.B, Branner, S, Wiberg, F.C, Wagtmann, N.R. | | 登録日 | 2002-10-18 | | 公開日 | 2002-12-27 | | 最終更新日 | 2020-07-29 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | Crystal structure of human dipeptidyl peptidase IV/CD26 in complex with a substrate analogue
Nat.Struct.Biol., 10, 2003
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3MOE
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3MOF
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3MOH
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1NHX
 | | PEPCK COMPLEX WITH A GTP-COMPETITIVE INHIBITOR | | 分子名称: | 1,2-ETHANEDIOL, MANGANESE (II) ION, N-{4-[1-(2-FLUOROBENZYL)-3-BUTYL-2,6-DIOXO-2,3,6,7-TETRAHYDRO-1H-PURIN-8-YLMETHYL]-PHENYL}-ACETAMIDE, ... | | 著者 | Foley, L.H, Wang, P, Dunten, P, Ramsey, G, Gubler, M.-L, Wertheimer, S.J. | | 登録日 | 2002-12-19 | | 公開日 | 2003-09-30 | | 最終更新日 | 2024-02-14 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | X-RAY STRUCTURES OF TWO XANTHINE INHIBITORS BOUND TO PEPCK and N-3 modifications of substituted 1,8-Dibenzylxanthines
Bioorg.Med.Chem.Lett., 13, 2003
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3MVJ
 | | Human cyclic AMP-dependent protein kinase PKA inhibitor complex | | 分子名称: | (3R)-1-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrrolidin-3-amine, cAMP-dependent protein kinase catalytic subunit alpha, cAMP-dependent protein kinase inhibitor alpha | | 著者 | Pandit, J, Vajdos, F. | | 登録日 | 2010-05-04 | | 公開日 | 2010-06-02 | | 最終更新日 | 2017-11-08 | | 実験手法 | X-RAY DIFFRACTION (2.49 Å) | | 主引用文献 | Design of selective, ATP-competitive inhibitors of Akt.
J.Med.Chem., 53, 2010
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3NJW
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