Author results

2BCJ
  • Download 2bcj
  • View 2bcj
Molmil generated image of 2bcj
CRYSTAL STRUCTURE OF G PROTEIN-COUPLED RECEPTOR KINASE 2 IN COMPLEX WITH GALPHA-Q AND GBETAGAMMA SUBUNITS
分子名称:G-protein-coupled receptor kinase 2, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Tesmer, J.J.G.
登録日2005-10-19
公開日2005-12-20
最終更新日2017-06-28
実験手法X-RAY DIFFRACTION (3.061 Å)
主引用文献Snapshot of Activated G Proteins at the Membrane: The Gq-GRK2-G Complex
Science, 310, 2005
1CS4
  • Download 1cs4
  • View 1cs4
Molmil generated image of 1cs4
COMPLEX OF GS-ALPHA WITH THE CATALYTIC DOMAINS OF MAMMALIAN ADENYLYL CYCLASE: COMPLEX WITH 2'-DEOXY-ADENOSINE 3'-MONOPHOSPHATE, PYROPHOSPHATE AND MG
分子名称:TYPE V ADENYLATE CYCLASE, TYPE II ADENYLATE CYCLASE, GUANINE NUCLEOTIDE-BINDING PROTEIN G(S), ...
著者Tesmer, J.J.G., Dessauer, C.A., Sunahara, R.K., Johnson, R.A., Gilman, A.G., Sprang, S.R.
登録日1999-08-16
公開日2001-01-10
最終更新日2011-07-13
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献Molecular basis for P-site inhibition of adenylyl cyclase.
Biochemistry, 39, 2000
1GPM
  • Download 1gpm
  • View 1gpm
Molmil generated image of 1gpm
ESCHERICHIA COLI GMP SYNTHETASE COMPLEXED WITH AMP AND PYROPHOSPHATE
分子名称:GMP SYNTHETASE, PHOSPHATE ION, PYROPHOSPHATE 2-, ...
著者Tesmer, J.J.G.
登録日1995-04-04
公開日1996-01-29
最終更新日2011-07-13
実験手法X-RAY DIFFRACTION (2.2 Å)
主引用文献The crystal structure of GMP synthetase reveals a novel catalytic triad and is a structural paradigm for two enzyme families.
Nat.Struct.Biol., 3, 1996
1OMW
  • Download 1omw
  • View 1omw
Molmil generated image of 1omw
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(T) beta subunit 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) gamma-2 subunit
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2011-07-27
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
1YM7
  • Download 1ym7
  • View 1ym7
Molmil generated image of 1ym7
G PROTEIN-COUPLED RECEPTOR KINASE 2 (GRK2)
分子名称:Beta-adrenergic receptor kinase 1
著者Lodowski, D.T., Barnhill, J.F., Pyskadlo, R.M., Ghirlando, R., Sterne-Marr, R., Tesmer, J.J.G.
登録日2005-01-20
公開日2005-07-05
最終更新日2011-07-13
実験手法X-RAY DIFFRACTION (4.5 Å)
主引用文献The role of Gbetagamma and domain interfaces in the activation of G protein-coupled receptor kinase 2
Biochemistry, 44, 2005
5TXF
  • Download 5txf
  • View 5txf
Molmil generated image of 5txf
CRYSTAL STRUCTURE OF LECITHIN:CHOLESTEROL ACYLTRANSFERASE (LCAT) IN A CLOSED CONFORMATION
分子名称:Phosphatidylcholine-sterol acyltransferase, N-ACETYL-D-GLUCOSAMINE, BETA-D-MANNOSE
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2017-12-20
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
5W5V
  • Download 5w5v
  • View 5w5v
Molmil generated image of 5w5v
TBK1 CO-CRYSTAL STRUCTURE WITH AMLEXANOX
分子名称:Serine/threonine-protein kinase TBK1, 2-amino-7-(1-methylethyl)-5-oxo-5H-chromeno[2,3-b]pyridine-3-carboxylic acid
著者Beyett, T.S., Tesmer, J.J.G.
登録日2017-06-15
公開日2018-06-27
最終更新日2018-09-26
実験手法X-RAY DIFFRACTION (3.645 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
5WG3
  • Download 5wg3
  • View 5wg3
Molmil generated image of 5wg3
HUMAN GRK2 IN COMPLEX WITH GBETAGAMMA SUBUNITS AND CCG258748
分子名称:Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-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2017-07-13
公開日2017-12-27
最終更新日2018-01-17
実験手法X-RAY DIFFRACTION (2.896 Å)
主引用文献Structural Determinants Influencing the Potency and Selectivity of Indazole-Paroxetine Hybrid G Protein-Coupled Receptor Kinase 2 Inhibitors.
Mol. Pharmacol., 92, 2017
5WG4
  • Download 5wg4
  • View 5wg4
Molmil generated image of 5wg4
HUMAN GRK2 IN COMPLEX WITH GBETAGAMMA SUBUNITS AND CCG257284
分子名称:Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-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2017-07-13
公開日2017-12-27
実験手法X-RAY DIFFRACTION (2.31 Å)
主引用文献Structural Determinants Influencing the Potency and Selectivity of Indazole-Paroxetine Hybrid G Protein-Coupled Receptor Kinase 2 Inhibitors.
Mol. Pharmacol., 92, 2017
5WG5
  • Download 5wg5
  • View 5wg5
Molmil generated image of 5wg5
HUMAN GRK2 IN COMPLEX WITH GBETAGAMMA SUBUNITS AND CCG224061
分子名称:Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-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2017-07-13
公開日2017-12-27
実験手法X-RAY DIFFRACTION (3.1 Å)
主引用文献Structural Determinants Influencing the Potency and Selectivity of Indazole-Paroxetine Hybrid G Protein-Coupled Receptor Kinase 2 Inhibitors.
Mol. Pharmacol., 92, 2017
6BNM
  • Download 6bnm
  • View 6bnm
Molmil generated image of 6bnm
CRYSTAL STRUCTURE OF THE P-REX2 PH DOMAIN
分子名称:Phosphatidylinositol 3,4,5-trisphosphate-dependent Rac exchanger 2 protein, CHLORIDE ION
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2019-06-05
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
6BNY
  • Download 6bny
  • View 6bny
Molmil generated image of 6bny
TBK1 IN COMPLEX WITH TETRAZOLE ANALOG OF AMLEXANOX
分子名称:Serine/threonine-protein kinase TBK1, 2-amino-7-(propan-2-yl)-3-(1H-tetrazol-5-yl)-5H-[1]benzopyrano[2,3-b]pyridin-5-one
著者Beyett, T.S., Tesmer, J.J.G.
登録日2017-11-17
公開日2018-09-26
最終更新日2019-02-20
実験手法X-RAY DIFFRACTION (3.341 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
6BOD
  • Download 6bod
  • View 6bod
Molmil generated image of 6bod
TBK1 IN COMPLEX WITH ETHYL ESTER ANALOG OF AMLEXANOX
分子名称:Serine/threonine-protein kinase TBK1, ethyl 2-amino-5-oxo-7-(propan-2-yl)-5H-[1]benzopyrano[2,3-b]pyridine-3-carboxylate
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2019-02-20
実験手法X-RAY DIFFRACTION (3.197 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
6BOE
  • Download 6boe
  • View 6boe
Molmil generated image of 6boe
TBK1 IN COMPLEX WITH AMIDE-COUPLED TETRAZOLE ANALOG OF AMLEXANOX
分子名称:Serine/threonine-protein kinase TBK1, 2-amino-5-oxo-7-(propan-2-yl)-N-(1H-tetrazol-5-yl)-5H-[1]benzopyrano[2,3-b]pyridine-3-carboxamide
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2019-02-20
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
6C2Y
  • Download 6c2y
  • View 6c2y
Molmil generated image of 6c2y
HUMAN GRK2 IN COMPLEX WITH GBETAGAMMA SUBUNITS AND CCG257142
分子名称:Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-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2018-05-02
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
6CQ0
  • Download 6cq0
  • View 6cq0
Molmil generated image of 6cq0
TBK1 IN COMPLEX WITH DIMETHYL AMINO ANALOG OF AMLEXANOX
分子名称:Serine/threonine-protein kinase TBK1, 2-amino-7-[3-(dimethylamino)propyl]-5-oxo-5H-[1]benzopyrano[2,3-b]pyridine-3-carboxylic acid
著者Beyett, T.S., Tesmer, J.J.G.
登録日2018-03-14
公開日2018-12-05
最終更新日2019-02-20
実験手法X-RAY DIFFRACTION (3.19 Å)
主引用文献Design, synthesis, and biological activity of substituted 2-amino-5-oxo-5H-chromeno[2,3-b]pyridine-3-carboxylic acid derivatives as inhibitors of the inflammatory kinases TBK1 and IKK epsilon for the treatment of obesity.
Bioorg. Med. Chem., 26, 2018
6CQ4
  • Download 6cq4
  • View 6cq4
Molmil generated image of 6cq4
TBK1 IN COMPLEX WITH CYCLOHEXYL ANALOG OF AMLEXANOX
分子名称:Serine/threonine-protein kinase TBK1, 2-amino-7-(4,4-difluorocyclohexyl)-5-oxo-5H-[1]benzopyrano[2,3-b]pyridine-3-carboxylic acid
著者Beyett, T.S., Tesmer, J.J.G.
登録日2018-03-14
公開日2018-12-05
最終更新日2019-02-20
実験手法X-RAY DIFFRACTION (3.2 Å)
主引用文献Design, synthesis, and biological activity of substituted 2-amino-5-oxo-5H-chromeno[2,3-b]pyridine-3-carboxylic acid derivatives as inhibitors of the inflammatory kinases TBK1 and IKK epsilon for the treatment of obesity.
Bioorg. Med. Chem., 26, 2018
6CQ5
  • Download 6cq5
  • View 6cq5
Molmil generated image of 6cq5
TBK1 IN COMPLEX WITH SULFONE ANALOG OF AMLEXANOX
分子名称:Serine/threonine-protein kinase TBK1, 2-amino-7-(1,1-dioxo-1lambda~6~-thian-4-yl)-5-oxo-5H-[1]benzopyrano[2,3-b]pyridine-3-carboxylic acid
著者Beyett, T.S., Tesmer, J.J.G.
登録日2018-03-14
公開日2018-12-05
最終更新日2019-02-20
実験手法X-RAY DIFFRACTION (3.354 Å)
主引用文献Design, synthesis, and biological activity of substituted 2-amino-5-oxo-5H-chromeno[2,3-b]pyridine-3-carboxylic acid derivatives as inhibitors of the inflammatory kinases TBK1 and IKK epsilon for the treatment of obesity.
Bioorg. Med. Chem., 26, 2018
6EEB
  • Download 6eeb
  • View 6eeb
Molmil generated image of 6eeb
CALMODULIN IN COMPLEX WITH MALBRANCHEAMIDE
分子名称:Calmodulin-1, (5aS,12aS,13aS)-8,9-dichloro-12,12-dimethyl-2,3,11,12,12a,13-hexahydro-1H,5H,6H-5a,13a-(epiminomethano)indolizino[7,6-b]carbazol-14-one, CALCIUM ION, ...
著者Beyett, T.S., Fraley, A.E., Tesmer, J.J.G.
登録日2018-08-13
公開日2019-08-07
最終更新日2019-08-21
実験手法X-RAY DIFFRACTION (1.96 Å)
主引用文献Perturbation of the interactions of calmodulin with GRK5 using a natural product chemical probe.
Proc.Natl.Acad.Sci.USA, 116, 2019
6O5G
  • Download 6o5g
  • View 6o5g
Molmil generated image of 6o5g
CALMODULIN IN COMPLEX WITH ISOMALBRANCHEAMIDE D
分子名称:Calmodulin-1, (5aS,12aS,13aS)-9-bromo-8-chloro-12,12-dimethyl-2,3,11,12,12a,13-hexahydro-1H,5H,6H-5a,13a-(epiminomethano)indolizino[7,6-b]carbazol-14-one, CALCIUM ION, ...
著者Beyett, T.S., Fraley, A.E., Tesmer, J.J.G.
登録日2019-03-02
公開日2019-08-07
最終更新日2019-08-21
実験手法X-RAY DIFFRACTION (1.89 Å)
主引用文献Perturbation of the interactions of calmodulin with GRK5 using a natural product chemical probe.
Proc.Natl.Acad.Sci.USA, 116, 2019
3KRW
  • Download 3krw
  • View 3krw
Molmil generated image of 3krw
HUMAN GRK2 IN COMPLEX WITH GBETGAMMA SUBUNITS AND BALANOL (SOAK)
分子名称:Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Tesmer, J.J.G., Tesmer, V.M.
登録日2009-11-19
公開日2010-02-16
最終更新日2011-07-13
実験手法X-RAY DIFFRACTION (2.9 Å)
主引用文献Structure of human g protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol.
J.Med.Chem., 53, 2010
3KRX
  • Download 3krx
  • View 3krx
Molmil generated image of 3krx
HUMAN GRK2 IN COMPLEX WITH GBETGAMMA SUBUNITS AND BALANOL (CO-CRYSTAL)
分子名称:Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Tesmer, J.J.G., Tesmer, V.M.
登録日2009-11-19
公開日2010-02-16
最終更新日2011-07-13
実験手法X-RAY DIFFRACTION (3.1 Å)
主引用文献Structure of human g protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol.
J.Med.Chem., 53, 2010
3UZS
  • Download 3uzs
  • View 3uzs
Molmil generated image of 3uzs
STRUCTURE OF THE C13.28 RNA APTAMER BOUND TO THE G PROTEIN-COUPLED RECEPTOR KINASE 2-HETEROTRIMERIC G PROTEIN BETA 1 AND GAMMA 2 SUBUNIT COMPLEX
分子名称:Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Tesmer, J.J.G., Tesmer, V.M.
登録日2011-12-07
公開日2012-07-11
最終更新日2012-08-29
実験手法X-RAY DIFFRACTION (4.52 Å)
主引用文献Molecular mechanism for inhibition of g protein-coupled receptor kinase 2 by a selective RNA aptamer.
Structure, 20, 2012
3UZT
  • Download 3uzt
  • View 3uzt
Molmil generated image of 3uzt
STRUCTURE OF THE C13.18 RNA APTAMER IN COMPLEX WITH G PROTEIN-COUPLED RECEPTOR KINASE 2
分子名称:Beta-adrenergic receptor kinase 1, C13.18 RNA Aptamer, MAGNESIUM ION
著者Tesmer, J.J.G., Tesmer, V.M.
登録日2011-12-07
公開日2012-07-11
最終更新日2012-08-29
実験手法X-RAY DIFFRACTION (3.51 Å)
主引用文献Molecular mechanism for inhibition of g protein-coupled receptor kinase 2 by a selective RNA aptamer.
Structure, 20, 2012
3CIK
  • Download 3cik
  • View 3cik
Molmil generated image of 3cik
HUMAN GRK2 IN COMPLEX WITH GBETAGAMMA SUBUNITS
分子名称:Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ...
著者Tesmer, J.J.G., Lodowski, D.T.
登録日2008-03-11
公開日2009-02-17
最終更新日2012-03-07
実験手法X-RAY DIFFRACTION (2.75 Å)
主引用文献Structure of human G protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol.
J.Med.Chem., 53, 2010