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
|
|
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
|
|
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
|
|
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
|
|
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
|
|
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
|
|
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
|
|
5W5V
 | | TBK1 co-crystal structure with amlexanox | | 分子名称: | 2-amino-7-(1-methylethyl)-5-oxo-5H-chromeno[2,3-b]pyridine-3-carboxylic acid, Serine/threonine-protein kinase TBK1 | | 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 | 2023-10-04 | | 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
|
|
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
|
|
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
|
|
8SOA
 | | Phosphoinositide phosphate 3 kinase gamma bound with ATP | | 分子名称: | ADENOSINE-5'-TRIPHOSPHATE, Phosphoinositide 3-kinase regulatory subunit 5, phosphatidylinositol-4,5-bisphosphate 3-kinase | | 著者 | Chen, C.-L, Tesmer, J.J.G. | | 登録日 | 2023-04-28 | | 公開日 | 2024-04-03 | | 最終更新日 | 2024-04-17 | | 実験手法 | ELECTRON MICROSCOPY (3.32 Å) | | 主引用文献 | Molecular basis for G beta gamma-mediated activation of phosphoinositide 3-kinase gamma.
Nat.Struct.Mol.Biol., 2024
|
|
8SO9
 | | Phosphoinositide phosphate 3 kinase gamma | | 分子名称: | Phosphoinositide 3-kinase regulatory subunit 5, phosphatidylinositol-4,5-bisphosphate 3-kinase | | 著者 | Chen, C.-L, Tesmer, J.J.G. | | 登録日 | 2023-04-28 | | 公開日 | 2024-04-03 | | 最終更新日 | 2024-04-17 | | 実験手法 | ELECTRON MICROSCOPY (3.03 Å) | | 主引用文献 | Molecular basis for G beta gamma-mediated activation of phosphoinositide 3-kinase gamma.
Nat.Struct.Mol.Biol., 2024
|
|
8SL4
 | |
8SOB
 | | Phosphoinositide phosphate 3 kinase gamma bound with ADP | | 分子名称: | ADENOSINE-5'-DIPHOSPHATE, Phosphoinositide 3-kinase regulatory subunit 5, phosphatidylinositol-4,5-bisphosphate 3-kinase | | 著者 | Chen, C.-L, Tesmer, J.J.G. | | 登録日 | 2023-04-28 | | 公開日 | 2024-04-03 | | 最終更新日 | 2024-04-17 | | 実験手法 | ELECTRON MICROSCOPY (3.9 Å) | | 主引用文献 | Molecular basis for G beta gamma-mediated activation of phosphoinositide 3-kinase gamma.
Nat.Struct.Mol.Biol., 2024
|
|
8SL3
 | | Human adenylyl Cyclase 5 in complex with Gbg | | 分子名称: | Adenylate cyclase type 5, GERAN-8-YL GERAN, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | 著者 | Yen, Y.C, Tesmer, J.J.G. | | 登録日 | 2023-04-20 | | 公開日 | 2024-04-03 | | 最終更新日 | 2024-04-24 | | 実験手法 | ELECTRON MICROSCOPY (7 Å) | | 主引用文献 | Structure of adenylyl cyclase 5 in complex with G beta gamma offers insights into ADCY5-related dyskinesia.
Nat.Struct.Mol.Biol., 2024
|
|
8SOE
 | |
8SOD
 | |
8SOC
 | |
8UAQ
 | | Crystal Structure of Human G Protein-Coupled Receptor Kinase 5 in Complex with GRL018-21 | | 分子名称: | (3Z)-N-[(1R)-1-(4-fluorophenyl)ethyl]-3-[(4-{[(2S)-2-(furan-2-yl)-2-hydroxyacetyl]amino}-3,5-dimethyl-1H-pyrrol-2-yl)methylidene]-2-oxo-2,3-dihydro-1H-indole-5-carboxamide, G protein-coupled receptor kinase 5 | | 著者 | Chen, Y, Tesmer, J.J.G. | | 登録日 | 2023-09-21 | | 公開日 | 2023-12-13 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Development of a new class of potent and highly selective G protein-coupled receptor kinase 5 inhibitors and structural insight from crystal structures of inhibitor complexes.
Eur.J.Med.Chem., 264, 2023
|
|
8UAP
 | |
8TUA
 | | Full-length P-Rex1 in complex with inositol 1,3,4,5-tetrakisphosphate (IP4) | | 分子名称: | INOSITOL-(1,3,4,5)-TETRAKISPHOSPHATE, Phosphatidylinositol 3,4,5-trisphosphate-dependent Rac exchanger 1 protein | | 著者 | Cash, J.N, Tesmer, J.J.G. | | 登録日 | 2023-08-15 | | 公開日 | 2024-04-10 | | 実験手法 | ELECTRON MICROSCOPY (4.1 Å) | | 主引用文献 | Full-length P-Rex1 in complex with inositol 1,3,4,5-tetrakisphosphate (IP4)
Elife, 2024
|
|
4EKD
 | |
4EKC
 | |
3UZT
 | |
3UZS
 | |
