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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6E4F
 | | Crystal structure of ARQ 531 in complex with the kinase domain of BTK | | Descriptor: | 1,2-ETHANEDIOL, 1,5-anhydro-2-{[5-(2-chloro-4-phenoxybenzene-1-carbonyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino}-2,3,4-trideoxy-D-erythro-hexitol, IMIDAZOLE, ... | | Authors: | Eathiraj, S. | | Deposit date: | 2018-07-17 | | Release date: | 2018-09-05 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (1.15 Å) | | Cite: | The BTK Inhibitor ARQ 531 Targets Ibrutinib-Resistant CLL and Richter Transformation.
Cancer Discov, 8, 2018
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3MJH
 | | Crystal Structure of Human Rab5A in complex with the C2H2 Zinc Finger of EEA1 | | Descriptor: | Early endosome antigen 1, GUANOSINE-5'-TRIPHOSPHATE, MAGNESIUM ION, ... | | Authors: | Mishra, A.K, Eathiraj, S, Lambright, D.G. | | Deposit date: | 2010-04-12 | | Release date: | 2010-05-05 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (2.03 Å) | | Cite: | Structural basis for Rab GTPase recognition and endosome tethering by the C2H2 zinc finger of Early Endosomal Autoantigen 1 (EEA1).
Proc.Natl.Acad.Sci.USA, 107, 2010
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2G77
 | | Crystal Structure of Gyp1 TBC domain in complex with Rab33 GTPase bound to GDP and AlF3 | | Descriptor: | ALUMINUM FLUORIDE, GTPase-activating protein GYP1, GUANOSINE-5'-DIPHOSPHATE, ... | | Authors: | Pan, X, Eathiraj, S, Munson, M, Lambright, D.G. | | Deposit date: | 2006-02-27 | | Release date: | 2006-07-25 | | Last modified: | 2021-10-20 | | Method: | X-RAY DIFFRACTION (2.26 Å) | | Cite: | TBC-domain GAPs for Rab GTPases accelerate GTP hydrolysis by a dual-finger mechanism.
Nature, 442, 2006
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