1GPM
 
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2BCJ
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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: | 2'-DEOXY-ADENOSINE 3'-MONOPHOSPHATE, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, 5'-GUANOSINE-DIPHOSPHATE-MONOTHIOPHOSPHATE, ... | | 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 | 2024-02-07 | | 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
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7SJ4
 | | Human Trio residues 1284-1959 in complex with Rac1 | | 分子名称: | Ras-related C3 botulinum toxin substrate 1, Triple functional domain protein | | 著者 | Chen, C.-L, Ravala, S.K, Bandekar, S.J, Cash, J, Tesmer, J.J.G. | | 登録日 | 2021-10-15 | | 公開日 | 2022-07-06 | | 最終更新日 | 2022-08-24 | | 実験手法 | ELECTRON MICROSCOPY (2.86 Å) | | 主引用文献 | Structural/functional studies of Trio provide insights into its configuration and show that conserved linker elements enhance its activity for Rac1.
J.Biol.Chem., 298, 2022
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6U7C
 | | Human GRK2 in complex with Gbetagamma subunits and CCG258747 | | 分子名称: | 5-[(3S,4R)-3-{[(2H-1,3-benzodioxol-5-yl)oxy]methyl}piperidin-4-yl]-2-fluoro-N-[(2H-indazol-3-yl)methyl]benzamide, 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 | 2019-09-02 | | 公開日 | 2020-04-15 | | 最終更新日 | 2023-10-11 | | 実験手法 | X-RAY DIFFRACTION (2.44 Å) | | 主引用文献 | A New Paroxetine-Based GRK2 Inhibitor Reduces Internalization of themu-Opioid Receptor.
Mol.Pharmacol., 97, 2020
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6O5G
 | | Calmodulin in complex with isomalbrancheamide D | | 分子名称: | (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, Calmodulin-1, ... | | 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 | 2023-10-11 | | 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
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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(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
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6PCV
 | | Single Particle Reconstruction of Phosphatidylinositol (3,4,5) trisphosphate-dependent Rac exchanger 1 bound to G protein beta gamma subunits | | 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, Phosphatidylinositol (3,4,5) trisphosphate-dependent Rac exchanger 1 | | 著者 | Cash, J.N, Cianfrocco, M.A, Tesmer, J.J.G. | | 登録日 | 2019-06-18 | | 公開日 | 2019-10-23 | | 最終更新日 | 2024-03-20 | | 実験手法 | ELECTRON MICROSCOPY (3.2 Å) | | 主引用文献 | Cryo-electron microscopy structure and analysis of the P-Rex1-G beta gamma signaling scaffold.
Sci Adv, 5, 2019
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6MTW
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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 | 2023-08-23 | | 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
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7MT8
 | | Rhodopsin kinase (GRK1)-S5E/S488E/T489E in complex with rhodopsin | | 分子名称: | RETINAL, Rhodopsin, Rhodopsin kinase GRK1, ... | | 著者 | Chen, Q, Chen, C.-L, Tesmer, J.J.G. | | 登録日 | 2021-05-13 | | 公開日 | 2021-07-07 | | 最終更新日 | 2021-08-25 | | 実験手法 | ELECTRON MICROSCOPY (5.8 Å) | | 主引用文献 | Structures of rhodopsin in complex with G-protein-coupled receptor kinase 1.
Nature, 595, 2021
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7MTB
 | | Rhodopsin kinase (GRK1)-S5E/S488E/T489E in complex with rhodopsin and Fab6 | | 分子名称: | Fab6 heavy chain, Fab6 light chain, RETINAL, ... | | 著者 | Chen, Q, Chen, C.-L, Tesmer, J.J.G. | | 登録日 | 2021-05-13 | | 公開日 | 2021-07-07 | | 最終更新日 | 2021-08-25 | | 実験手法 | ELECTRON MICROSCOPY (4 Å) | | 主引用文献 | Structures of rhodopsin in complex with G-protein-coupled receptor kinase 1.
Nature, 595, 2021
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7MTA
 | | Rhodopsin kinase (GRK1)-S5E/S488E/T489E in complex with rhodopsin and Fab1 | | 分子名称: | Fab1 Heavy chain, Fab1 Light chain, RETINAL, ... | | 著者 | Chen, Q, Chen, C.-L, Tesmer, J.J.G. | | 登録日 | 2021-05-13 | | 公開日 | 2021-07-07 | | 最終更新日 | 2021-08-25 | | 実験手法 | ELECTRON MICROSCOPY (4.1 Å) | | 主引用文献 | Structures of rhodopsin in complex with G-protein-coupled receptor kinase 1.
Nature, 595, 2021
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7MT9
 | | Rhodopsin kinase (GRK1) in complex with rhodopsin | | 分子名称: | RETINAL, Rhodopsin, Rhodopsin kinase GRK1, ... | | 著者 | Chen, Q, Chen, C.-L, Tesmer, J.J.G. | | 登録日 | 2021-05-13 | | 公開日 | 2021-07-07 | | 最終更新日 | 2021-08-25 | | 実験手法 | ELECTRON MICROSCOPY (7 Å) | | 主引用文献 | Structures of rhodopsin in complex with G-protein-coupled receptor kinase 1.
Nature, 595, 2021
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6CQ4
 | | TBK1 in Complex with Cyclohexyl Analog of Amlexanox | | 分子名称: | 2-amino-7-(4,4-difluorocyclohexyl)-5-oxo-5H-[1]benzopyrano[2,3-b]pyridine-3-carboxylic acid, Serine/threonine-protein kinase TBK1 | | 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 | 2023-10-04 | | 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
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6CQ5
 | | TBK1 in Complex with Sulfone Analog of Amlexanox | | 分子名称: | 2-amino-7-(1,1-dioxo-1lambda~6~-thian-4-yl)-5-oxo-5H-[1]benzopyrano[2,3-b]pyridine-3-carboxylic acid, Serine/threonine-protein kinase TBK1 | | 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 | 2023-10-04 | | 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
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6CQ0
 | | TBK1 in Complex with Dimethyl Amino Analog of Amlexanox | | 分子名称: | 2-amino-7-[3-(dimethylamino)propyl]-5-oxo-5H-[1]benzopyrano[2,3-b]pyridine-3-carboxylic acid, Serine/threonine-protein kinase TBK1 | | 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 | 2023-10-04 | | 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
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6EEB
 | | Calmodulin in complex with malbrancheamide | | 分子名称: | (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, Calmodulin-1, ... | | 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 | 2023-10-11 | | 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
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6BOE
 | | 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
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6BNM
 | | 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
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6C2Y
 | | 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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6BNY
 | | TBK1 in complex with tetrazole analog of amlexanox | | 分子名称: | 2-amino-7-(propan-2-yl)-3-(1H-tetrazol-5-yl)-5H-[1]benzopyrano[2,3-b]pyridin-5-one, Serine/threonine-protein kinase TBK1 | | 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 | 2023-10-04 | | 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
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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 | 2023-10-04 | | 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
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7SK9
 | | Cryo-EM structure of human ACKR3 in complex with a small molecule partial agonist CCX662, and an intracellular Fab | | 分子名称: | (1R)-4-[7-(3-carboxypropoxy)-6-methylquinolin-8-yl]-1-{[2-(4-hydroxypiperidin-1-yl)-1,3-thiazol-4-yl]methyl}-1,4-diazepan-1-ium, Atypical chemokine receptor 3, CHOLESTEROL, ... | | 著者 | Yen, Y.C, Schafer, C.T, Gustavsson, M, Handel, T.M, Tesmer, J.J.G. | | 登録日 | 2021-10-19 | | 公開日 | 2022-07-27 | | 実験手法 | ELECTRON MICROSCOPY (3.7 Å) | | 主引用文献 | Structures of atypical chemokine receptor 3 reveal the basis for its promiscuity and signaling bias.
Sci Adv, 8, 2022
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7SK3
 | | Cryo-EM structure of ACKR3 in complex with CXCL12, an intracellular Fab, and an extracellular Fab | | 分子名称: | Atypical chemokine receptor 3, CHOLESTEROL, CID24 Fab heavy chain, ... | | 著者 | Yen, Y.C, Schafer, C.T, Gustavsson, M, Handel, T.M, Tesmer, J.J.G. | | 登録日 | 2021-10-19 | | 公開日 | 2022-07-27 | | 実験手法 | ELECTRON MICROSCOPY (3.8 Å) | | 主引用文献 | Structures of atypical chemokine receptor 3 reveal the basis for its promiscuity and signaling bias.
Sci Adv, 8, 2022
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