6PBC
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![BU of 6pbc by Molmil](/molmil-images/mine/6pbc) | Structural basis for the activation of PLC-gamma isozymes by phosphorylation and cancer-associated mutations | Descriptor: | 1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase gamma,1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase gamma-1, CALCIUM ION, SODIUM ION | Authors: | Hajicek, N, Sondek, J. | Deposit date: | 2019-06-13 | Release date: | 2020-01-08 | Last modified: | 2024-03-13 | Method: | X-RAY DIFFRACTION (2.46 Å) | Cite: | Structural basis for the activation of PLC-gamma isozymes by phosphorylation and cancer-associated mutations. Elife, 8, 2019
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7T8T
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![BU of 7t8t by Molmil](/molmil-images/mine/7t8t) | CryoEM structure of PLCg1 | Descriptor: | 1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase gamma, CALCIUM ION | Authors: | Endo-Streeter, S, Sondek, J. | Deposit date: | 2021-12-17 | Release date: | 2022-12-21 | Last modified: | 2024-06-05 | Method: | ELECTRON MICROSCOPY (3.68 Å) | Cite: | CryoEM structure of PLCg1 To Be Published
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7PWD
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![BU of 7pwd by Molmil](/molmil-images/mine/7pwd) | Structure of an inhibited GRK2-G-beta and G-gamma complex | Descriptor: | 4-chloranyl-N-[2-(4-chlorophenyl)ethyl]thieno[2,3-c]pyridine-2-carboxamide, Beta-adrenergic receptor kinase 1, CHLORIDE ION, ... | Authors: | Faucher, N, Tauchert, M.J, Konz Makino, D.L, Vuillard, L.M. | Deposit date: | 2021-10-06 | Release date: | 2021-10-20 | Last modified: | 2024-06-19 | Method: | X-RAY DIFFRACTION (2.6 Å) | Cite: | Synthesis of thieno[2,3-c]pyridine derived GRK2 inhibitors Monatsh Chem, 2022
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8GMB
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![BU of 8gmb by Molmil](/molmil-images/mine/8gmb) | Crystal structure of the full-length Bruton's tyrosine kinase (PH-TH domain not visible) | Descriptor: | 2-[3'-(hydroxymethyl)-1-methyl-5-({5-[(2S)-2-methyl-4-(oxetan-3-yl)piperazin-1-yl]pyridin-2-yl}amino)-6-oxo[1,6-dihydro[3,4'-bipyridine]]-2'-yl]-7,7-dimethyl-3,4,7,8-tetrahydro-2H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1(6H)-one, Tyrosine-protein kinase BTK | Authors: | Lin, D.Y, Andreotti, A.H. | Deposit date: | 2023-03-24 | Release date: | 2023-08-16 | Last modified: | 2024-01-31 | Method: | X-RAY DIFFRACTION (3.4 Å) | Cite: | Conformational heterogeneity of the BTK PHTH domain drives multiple regulatory states. Elife, 12, 2024
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7APJ
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![BU of 7apj by Molmil](/molmil-images/mine/7apj) | Structure of autoinhibited Akt1 reveals mechanism of PIP3-mediated activation | Descriptor: | NB41, RAC-alpha serine/threonine-protein kinase,Non-specific serine/threonine protein kinase,RAC-alpha serine/threonine-protein kinase | Authors: | Truebestein, L, Hornegger, H, Leonard, T.A. | Deposit date: | 2020-10-16 | Release date: | 2021-08-25 | Last modified: | 2024-01-31 | Method: | X-RAY DIFFRACTION (2.05 Å) | Cite: | Structure of autoinhibited Akt1 reveals mechanism of PIP 3 -mediated activation. Proc.Natl.Acad.Sci.USA, 118, 2021
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3CIK
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![BU of 3cik by Molmil](/molmil-images/mine/3cik) | Human GRK2 in Complex with Gbetagamma subunits | Descriptor: | Beta-adrenergic receptor kinase 1, 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: | Tesmer, J.J.G, Lodowski, D.T. | Deposit date: | 2008-03-11 | Release date: | 2009-02-17 | Last modified: | 2012-03-07 | Method: | X-RAY DIFFRACTION (2.75 Å) | Cite: | Structure of human G protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol. J.Med.Chem., 53, 2010
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7K7L
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![BU of 7k7l by Molmil](/molmil-images/mine/7k7l) | |
7K7Z
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![BU of 7k7z by Molmil](/molmil-images/mine/7k7z) | |
6S9W
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![BU of 6s9w by Molmil](/molmil-images/mine/6s9w) | |
6S9X
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![BU of 6s9x by Molmil](/molmil-images/mine/6s9x) | Crystal Structure of AKT1 in Complex with Covalent-Allosteric AKT Inhibitor 15c | Descriptor: | RAC-alpha serine/threonine-protein kinase, ~{N}-[3-[1-[[4-[5-[(4-hydroxyphenyl)methyl]-6-oxidanylidene-2-phenyl-1~{H}-pyrazin-3-yl]phenyl]methyl]piperidin-4-yl]-2-oxidanylidene-1~{H}-benzimidazol-5-yl]propanamide | Authors: | Landel, I, Mueller, M.P, Rauh, D. | Deposit date: | 2019-07-15 | Release date: | 2019-10-16 | Last modified: | 2024-01-24 | Method: | X-RAY DIFFRACTION (2.6 Å) | Cite: | Covalent-Allosteric Inhibitors to Achieve Akt Isoform-Selectivity. Angew.Chem.Int.Ed.Engl., 58, 2019
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4MK0
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![BU of 4mk0 by Molmil](/molmil-images/mine/4mk0) | |
5KCV
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![BU of 5kcv by Molmil](/molmil-images/mine/5kcv) | Crystal structure of allosteric inhibitor, ARQ 092, in complex with autoinhibited form of AKT1 | Descriptor: | 3-[3-[4-(1-azanylcyclobutyl)phenyl]-5-phenyl-imidazo[4,5-b]pyridin-2-yl]pyridin-2-amine, RAC-alpha serine/threonine-protein kinase | Authors: | Eathiraj, S. | Deposit date: | 2016-06-07 | Release date: | 2016-06-29 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (2.7 Å) | Cite: | Discovery of 3-(3-(4-(1-Aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine (ARQ 092): An Orally Bioavailable, Selective, and Potent Allosteric AKT Inhibitor. J.Med.Chem., 59, 2016
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8JPC
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![BU of 8jpc by Molmil](/molmil-images/mine/8jpc) | cryo-EM structure of NTSR1-GRK2-Galpha(q) complexes 2 | Descriptor: | 2-[{2-(1-fluorocyclopropyl)-4-[4-(2-methoxyphenyl)piperidin-1-yl]quinazolin-6-yl}(methyl)amino]ethan-1-ol, Beta-adrenergic receptor kinase 1, GUANOSINE-5'-DIPHOSPHATE, ... | Authors: | Duan, J, Liu, H, Zhao, F, Yuan, Q, Ji, Y, Xu, H.E. | Deposit date: | 2023-06-11 | Release date: | 2023-08-09 | Last modified: | 2023-08-30 | Method: | ELECTRON MICROSCOPY (3.07 Å) | Cite: | GPCR activation and GRK2 assembly by a biased intracellular agonist. Nature, 620, 2023
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8JPB
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![BU of 8jpb by Molmil](/molmil-images/mine/8jpb) | cryo-EM structure of NTSR1-GRK2-Galpha(q) complexes 1 | Descriptor: | 2-[{2-(1-fluorocyclopropyl)-4-[4-(2-methoxyphenyl)piperidin-1-yl]quinazolin-6-yl}(methyl)amino]ethan-1-ol, Beta-adrenergic receptor kinase 1, GUANOSINE-5'-DIPHOSPHATE, ... | Authors: | Duan, J, Liu, H, Zhao, F, Yuan, Q, Ji, Y, Xu, H.E. | Deposit date: | 2023-06-11 | Release date: | 2023-08-09 | Last modified: | 2023-08-30 | Method: | ELECTRON MICROSCOPY (3.07 Å) | Cite: | GPCR activation and GRK2 assembly by a biased intracellular agonist. Nature, 620, 2023
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8JPD
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![BU of 8jpd by Molmil](/molmil-images/mine/8jpd) | Focused refinement structure of GRK2 in NTSR1-GRK2-Galpha(q) complexes | Descriptor: | Beta-adrenergic receptor kinase 1, STAUROSPORINE | Authors: | Duan, J, Liu, H, Zhao, F, Yuan, Q, Ji, Y, Xu, H.E. | Deposit date: | 2023-06-11 | Release date: | 2023-08-09 | Last modified: | 2023-08-30 | Method: | ELECTRON MICROSCOPY (2.81 Å) | Cite: | GPCR activation and GRK2 assembly by a biased intracellular agonist. Nature, 620, 2023
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4PNK
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![BU of 4pnk by Molmil](/molmil-images/mine/4pnk) | G protein-coupled receptor kinase 2 in complex with GSK180736A | Descriptor: | (4S)-4-(4-fluorophenyl)-N-(2H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | Authors: | Homan, K.T, Larimore, K.M, Elkins, J, Knapp, S, Tesmer, J.J.G. | Deposit date: | 2014-05-23 | Release date: | 2014-10-08 | Last modified: | 2023-12-27 | Method: | X-RAY DIFFRACTION (2.56 Å) | Cite: | Identification and structure-function analysis of subfamily selective g protein-coupled receptor kinase inhibitors. Acs Chem.Biol., 10, 2015
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2J59
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![BU of 2j59 by Molmil](/molmil-images/mine/2j59) | Crystal structure of the ARF1:ARHGAP21-ArfBD complex | Descriptor: | 1,2-ETHANEDIOL, 1,4-DIETHYLENE DIOXIDE, ADP-RIBOSYLATION FACTOR 1, ... | Authors: | Menetrey, J, Perderiset, M, Cicolari, J, Dubois, T, El Khatib, N, El Khadali, F, Franco, M, Chavrier, P, Houdusse, A. | Deposit date: | 2006-09-13 | Release date: | 2007-02-20 | Last modified: | 2023-12-13 | Method: | X-RAY DIFFRACTION (2.1 Å) | Cite: | Structural Basis for Arf1-Mediated Recruitment of Arhgap21 to Golgi Membranes. Embo J., 26, 2007
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7CSP
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![BU of 7csp by Molmil](/molmil-images/mine/7csp) | Structure of Ephexin4 IDPSH | Descriptor: | Rho guanine nucleotide exchange factor 16 | Authors: | Zhang, M, Lin, L, Wang, C, Zhu, J. | Deposit date: | 2020-08-15 | Release date: | 2021-02-24 | Last modified: | 2023-11-29 | Method: | X-RAY DIFFRACTION (3 Å) | Cite: | Double inhibition and activation mechanisms of Ephexin family RhoGEFs. Proc.Natl.Acad.Sci.USA, 118, 2021
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7CSR
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![BU of 7csr by Molmil](/molmil-images/mine/7csr) | Structure of Ephexin4 R676L | Descriptor: | Rho guanine nucleotide exchange factor 16 | Authors: | Zhang, M, Lin, L, Wang, C, Zhu, J. | Deposit date: | 2020-08-17 | Release date: | 2021-02-24 | Last modified: | 2023-11-29 | Method: | X-RAY DIFFRACTION (3 Å) | Cite: | Double inhibition and activation mechanisms of Ephexin family RhoGEFs. Proc.Natl.Acad.Sci.USA, 118, 2021
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7CSO
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![BU of 7cso by Molmil](/molmil-images/mine/7cso) | Structure of Ephexin4 DH-PH-SH3 | Descriptor: | Rho guanine nucleotide exchange factor 16, SULFATE ION | Authors: | Zhang, M, Lin, L, Wang, C, Zhu, J. | Deposit date: | 2020-08-15 | Release date: | 2021-02-24 | Last modified: | 2024-03-27 | Method: | X-RAY DIFFRACTION (2.39 Å) | Cite: | Double inhibition and activation mechanisms of Ephexin family RhoGEFs. Proc.Natl.Acad.Sci.USA, 118, 2021
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1OMW
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![BU of 1omw by Molmil](/molmil-images/mine/1omw) | Crystal Structure of the complex between G Protein-Coupled Receptor Kinase 2 and Heterotrimeric G Protein beta 1 and gamma 2 subunits | Descriptor: | 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 | Authors: | Lodowski, D.T, Pitcher, J.A, Capel, W.D, Lefkowitz, R.J, Tesmer, J.J.G. | Deposit date: | 2003-02-26 | Release date: | 2003-06-03 | Last modified: | 2023-08-16 | Method: | X-RAY DIFFRACTION (2.5 Å) | Cite: | 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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6BBP
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![BU of 6bbp by Molmil](/molmil-images/mine/6bbp) | Model for compact volume of truncated monomeric Cytohesin-3 (Grp1; amino acids 63-399) E161A 6GS Arf6 Q67L fusion protein | Descriptor: | Cytohesin-3,ADP-ribosylation factor 6, GUANOSINE-5'-TRIPHOSPHATE, INOSITOL-(1,3,4,5)-TETRAKISPHOSPHATE, ... | Authors: | Das, S, Malaby, A.W, Lambright, D.G. | Deposit date: | 2017-10-19 | Release date: | 2018-01-10 | Last modified: | 2023-11-29 | Method: | ELECTRON MICROSCOPY (35 Å) | Cite: | Structural Dynamics Control Allosteric Activation of Cytohesin Family Arf GTPase Exchange Factors. Structure, 26, 2018
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6BCA
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![BU of 6bca by Molmil](/molmil-images/mine/6bca) | |
7Z3J
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![BU of 7z3j by Molmil](/molmil-images/mine/7z3j) | Structure of crystallisable rat Phospholipase C gamma 1 in complex with inositol 1,4,5-trisphosphate | Descriptor: | 1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase gamma-1, CALCIUM ION, D-MYO-INOSITOL-1,4,5-TRIPHOSPHATE, ... | Authors: | Pinotsis, N, Bunney, T.D, Katan, M. | Deposit date: | 2022-03-02 | Release date: | 2022-07-20 | Last modified: | 2024-01-31 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | Characterization of the membrane interactions of phospholipase C gamma reveals key features of the active enzyme. Sci Adv, 8, 2022
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6C2Y
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![BU of 6c2y by Molmil](/molmil-images/mine/6c2y) | Human GRK2 in complex with Gbetagamma subunits and CCG257142 | Descriptor: | (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, ... | Authors: | Bouley, R, Tesmer, J.J.G. | Deposit date: | 2018-01-09 | Release date: | 2018-04-25 | Last modified: | 2023-10-04 | Method: | X-RAY DIFFRACTION (2.74 Å) | Cite: | 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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