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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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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5WG3
| Human GRK2 in complex with Gbetagamma subunits and CCG258748 | 分子名称: | 2-fluoro-5-[(3S,4R)-3-{[(1H-indazol-5-yl)oxy]methyl}piperidin-4-yl]-N-[(1H-pyrazol-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 | 2017-07-13 | 公開日 | 2017-12-27 | 最終更新日 | 2023-10-04 | 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
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5WG5
| Human GRK2 in complex with Gbetagamma subunits and CCG224061 | 分子名称: | 5-{[(3S,4R)-4-(4-fluorophenyl)piperidin-3-yl]methoxy}-2H-indazole, 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 | 2017-07-13 | 公開日 | 2017-12-27 | 最終更新日 | 2023-10-04 | 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
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5WG4
| Human GRK2 in complex with Gbetagamma subunits and CCG257284 | 分子名称: | 2-fluoro-5-[(3S,4R)-3-{[(1H-indazol-5-yl)oxy]methyl}piperidin-4-yl]-N-[(pyridin-2-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 | 2017-07-13 | 公開日 | 2017-12-27 | 最終更新日 | 2023-10-04 | 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
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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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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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6MTW
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5TXF
| 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
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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 | 2024-06-05 | 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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7SK6
| Cryo-EM structure of human ACKR3 in complex with chemokine N-terminal mutant CXCL12_LRHQ and an intracellular Fab | 分子名称: | Atypical chemokine receptor 3, CID24 Fab heavy chain, CID24 Fab light 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 (4 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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7SK4
| Cryo-EM structure of ACKR3 in complex with chemokine N-terminal mutant CXCL12_LRHQ, 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 (3.3 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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7SK8
| Cryo-EM structure of human ACKR3 in complex with CXCL12, a small molecule partial agonist CCX662, an extracellular Fab, 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 (3.3 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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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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7SK5
| Cryo-EM structure of ACKR3 in complex with CXCL12 and an intracellular Fab | 分子名称: | Anti-Fab nanobody, 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 (4 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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7SK7
| Cryo-EM structure of human ACKR3 in complex with CXCL12, a small molecule partial agonist CCX662, and an extracellular 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, Anti-Fab nanobody, Atypical chemokine receptor 3, ... | 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 (3.3 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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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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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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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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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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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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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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