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5HE0
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BU of 5he0 by Molmil
Bovine GRK2 in complex with Gbetagamma subunits and CCG215022
分子名称: (4S)-4-{4-fluoro-3-[(pyridin-2-ylmethyl)carbamoyl]phenyl}-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Cato, M.C, Waninger-Saroni, J, Tesmer, J.J.G.
登録日2016-01-05
公開日2016-05-11
最終更新日2023-09-27
実験手法X-RAY DIFFRACTION (2.56 Å)
主引用文献Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors.
J.Med.Chem., 59, 2016
3C4Z
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BU of 3c4z by Molmil
Crystal structure of G protein coupled receptor kinase 1 bound to ADP and magnesium chloride at 1.84A
分子名称: ADENOSINE-5'-DIPHOSPHATE, CHLORIDE ION, MAGNESIUM ION, ...
著者Singh, P, Tesmer, J.J.G.
登録日2008-01-30
公開日2008-03-11
最終更新日2023-08-30
実験手法X-RAY DIFFRACTION (1.84 Å)
主引用文献Structures of rhodopsin kinase in different ligand states reveal key elements involved in G protein-coupled receptor kinase activation.
J.Biol.Chem., 283, 2008
3C50
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BU of 3c50 by Molmil
Crystal Structure of G protein coupled receptor kinase 1 bound to ADP and magnesium chloride at 2.6A
分子名称: 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, ADENOSINE-5'-DIPHOSPHATE, CHLORIDE ION, ...
著者Singh, P, Tesmer, J.J.G.
登録日2008-01-30
公開日2008-03-11
最終更新日2023-08-30
実験手法X-RAY DIFFRACTION (2.6 Å)
主引用文献Structures of rhodopsin kinase in different ligand states reveal key elements involved in G protein-coupled receptor kinase activation.
J.Biol.Chem., 283, 2008
3C4Y
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BU of 3c4y by Molmil
Crystal Structure of Apo form of G protein coupled receptor kinase 1 at 7.51A
分子名称: Rhodopsin kinase
著者Singh, P, Tesmer, J.J.G.
登録日2008-01-30
公開日2008-03-11
最終更新日2023-08-30
実験手法X-RAY DIFFRACTION (7.509 Å)
主引用文献Structures of rhodopsin kinase in different ligand states reveal key elements involved in G protein-coupled receptor kinase activation.
J.Biol.Chem., 283, 2008
3C51
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BU of 3c51 by Molmil
Crystal structure of G protein coupled receptor kinase 1 bound to ADP and magnesium chloride at 3.55A
分子名称: ADENOSINE-5'-DIPHOSPHATE, BROMIDE ION, MAGNESIUM ION, ...
著者Singh, P, Tesmer, J.J.G.
登録日2008-01-30
公開日2008-03-11
最終更新日2023-08-30
実験手法X-RAY DIFFRACTION (3.55 Å)
主引用文献Structures of rhodopsin kinase in different ligand states reveal key elements involved in G protein-coupled receptor kinase activation.
J.Biol.Chem., 283, 2008
3C4X
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BU of 3c4x by Molmil
Crystal Structure of G protein coupled receptor kinase 1 bound to ATP and magnesium chloride at 2.9A
分子名称: ADENOSINE-5'-TRIPHOSPHATE, CHLORIDE ION, MAGNESIUM ION, ...
著者Singh, P, Tesmer, J.J.G.
登録日2008-01-30
公開日2008-03-11
最終更新日2023-08-30
実験手法X-RAY DIFFRACTION (2.9 Å)
主引用文献Structures of rhodopsin kinase in different ligand states reveal key elements involved in G protein-coupled receptor kinase activation.
J.Biol.Chem., 283, 2008
3C4W
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BU of 3c4w by Molmil
Crystal Structure of G protein coupled receptor kinase 1 bound to ATP and magnesium chloride at 2.7A
分子名称: ADENOSINE-5'-TRIPHOSPHATE, CHLORIDE ION, MAGNESIUM ION, ...
著者Singh, P, Tesmer, J.J.G.
登録日2008-01-30
公開日2008-03-11
最終更新日2023-08-30
実験手法X-RAY DIFFRACTION (2.7 Å)
主引用文献Structures of rhodopsin kinase in different ligand states reveal key elements involved in G protein-coupled receptor kinase activation.
J.Biol.Chem., 283, 2008
1ZCA
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BU of 1zca by Molmil
Crystal structure of G alpha 12 in complex with GDP, Mg2+ and AlF4-
分子名称: G alpha i/12, GUANOSINE-5'-DIPHOSPHATE, MAGNESIUM ION, ...
著者Nance, M.R, Tesmer, J.J.G.
登録日2005-04-11
公開日2005-11-15
最終更新日2023-08-23
実験手法X-RAY DIFFRACTION (2.9 Å)
主引用文献A new approach to producing functional G alpha subunits yields the activated and deactivated structures of G alpha(12/13) proteins.
Biochemistry, 45, 2006
1ZCB
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BU of 1zcb by Molmil
Crystal structure of G alpha 13 in complex with GDP
分子名称: G alpha i/13, GUANOSINE-5'-DIPHOSPHATE
著者Nance, M.R, Tesmer, J.J.G.
登録日2005-04-11
公開日2005-11-15
最終更新日2023-08-23
実験手法X-RAY DIFFRACTION (2 Å)
主引用文献A new approach to producing functional G alpha subunits yields the activated and deactivated structures of G alpha(12/13) proteins.
Biochemistry, 45, 2006
2ACX
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BU of 2acx by Molmil
Crystal Structure of G protein coupled receptor kinase 6 bound to AMPPNP
分子名称: G protein-coupled receptor kinase 6, MAGNESIUM ION, PHOSPHATE ION, ...
著者Lodowski, D.T, Tesmer, V.M, Benovic, J.L, Tesmer, J.J.
登録日2005-07-19
公開日2006-04-25
最終更新日2023-08-23
実験手法X-RAY DIFFRACTION (2.6 Å)
主引用文献The Structure of G Protein-coupled Receptor Kinase (GRK)-6 Defines a Second Lineage of GRKs.
J.Biol.Chem., 281, 2006
3PUI
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BU of 3pui by Molmil
Cocaine Esterase with mutations G4C, S10C
分子名称: CHLORIDE ION, Cocaine esterase, SODIUM ION
著者Nance, M.R, Tesmer, J.J.G.
登録日2010-12-04
公開日2011-09-21
最終更新日2023-09-06
実験手法X-RAY DIFFRACTION (1.53 Å)
主引用文献Subunit stabilization and polyethylene glycolation of cocaine esterase improves in vivo residence time.
Mol.Pharmacol., 80, 2011
3PUH
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BU of 3puh by Molmil
Cocaine Esterase, wild-type biologically active dimer
分子名称: Cocaine esterase, GLYCEROL, SULFATE ION
著者Nance, M.R, Tesmer, J.J.G.
登録日2010-12-04
公開日2011-09-21
最終更新日2024-02-21
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献Subunit stabilization and polyethylene glycolation of cocaine esterase improves in vivo residence time.
Mol.Pharmacol., 80, 2011
3QC9
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BU of 3qc9 by Molmil
Crystal structure of cross-linked bovine GRK1 T8C/N480C double mutant complexed with ADP and Mg
分子名称: ADENOSINE-5'-DIPHOSPHATE, GLYCEROL, MAGNESIUM ION, ...
著者Huang, C.-C, Tesmer, J.J.G.
登録日2011-01-15
公開日2011-02-16
最終更新日2023-09-13
実験手法X-RAY DIFFRACTION (2.7 Å)
主引用文献Activation of G Protein-Coupled Receptor Kinase 1 Involves Interactions between Its N-Terminal Region and Its Kinase Domain.
Biochemistry, 50, 2011
6D8Z
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BU of 6d8z by Molmil
Crystal Structure of the C-terminal Guanine Nucleotide Exchange Factor Module of Human Trio
分子名称: Triple functional domain protein
著者Bandekar, S, Tesmer, J.J.
登録日2018-04-27
公開日2019-02-20
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (2.65 Å)
主引用文献Structure of the C-terminal guanine nucleotide exchange factor module of Trio in an autoinhibited conformation reveals its oncogenic potential.
Sci Signal, 12, 2019
1APB
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BU of 1apb by Molmil
A PRO TO GLY MUTATION IN THE HINGE OF THE ARABINOSE-BINDING PROTEIN ENHANCES BINDING AND ALTERS SPECIFICITY: SUGAR-BINDING AND CRYSTALLOGRAPHIC STUDIES
分子名称: L-ARABINOSE-BINDING PROTEIN, alpha-D-fucopyranose, beta-D-fucopyranose
著者Vermersch, P.S, Tesmer, J.J.G, Quiocho, F.A.
登録日1991-11-15
公開日1992-01-15
最終更新日2024-02-07
実験手法X-RAY DIFFRACTION (1.76 Å)
主引用文献A Pro to Gly mutation in the hinge of the arabinose-binding protein enhances binding and alters specificity. Sugar-binding and crystallographic studies.
J.Biol.Chem., 265, 1990
1BAP
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BU of 1bap by Molmil
A PRO TO GLY MUTATION IN THE HINGE OF THE ARABINOSE-BINDING PROTEIN ENHANCES BINDING AND ALTERS SPECIFICITY: SUGAR-BINDING AND CRYSTALLOGRAPHIC STUDIES
分子名称: L-ARABINOSE-BINDING PROTEIN, alpha-L-arabinopyranose, beta-L-arabinopyranose
著者Vermersch, P.S, Tesmer, J.J.G, Quiocho, F.A.
登録日1991-11-15
公開日1992-01-15
最終更新日2024-02-07
実験手法X-RAY DIFFRACTION (1.75 Å)
主引用文献A Pro to Gly mutation in the hinge of the arabinose-binding protein enhances binding and alters specificity. Sugar-binding and crystallographic studies.
J.Biol.Chem., 265, 1990
3PVU
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BU of 3pvu by Molmil
Bovine GRK2 in complex with Gbetagamma subunits and a selective kinase inhibitor (CMPD101)
分子名称: 3-({[4-methyl-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl]methyl}amino)-N-[2-(trifluoromethyl)benzyl]benzamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Thal, D.M, Tesmer, J.J.
登録日2010-12-07
公開日2011-06-01
最終更新日2023-09-06
実験手法X-RAY DIFFRACTION (2.48 Å)
主引用文献Molecular Mechanism of Selectivity among G Protein-Coupled Receptor Kinase 2 Inhibitors.
Mol.Pharmacol., 80, 2011
3PSC
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BU of 3psc by Molmil
Bovine GRK2 in complex with Gbetagamma subunits
分子名称: Beta-adrenergic receptor kinase 1, 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Thal, D.M, Tesmer, J.J.
登録日2010-12-01
公開日2011-06-01
最終更新日2023-09-06
実験手法X-RAY DIFFRACTION (2.67 Å)
主引用文献Molecular Mechanism of Selectivity among G Protein-Coupled Receptor Kinase 2 Inhibitors.
Mol.Pharmacol., 80, 2011
3PVW
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BU of 3pvw by Molmil
Bovine GRK2 in complex with Gbetagamma subunits and a selective kinase inhibitor (CMPD103A)
分子名称: Beta-adrenergic receptor kinase 1, 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Thal, D.M, Tesmer, J.J.
登録日2010-12-07
公開日2011-06-01
最終更新日2023-09-06
実験手法X-RAY DIFFRACTION (2.49 Å)
主引用文献Molecular Mechanism of Selectivity among G Protein-Coupled Receptor Kinase 2 Inhibitors.
Mol.Pharmacol., 80, 2011
6MTW
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BU of 6mtw by Molmil
Lysosomal Phospholipase A2 in complex with Zinc
分子名称: 2-acetamido-2-deoxy-beta-D-glucopyranose, CHLORIDE ION, Group XV phospholipase A2, ...
著者Bouley, R, Tesmer, J.J.G.
登録日2018-10-22
公開日2019-03-20
最終更新日2023-10-11
実験手法X-RAY DIFFRACTION (1.999 Å)
主引用文献Structural Basis of Lysosomal Phospholipase A2Inhibition by Zn2.
Biochemistry, 58, 2019
5TXF
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BU of 5txf by Molmil
Crystal structure of Lecithin:cholesterol acyltransferase (LCAT) in a closed conformation
分子名称: 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Phosphatidylcholine-sterol acyltransferase, ...
著者Manthei, K.A, Glukhova, A, Tesmer, J.J.G.
登録日2016-11-16
公開日2017-10-25
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (3.1 Å)
主引用文献A retractable lid in lecithin:cholesterol acyltransferase provides a structural mechanism for activation by apolipoprotein A-I.
J. Biol. Chem., 292, 2017
1OMW
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BU of 1omw by Molmil
Crystal Structure of the complex between G Protein-Coupled Receptor Kinase 2 and Heterotrimeric G Protein beta 1 and gamma 2 subunits
分子名称: G-protein coupled receptor kinase 2, Guanine nucleotide-binding protein G(I)/G(S)/G(O) gamma-2 subunit, Guanine nucleotide-binding protein G(I)/G(S)/G(T) beta subunit 1
著者Lodowski, D.T, Pitcher, J.A, Capel, W.D, Lefkowitz, R.J, Tesmer, J.J.G.
登録日2003-02-26
公開日2003-06-03
最終更新日2023-08-16
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献Keeping G proteins at Bay: A Complex Between G Protein-Coupled Receptor Kinase 2 and G-Beta-Gamma
Science, 300, 2003
6BOE
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BU of 6boe by Molmil
TBK1 in complex with amide-coupled tetrazole analog of amlexanox
分子名称: 2-amino-5-oxo-7-(propan-2-yl)-N-(1H-tetrazol-5-yl)-5H-[1]benzopyrano[2,3-b]pyridine-3-carboxamide, Serine/threonine-protein kinase TBK1
著者Beyett, T.S, Tesmer, J.J.G.
登録日2017-11-19
公開日2018-09-26
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (3.598 Å)
主引用文献Carboxylic Acid Derivatives of Amlexanox Display Enhanced Potency toward TBK1 and IKKepsilonand Reveal Mechanisms for Selective Inhibition.
Mol. Pharmacol., 94, 2018
6BNM
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BU of 6bnm by Molmil
Crystal Structure of the P-Rex2 PH domain
分子名称: CHLORIDE ION, Phosphatidylinositol 3,4,5-trisphosphate-dependent Rac exchanger 2 protein
著者Cash, J.N, Sharma, P.V, Tesmer, J.J.G.
登録日2017-11-17
公開日2018-11-21
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (1.9 Å)
主引用文献Structural and biochemical characterization of the pleckstrin homology domain of the RhoGEF P-Rex2 and its regulation by PIP3.
J.Struct.Biol., 1, 2019
6C2Y
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BU of 6c2y by Molmil
Human GRK2 in complex with Gbetagamma subunits and CCG257142
分子名称: (4R,5R,6S)-4-[4-fluoro-3-({[3-(methoxymethyl)-1,2,4-oxadiazol-5-yl]methyl}carbamoyl)phenyl]-N-(2H-indazol-5-yl)-6-methyl-2-oxohexahydropyrimidine-5-carboxamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Bouley, R, Tesmer, J.J.G.
登録日2018-01-09
公開日2018-04-25
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (2.74 Å)
主引用文献Utilizing a structure-based docking approach to develop potent G protein-coupled receptor kinase (GRK) 2 and 5 inhibitors.
Bioorg. Med. Chem. Lett., 28, 2018

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