5KQ5
 
 | | AMPK bound to allosteric activator | | 分子名称: | 5'-AMP-activated protein kinase catalytic subunit alpha-1, 5'-AMP-activated protein kinase subunit beta-1, 5'-AMP-activated protein kinase subunit gamma-1, ... | | 著者 | Calabrese, M.F, Kurumbail, R.G. | | 登録日 | 2016-07-05 | | 公開日 | 2016-08-17 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (3.41 Å) | | 主引用文献 | Discovery and Preclinical Characterization of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy.
J.Med.Chem., 59, 2016
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5ISO
 | | STRUCTURE OF FULL LENGTH HUMAN AMPK (NON-PHOSPHORYLATED AT T-LOOP) IN COMPLEX WITH A SMALL MOLECULE ACTIVATOR, A BENZIMIDAZOLE DERIVATIVE (991) | | 分子名称: | 5'-AMP-activated protein kinase catalytic subunit alpha-2, 5'-AMP-activated protein kinase subunit beta-1, 5'-AMP-activated protein kinase subunit gamma-1, ... | | 著者 | Xiao, B, Hubbard, J.A, Gamblin, S.J. | | 登録日 | 2016-03-15 | | 公開日 | 2017-03-29 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (2.63 Å) | | 主引用文献 | STRUCTURE OF FULL LENGTH HUMAN AMPK (NON-PHOSPHORYLATED AT T-LOOP) IN COMPLEX WITH A SMALL MOLECULE ACTIVATOR, A BENZIMIDAZOLE DERIVATIVE (991)
To Be Published
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4ZHX
 | | Novel binding site for allosteric activation of AMPK | | 分子名称: | (5S,6R,7R,9R,13cR,14R,16aS)-6-methoxy-5-methyl-7-(methylamino)-6,7,8,9,14,15,16,16a-octahydro-5H,13cH-5,9-epoxy-4b,9a,1 5-triazadibenzo[b,h]cyclonona[1,2,3,4-jkl]cyclopenta[e]-as-indacen-14-ol, 3-[4-(2-hydroxyphenyl)phenyl]-4-oxidanyl-6-oxidanylidene-7H-thieno[2,3-b]pyridine-5-carbonitrile, 5'-AMP-activated protein kinase catalytic subunit alpha-2, ... | | 著者 | Langendorf, C.G, Ngoei, K.R, Issa, S.M.A, Ling, N, Gorman, M.A, Parker, M.W, Sakamoto, K, Scott, J.W, Oakhill, J.S, Kemp, B.E. | | 登録日 | 2015-04-27 | | 公開日 | 2016-03-09 | | 最終更新日 | 2023-09-27 | | 実験手法 | X-RAY DIFFRACTION (2.99 Å) | | 主引用文献 | Structural basis of allosteric and synergistic activation of AMPK by furan-2-phosphonic derivative C2 binding.
Nat Commun, 7, 2016
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5EZV
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4QFG
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4EAG
 | | Co-crystal structure of an chimeric AMPK core with ATP | | 分子名称: | 5'-AMP-activated protein kinase subunit beta-1, 5'-AMP-activated protein kinase subunit gamma-1, ADENOSINE-5'-TRIPHOSPHATE, ... | | 著者 | Chen, L, Wang, J, Zhang, Y.-Y, Yan, S.F, Neumann, D, Schlattner, U, Wang, Z.-X, Wu, J.-W. | | 登録日 | 2012-03-22 | | 公開日 | 2012-06-06 | | 最終更新日 | 2023-11-08 | | 実験手法 | X-RAY DIFFRACTION (2.701 Å) | | 主引用文献 | AMP-activated protein kinase undergoes nucleotide-dependent conformational changes
Nat.Struct.Mol.Biol., 19, 2012
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7M74
 | | ATP-bound AMP-activated protein kinase | | 分子名称: | 5'-AMP-activated protein kinase catalytic subunit alpha-1, 5'-AMP-activated protein kinase subunit beta-2, 5'-AMP-activated protein kinase subunit gamma-1, ... | | 著者 | Yan, Y, Mukherjee, S, Harikumar, K.G, Strutzenberg, T, Zhou, X.E, Powell, S.K, Xu, T, Sheldon, R, Lamp, J, Brunzelle, J.S, Radziwon, K, Ellis, A, Novick, S.J, Vega, I.E, Jones, R, Miller, L.J, Xu, H.E, Griffin, P.R, Kossiakoff, A.A, Melcher, K. | | 登録日 | 2021-03-26 | | 公開日 | 2021-12-15 | | 最終更新日 | 2021-12-22 | | 実験手法 | ELECTRON MICROSCOPY (3.93 Å) | | 主引用文献 | Structure of an AMPK complex in an inactive, ATP-bound state.
Science, 373, 2021
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4EAL
 | | Co-crystal of AMPK core with ATP soaked with AMP | | 分子名称: | 5'-AMP-activated protein kinase catalytic subunit alpha-1, 5'-AMP-activated protein kinase subunit beta-1, 5'-AMP-activated protein kinase subunit gamma-1, ... | | 著者 | Chen, L, Wang, J, Zhang, Y.-Y, Yan, S.F, Neumann, D, Schlattner, U, Wang, Z.-X, Wu, J.-W. | | 登録日 | 2012-03-22 | | 公開日 | 2012-06-06 | | 最終更新日 | 2023-11-08 | | 実験手法 | X-RAY DIFFRACTION (2.506 Å) | | 主引用文献 | AMP-activated protein kinase undergoes nucleotide-dependent conformational changes
Nat.Struct.Mol.Biol., 19, 2012
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5T5T
 | | AMPK bound to allosteric activator | | 分子名称: | 5'-AMP-activated protein kinase catalytic subunit alpha-1, 5'-AMP-activated protein kinase subunit beta-1, 5'-AMP-activated protein kinase subunit gamma-1, ... | | 著者 | Calabrese, M.F, Kurumbail, R.G. | | 登録日 | 2016-08-31 | | 公開日 | 2017-03-29 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (3.46 Å) | | 主引用文献 | Selective Activation of AMPK beta 1-Containing Isoforms Improves Kidney Function in a Rat Model of Diabetic Nephropathy.
J. Pharmacol. Exp. Ther., 361, 2017
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7MYJ
 | | Structure of full length human AMPK (a2b1g1) in complex with a small molecule activator MSG011 | | 分子名称: | (5S,6R,7R,9R,13cR,14R,16aS)-6-methoxy-5-methyl-7-(methylamino)-6,7,8,9,14,15,16,16a-octahydro-5H,13cH-5,9-epoxy-4b,9a,1 5-triazadibenzo[b,h]cyclonona[1,2,3,4-jkl]cyclopenta[e]-as-indacen-14-ol, 5'-AMP-activated protein kinase catalytic subunit alpha-2, 5'-AMP-activated protein kinase subunit beta-1, ... | | 著者 | Ovens, A.J, Gee, Y.S, Ling, N.X.Y, Waters, N.J, Yu, D, Scott, J.W, Parker, M.W, Hoffman, N.J, Kemp, B.E, Baell, J.B, Oakhill, J.S, Langendorf, C.G. | | 登録日 | 2021-05-21 | | 公開日 | 2022-06-29 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (2.95 Å) | | 主引用文献 | Structure-function analysis of the AMPK activator SC4 and identification of a potent pan AMPK activator.
Biochem.J., 479, 2022
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5UFU
 | | Structure of AMPK bound to activator | | 分子名称: | 1,4:3,6-dianhydro-2-O-(6-chloro-5-{4-[1-(hydroxymethyl)cyclopropyl]phenyl}-1H-benzimidazol-2-yl)-D-mannitol, 5'-AMP-activated protein kinase catalytic subunit alpha-1, 5'-AMP-activated protein kinase subunit beta-1, ... | | 著者 | Calabrese, M.F, Kurumbail, R.G. | | 登録日 | 2017-01-05 | | 公開日 | 2017-05-17 | | 実験手法 | X-RAY DIFFRACTION (3.45 Å) | | 主引用文献 | Activation of Skeletal Muscle AMPK Promotes Glucose Disposal and Glucose Lowering in Non-human Primates and Mice.
Cell Metab., 25, 2017
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6E4T
 | | Structure of AMPK bound to activator | | 分子名称: | 1-O-{6-chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carbonyl}-beta-D-glucopyranuronic acid, 5'-AMP-activated protein kinase catalytic subunit alpha-1, 5'-AMP-activated protein kinase subunit beta-1, ... | | 著者 | Calabrese, M.F, Kurumbail, R.G. | | 登録日 | 2018-07-18 | | 公開日 | 2018-08-08 | | 最終更新日 | 2018-09-05 | | 実験手法 | X-RAY DIFFRACTION (3.4 Å) | | 主引用文献 | Acyl Glucuronide Metabolites of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1 H-indole-3-carboxylic Acid (PF-06409577) and Related Indole-3-carboxylic Acid Derivatives are Direct Activators of Adenosine Monophosphate-Activated Protein Kinase (AMPK).
J. Med. Chem., 61, 2018
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6E4U
 | | Structure of AMPK bound to activator | | 分子名称: | 1-O-{6-chloro-5-[6-(dimethylamino)-2-methoxypyridin-3-yl]-1H-indole-3-carbonyl}-beta-D-glucopyranuronic acid, 5'-AMP-activated protein kinase catalytic subunit alpha-1, 5'-AMP-activated protein kinase subunit beta-1, ... | | 著者 | Calabrese, M.F, Kurumbail, R.G. | | 登録日 | 2018-07-18 | | 公開日 | 2018-08-08 | | 最終更新日 | 2018-09-05 | | 実験手法 | X-RAY DIFFRACTION (3.27 Å) | | 主引用文献 | Acyl Glucuronide Metabolites of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1 H-indole-3-carboxylic Acid (PF-06409577) and Related Indole-3-carboxylic Acid Derivatives are Direct Activators of Adenosine Monophosphate-Activated Protein Kinase (AMPK).
J. Med. Chem., 61, 2018
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6E4W
 | | Structure of AMPK bound to activator | | 分子名称: | 1-O-(4,6-difluoro-5-{4-[(2S)-oxan-2-yl]phenyl}-1H-indole-3-carbonyl)-beta-D-glucopyranuronic acid, 5'-AMP-activated protein kinase catalytic subunit alpha-1, 5'-AMP-activated protein kinase subunit beta-1, ... | | 著者 | Calabrese, M.F, Kurumbail, R.G. | | 登録日 | 2018-07-18 | | 公開日 | 2018-08-08 | | 最終更新日 | 2018-09-05 | | 実験手法 | X-RAY DIFFRACTION (3.35 Å) | | 主引用文献 | Acyl Glucuronide Metabolites of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1 H-indole-3-carboxylic Acid (PF-06409577) and Related Indole-3-carboxylic Acid Derivatives are Direct Activators of Adenosine Monophosphate-Activated Protein Kinase (AMPK).
J. Med. Chem., 61, 2018
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3T4N
 | | Structure of the regulatory fragment of Saccharomyces cerevisiae AMPK in complex with ADP | | 分子名称: | ADENOSINE-5'-DIPHOSPHATE, Carbon catabolite-derepressing protein kinase, Nuclear protein SNF4, ... | | 著者 | Mayer, F.V, Heath, R, Underwood, E, Sanders, M.J, Carmena, D, McCartney, R, Leiper, F.C, Xiao, B, Jing, C, Walker, P.A, Haire, L.F, Ogrodowicz, R, Martin, S.R, Schmdit, M.C, Gamblin, S.J, Carling, D. | | 登録日 | 2011-07-26 | | 公開日 | 2011-11-09 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | | 主引用文献 | ADP Regulates SNF1, the Saccharomyces cerevisiae Homolog of AMP-Activated Protein Kinase.
Cell Metab, 14, 2011
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3TE5
 | | structure of the regulatory fragment of sacchromyces cerevisiae ampk in complex with NADH | | 分子名称: | 1,4-DIHYDRONICOTINAMIDE ADENINE DINUCLEOTIDE, Carbon catabolite-derepressing protein kinase, Nuclear protein SNF4, ... | | 著者 | Mayer, F.V, Heath, R, Underwood, E, Sanders, M.J, Carmena, D, McCartney, R, Leiper, F.C, Xiao, B, Jing, C, Walker, P.A, Haire, L.F, Ogrodowicz, R, Martin, S.R, Schmidt, M.C, Gamblin, S.J, Carling, D. | | 登録日 | 2011-08-12 | | 公開日 | 2011-11-09 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | ADP Regulates SNF1, the Saccharomyces cerevisiae Homolog of AMP-Activated Protein Kinase.
Cell Metab, 14, 2011
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7JHG
 | | Cryo-EM structure of ATP-bound fully inactive AMPK in complex with Dorsomorphin (Compound C) and Fab-nanobody | | 分子名称: | 5'-AMP-activated protein kinase catalytic subunit alpha-1, 5'-AMP-activated protein kinase subunit beta-2, 5'-AMP-activated protein kinase subunit gamma-1, ... | | 著者 | Yan, Y, Murkherjee, S, Zhou, X.E, Xu, T.H, Xu, H.E, Kossiakoff, A.A, Melcher, K. | | 登録日 | 2020-07-20 | | 公開日 | 2021-07-21 | | 最終更新日 | 2021-12-15 | | 実験手法 | ELECTRON MICROSCOPY (3.47 Å) | | 主引用文献 | Structure of an AMPK complex in an inactive, ATP-bound state.
Science, 373, 2021
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7JHH
 | | Cryo-EM structure of ATP-bound fully inactive AMPK in complex with Fab and nanobody | | 分子名称: | 5'-AMP-activated protein kinase catalytic subunit alpha-1, 5'-AMP-activated protein kinase subunit beta-2, 5'-AMP-activated protein kinase subunit gamma-1, ... | | 著者 | Yan, Y, Murkherjee, S, Zhou, X.E, Xu, T.H, Xu, H.E, Kossiakoff, A.A, Melcher, K. | | 登録日 | 2020-07-20 | | 公開日 | 2021-07-21 | | 最終更新日 | 2021-12-15 | | 実験手法 | ELECTRON MICROSCOPY (3.92 Å) | | 主引用文献 | Structure of an AMPK complex in an inactive, ATP-bound state.
Science, 373, 2021
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7JIJ
 | | ATP-bound AMP-activated protein kinase | | 分子名称: | 5'-AMP-activated protein kinase catalytic subunit alpha-1, 5'-AMP-activated protein kinase subunit beta-2, 5'-AMP-activated protein kinase subunit gamma-1, ... | | 著者 | Yan, Y, Zhou, X.E, Powell, K, Xu, T, Brunzelle, J.S, Xu, H.X, Melcher, K. | | 登録日 | 2020-07-23 | | 公開日 | 2021-07-28 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (5.5 Å) | | 主引用文献 | Structure of an AMPK complex in an inactive, ATP-bound state.
Science, 373, 2021
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3TDH
 | | Structure of the regulatory fragment of sccharomyces cerevisiae AMPK in complex with AMP | | 分子名称: | ADENOSINE MONOPHOSPHATE, Carbon catabolite-derepressing protein kinase, Nuclear protein SNF4, ... | | 著者 | Mayer, F.V, Heath, R, Underwood, E, Sanders, M.J, Carmena, D, McCartney, R, Leiper, F.C, Xiao, B, Jing, C, Walker, P.A, Haire, L.F, Ogrodowicz, R, Martin, S.R, Schmidt, M.C, Gamblin, S.J, Carling, D. | | 登録日 | 2011-08-11 | | 公開日 | 2011-11-09 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | | 主引用文献 | ADP Regulates SNF1, the Saccharomyces cerevisiae Homolog of AMP-Activated Protein Kinase.
Cell Metab, 14, 2011
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4QFR
 | | Structure of AMPK in complex with Cl-A769662 activator and STAUROSPORINE inhibitor | | 分子名称: | 2-chloro-4-hydroxy-3-(2'-hydroxybiphenyl-4-yl)-6-oxo-6,7-dihydrothieno[2,3-b]pyridine-5-carbonitrile, 5'-AMP-activated protein kinase catalytic subunit alpha-1, 5'-AMP-activated protein kinase subunit beta-1, ... | | 著者 | Calabrese, M.F, Kurumbail, R.G. | | 登録日 | 2014-05-21 | | 公開日 | 2014-08-06 | | 最終更新日 | 2017-11-22 | | 実験手法 | X-RAY DIFFRACTION (3.34 Å) | | 主引用文献 | Structural Basis for AMPK Activation: Natural and Synthetic Ligands Regulate Kinase Activity from Opposite Poles by Different Molecular Mechanisms.
Structure, 22, 2014
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4QFS
 | | Structure of AMPK in complex with Br2-A769662core activator and STAUROSPORINE inhibitor | | 分子名称: | 2-bromo-3-(4-bromophenyl)-4-hydroxy-6-oxo-6,7-dihydrothieno[2,3-b]pyridine-5-carbonitrile, 5'-AMP-activated protein kinase catalytic subunit alpha-1, 5'-AMP-activated protein kinase subunit beta-1, ... | | 著者 | Calabrese, M.F, Kurumbail, R.G. | | 登録日 | 2014-05-21 | | 公開日 | 2014-08-06 | | 最終更新日 | 2017-11-22 | | 実験手法 | X-RAY DIFFRACTION (3.55 Å) | | 主引用文献 | Structural Basis for AMPK Activation: Natural and Synthetic Ligands Regulate Kinase Activity from Opposite Poles by Different Molecular Mechanisms.
Structure, 22, 2014
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4RER
 | | Crystal structure of the phosphorylated human alpha1 beta2 gamma1 holo-AMPK complex bound to AMP and cyclodextrin | | 分子名称: | 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID, 5'-AMP-activated protein kinase catalytic subunit alpha-1, 5'-AMP-activated protein kinase subunit beta-2, ... | | 著者 | Zhou, X.E, Ke, J, Li, X, Wang, L, Gu, X, de Waal, P.W, Tan, M.H.E, Wang, D, Wu, D, Xu, H.E, Melcher, K. | | 登録日 | 2014-09-23 | | 公開日 | 2014-12-10 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (4.047 Å) | | 主引用文献 | Structural basis of AMPK regulation by adenine nucleotides and glycogen.
Cell Res., 25, 2015
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4REW
 | | Crystal structure of the non-phosphorylated human alpha1 beta2 gamma1 holo-AMPK complex | | 分子名称: | 5'-AMP-activated protein kinase catalytic subunit alpha-1, 5'-AMP-activated protein kinase subunit beta-2, 5'-AMP-activated protein kinase subunit gamma-1, ... | | 著者 | Zhou, X.E, Ke, J, Li, X, Wang, L, Gu, X, de Waal, P.W, Tan, M.H.E, Wang, D, Wu, D, Xu, H.E, Melcher, K. | | 登録日 | 2014-09-24 | | 公開日 | 2014-12-10 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (4.58 Å) | | 主引用文献 | Structural basis of AMPK regulation by adenine nucleotides and glycogen.
Cell Res., 25, 2015
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2V8Q
 | | Crystal structure of the regulatory fragment of mammalian AMPK in complexes with AMP | | 分子名称: | 5'-AMP-ACTIVATED PROTEIN KINASE CATALYTIC SUBUNIT ALPHA-1, 5'-AMP-ACTIVATED PROTEIN KINASE SUBUNIT BETA-2, 5'-AMP-ACTIVATED PROTEIN KINASE SUBUNIT GAMMA-1, ... | | 著者 | Xiao, B, Heath, R, Saiu, P, Leiper, F.C, Leone, P, Jing, C, Walker, P.A, Haire, L, Eccleston, J.F, Davis, C.T, Martin, S.R, Carling, D, Gamblin, S.J. | | 登録日 | 2007-08-13 | | 公開日 | 2007-09-25 | | 最終更新日 | 2011-07-13 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | Structural Basis for AMP Binding to Mammalian AMP-Activated Protein Kinase
Nature, 449, 2007
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