6CQ0
 
 | | TBK1 in Complex with Dimethyl Amino Analog of Amlexanox | | Descriptor: | 2-amino-7-[3-(dimethylamino)propyl]-5-oxo-5H-[1]benzopyrano[2,3-b]pyridine-3-carboxylic acid, Serine/threonine-protein kinase TBK1 | | Authors: | Beyett, T.S, Tesmer, J.J.G. | | Deposit date: | 2018-03-14 | | Release date: | 2018-12-05 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (3.19 Å) | | Cite: | 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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8SL4
 | | Dimeric form of human adenylyl cyclase 5 | | Descriptor: | Adenylate cyclase type 5 | | Authors: | Yen, Y.C, Tesmer, J.J.G. | | Deposit date: | 2023-04-20 | | Release date: | 2024-04-03 | | Last modified: | 2024-05-01 | | Method: | ELECTRON MICROSCOPY (7 Å) | | Cite: | Structure of adenylyl cyclase 5 in complex with G beta gamma offers insights into ADCY5-related dyskinesia.
Nat.Struct.Mol.Biol., 2024
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8SOA
 | | Phosphoinositide phosphate 3 kinase gamma bound with ATP | | Descriptor: | ADENOSINE-5'-TRIPHOSPHATE, Phosphoinositide 3-kinase regulatory subunit 5, phosphatidylinositol-4,5-bisphosphate 3-kinase | | Authors: | Chen, C.-L, Tesmer, J.J.G. | | Deposit date: | 2023-04-28 | | Release date: | 2024-04-03 | | Last modified: | 2024-04-17 | | Method: | ELECTRON MICROSCOPY (3.32 Å) | | Cite: | Molecular basis for G beta gamma-mediated activation of phosphoinositide 3-kinase gamma.
Nat.Struct.Mol.Biol., 2024
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8SOE
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8SOB
 | | Phosphoinositide phosphate 3 kinase gamma bound with ADP | | Descriptor: | ADENOSINE-5'-DIPHOSPHATE, Phosphoinositide 3-kinase regulatory subunit 5, phosphatidylinositol-4,5-bisphosphate 3-kinase | | Authors: | Chen, C.-L, Tesmer, J.J.G. | | Deposit date: | 2023-04-28 | | Release date: | 2024-04-03 | | Last modified: | 2024-04-17 | | Method: | ELECTRON MICROSCOPY (3.9 Å) | | Cite: | Molecular basis for G beta gamma-mediated activation of phosphoinositide 3-kinase gamma.
Nat.Struct.Mol.Biol., 2024
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8SO9
 | | Phosphoinositide phosphate 3 kinase gamma | | Descriptor: | Phosphoinositide 3-kinase regulatory subunit 5, phosphatidylinositol-4,5-bisphosphate 3-kinase | | Authors: | Chen, C.-L, Tesmer, J.J.G. | | Deposit date: | 2023-04-28 | | Release date: | 2024-04-03 | | Last modified: | 2024-04-17 | | Method: | ELECTRON MICROSCOPY (3.03 Å) | | Cite: | Molecular basis for G beta gamma-mediated activation of phosphoinositide 3-kinase gamma.
Nat.Struct.Mol.Biol., 2024
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8SL3
 | | Human adenylyl Cyclase 5 in complex with Gbg | | Descriptor: | Adenylate cyclase type 5, GERAN-8-YL GERAN, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Yen, Y.C, Tesmer, J.J.G. | | Deposit date: | 2023-04-20 | | Release date: | 2024-04-03 | | Last modified: | 2024-04-24 | | Method: | ELECTRON MICROSCOPY (7 Å) | | Cite: | Structure of adenylyl cyclase 5 in complex with G beta gamma offers insights into ADCY5-related dyskinesia.
Nat.Struct.Mol.Biol., 2024
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8SOC
 | | Phosphoinositide phosphate 3 kinase gamma bound with ADP and Gbetagamma | | Descriptor: | ADENOSINE-5'-DIPHOSPHATE, 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, ... | | Authors: | Chen, C.-L, Tesmer, J.J.G. | | Deposit date: | 2023-04-28 | | Release date: | 2024-04-03 | | Last modified: | 2024-04-17 | | Method: | ELECTRON MICROSCOPY (3.5 Å) | | Cite: | Molecular basis for G beta gamma-mediated activation of phosphoinositide 3-kinase gamma.
Nat.Struct.Mol.Biol., 2024
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8SOD
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8UAP
 | | Crystal Structure of Human G Protein-Coupled Receptor Kinase 5 D311N in Complex with CCG273441 | | Descriptor: | (3Z)-3-{[4-(2-chloroacetamido)-3,5-dimethyl-1H-pyrrol-2-yl]methylidene}-N-[(1R)-1-(4-fluorophenyl)ethyl]-2-oxo-2,3-dihydro-1H-indole-5-carboxamide, G protein-coupled receptor kinase 5 | | Authors: | Chen, Y, Tesmer, J.J.G. | | Deposit date: | 2023-09-21 | | Release date: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | 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
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8UAQ
 | | Crystal Structure of Human G Protein-Coupled Receptor Kinase 5 in Complex with GRL018-21 | | Descriptor: | (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 | | Authors: | Chen, Y, Tesmer, J.J.G. | | Deposit date: | 2023-09-21 | | Release date: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | 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
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8TUA
 | | Full-length P-Rex1 in complex with inositol 1,3,4,5-tetrakisphosphate (IP4) | | Descriptor: | INOSITOL-(1,3,4,5)-TETRAKISPHOSPHATE, Phosphatidylinositol 3,4,5-trisphosphate-dependent Rac exchanger 1 protein | | Authors: | Cash, J.N, Tesmer, J.J.G. | | Deposit date: | 2023-08-15 | | Release date: | 2024-04-10 | | Method: | ELECTRON MICROSCOPY (4.1 Å) | | Cite: | Full-length P-Rex1 in complex with inositol 1,3,4,5-tetrakisphosphate (IP4)
Elife, 2024
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6VSK
 | | Crystal structure of the P-Rex1 DEP1 domain | | Descriptor: | Phosphatidylinositol 3,4,5-trisphosphate-dependent Rac exchanger 1 protein | | Authors: | Tesmer, J, Ravala, S.K. | | Deposit date: | 2020-02-11 | | Release date: | 2020-07-22 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (3.12 Å) | | Cite: | The first DEP domain of the RhoGEF P-Rex1 autoinhibits activity and contributes to membrane binding.
J.Biol.Chem., 295, 2020
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