4EJN
 
 | | Crystal structure of autoinhibited form of AKT1 in complex with N-(4-(5-(3-acetamidophenyl)-2-(2-aminopyridin-3-yl)-3H-imidazo[4,5-b]pyridin-3-yl)benzyl)-3-fluorobenzamide | | Descriptor: | 1,2-ETHANEDIOL, 2-BUTANOL, N-(4-{5-[3-(acetylamino)phenyl]-2-(2-aminopyridin-3-yl)-3H-imidazo[4,5-b]pyridin-3-yl}benzyl)-3-fluorobenzamide, ... | | Authors: | Eathiraj, S. | | Deposit date: | 2012-04-06 | | Release date: | 2012-05-23 | | Last modified: | 2024-10-16 | | Method: | X-RAY DIFFRACTION (2.19 Å) | | Cite: | Discovery and optimization of a series of 3-(3-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amines: orally bioavailable, selective, and potent ATP-independent Akt inhibitors.
J.Med.Chem., 55, 2012
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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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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: | 2024-11-06 | | 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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2HV8
 | | Crystal structure of GTP-bound Rab11 in complex with FIP3 | | Descriptor: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, GUANOSINE-5'-TRIPHOSPHATE, MAGNESIUM ION, ... | | Authors: | Eathiraj, S, Mishra, A, Prekeris, R, Lambright, D.G. | | Deposit date: | 2006-07-27 | | Release date: | 2006-11-21 | | Last modified: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (1.86 Å) | | Cite: | Structural Basis for Rab11-mediated Recruitment of FIP3 to Recycling Endosomes.
J.Mol.Biol., 364, 2006
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3RHK
 | | Crystal structure of the catalytic domain of c-Met kinase in complex with ARQ 197 | | Descriptor: | 1-[(3R,4R)-4-(1H-indol-3-yl)-2,5-dioxopyrrolidin-3-yl]pyrrolo[3,2,1-ij]quinolinium, Hepatocyte growth factor receptor | | Authors: | Eathiraj, S, Palma, R, Volckova, E, Hirschi, M, France, D.S, Ashwell, M.A, Chan, T.C. | | Deposit date: | 2011-04-11 | | Release date: | 2011-04-27 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (1.94 Å) | | Cite: | Discovery of a novel mode of protein kinase inhibition characterized by the mechanism of inhibition of human mesenchymal-epithelial transition factor (c-Met) protein autophosphorylation by ARQ 197.
J.Biol.Chem., 286, 2011
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3RHX
 | | Crystal structure of the catalytic domain of FGFR1 kinase in complex with ARQ 069 | | Descriptor: | (6S)-6-phenyl-5,6-dihydrobenzo[h]quinazolin-2-amine, 1,2-ETHANEDIOL, Basic fibroblast growth factor receptor 1, ... | | Authors: | Eathiraj, S, Palma, R, Hirschi, M, Volckova, E, Nakuci, E, Castro, J, Chen, C.R, Chan, T.C, France, D.S, Ashwell, M.A. | | Deposit date: | 2011-04-12 | | Release date: | 2011-05-04 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (2.01 Å) | | Cite: | A novel mode of protein kinase inhibition exploiting hydrophobic motifs of autoinhibited kinases: discovery of ATP-independent inhibitors of fibroblast growth factor receptor.
J.Biol.Chem., 286, 2011
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3RI1
 | | Crystal structure of the catalytic domain of FGFR2 kinase in complex with ARQ 069 | | Descriptor: | (6S)-6-phenyl-5,6-dihydrobenzo[h]quinazolin-2-amine, Fibroblast growth factor receptor 2, SULFATE ION | | Authors: | Eathiraj, S, Palma, R, Hirschi, M, Volckova, E, Nakuci, E, Castro, J, Chen, C.R, Chan, T.C, France, D.S, Ashwell, M.A. | | Deposit date: | 2011-04-12 | | Release date: | 2011-05-04 | | Last modified: | 2024-10-30 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | A novel mode of protein kinase inhibition exploiting hydrophobic motifs of autoinhibited kinases: discovery of ATP-independent inhibitors of fibroblast growth factor receptor.
J.Biol.Chem., 286, 2011
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1YZK
 | | GppNHp bound Rab11 GTPase | | Descriptor: | MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-GUANYLATE ESTER, Ras-related protein Rab-11A | | Authors: | Eathiraj, S, Pan, X, Ritacco, C, Lambright, D.G. | | Deposit date: | 2005-02-28 | | Release date: | 2005-07-26 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Structural basis of family-wide Rab GTPase recognition by rabenosyn-5.
Nature, 436, 2005
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1YZQ
 | | GppNHp-Bound Rab6 GTPase | | Descriptor: | MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-GUANYLATE ESTER, small GTP binding protein RAB6 isoform | | Authors: | Eathiraj, S, Pan, X, Ritacco, C, Lambright, D.G. | | Deposit date: | 2005-02-28 | | Release date: | 2005-07-26 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (1.78 Å) | | Cite: | Structural basis of family-wide Rab GTPase recognition by rabenosyn-5.
Nature, 436, 2005
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1YZM
 | | Structure of Rabenosyn (458-503), Rab4 binding domain | | Descriptor: | FYVE-finger-containing Rab5 effector protein rabenosyn-5 | | Authors: | Eathiraj, S, Pan, X, Ritacco, C, Lambright, D.G. | | Deposit date: | 2005-02-28 | | Release date: | 2005-07-26 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (1.5 Å) | | Cite: | Structural basis of family-wide Rab GTPase recognition by rabenosyn-5.
Nature, 436, 2005
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1YZU
 | | GppNHp-Bound Rab21 GTPase at 2.50 A Resolution | | Descriptor: | MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-GUANYLATE ESTER, Ras-related protein Rab-21 | | Authors: | Eathiraj, S, Pan, X, Ritacco, C, Lambright, D.G. | | Deposit date: | 2005-02-28 | | Release date: | 2005-07-26 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Structural basis of family-wide Rab GTPase recognition by rabenosyn-5.
Nature, 436, 2005
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1Z0A
 | | GDP-Bound Rab2A GTPase | | Descriptor: | GUANOSINE-5'-DIPHOSPHATE, MAGNESIUM ION, Ras-related protein Rab-2A | | Authors: | Eathiraj, S, Pan, X, Ritacco, C, Lambright, D.G. | | Deposit date: | 2005-03-01 | | Release date: | 2005-07-26 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (2.12 Å) | | Cite: | Structural basis of family-wide Rab GTPase recognition by rabenosyn-5.
Nature, 436, 2005
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1Z0J
 | | Structure of GTP-Bound Rab22Q64L GTPase in complex with the minimal Rab binding domain of Rabenosyn-5 | | Descriptor: | 2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, FYVE-finger-containing Rab5 effector protein rabenosyn-5, GLYCEROL, ... | | Authors: | Eathiraj, S, Pan, X, Ritacco, C, Lambright, D.G. | | Deposit date: | 2005-03-01 | | Release date: | 2005-07-26 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (1.32 Å) | | Cite: | Structural basis of family-wide Rab GTPase recognition by rabenosyn-5.
Nature, 436, 2005
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1YZL
 | | GppNHp-Bound Rab9 GTPase | | Descriptor: | MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-GUANYLATE ESTER, Ras-related protein Rab-9A | | Authors: | Eathiraj, S, Pan, X, Ritacco, C, Lambright, D.G. | | Deposit date: | 2005-02-28 | | Release date: | 2005-07-26 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (1.85 Å) | | Cite: | Structural basis of family-wide Rab GTPase recognition by rabenosyn-5.
Nature, 436, 2005
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1Z0I
 | | GDP-Bound Rab21 GTPase | | Descriptor: | GUANOSINE-5'-DIPHOSPHATE, MAGNESIUM ION, Ras-related protein Rab-21 | | Authors: | Eathiraj, S, Pan, X, Ritacco, C, Lambright, D.G. | | Deposit date: | 2005-03-01 | | Release date: | 2005-07-26 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (2.33 Å) | | Cite: | Structural basis of family-wide Rab GTPase recognition by rabenosyn-5.
Nature, 436, 2005
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1Z2A
 | | GDP-Bound Rab23 GTPase crystallized in P2(1)2(1)2(1) space group | | Descriptor: | GUANOSINE-5'-DIPHOSPHATE, MAGNESIUM ION, Ras-related protein Rab-23 | | Authors: | Eathiraj, S, Pan, X, Ritacco, C, Lambright, D.G. | | Deposit date: | 2005-03-07 | | Release date: | 2005-07-26 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Structural basis of family-wide Rab GTPase recognition by rabenosyn-5.
Nature, 436, 2005
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1Z0F
 | | GDP-Bound Rab14 GTPase | | Descriptor: | GUANOSINE-5'-DIPHOSPHATE, MAGNESIUM ION, RAB14, ... | | Authors: | Eathiraj, S, Pan, X, Ritacco, C, Lambright, D.G. | | Deposit date: | 2005-03-01 | | Release date: | 2005-07-26 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (2.15 Å) | | Cite: | Structural basis of family-wide Rab GTPase recognition by rabenosyn-5.
Nature, 436, 2005
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1Z06
 | | GppNHp-Bound Rab33 GTPase | | Descriptor: | MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-GUANYLATE ESTER, Ras-related protein Rab-33B | | Authors: | Eathiraj, S, Pan, X, Ritacco, C, Lambright, D.G. | | Deposit date: | 2005-03-01 | | Release date: | 2005-07-26 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (1.81 Å) | | Cite: | Structural basis of family-wide Rab GTPase recognition by rabenosyn-5.
Nature, 436, 2005
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1Z0D
 | | GDP-Bound Rab5c GTPase | | Descriptor: | GUANOSINE-5'-DIPHOSPHATE, MAGNESIUM ION, PHOSPHATE ION, ... | | Authors: | Eathiraj, S, Pan, X, Ritacco, C, Lambright, D.G. | | Deposit date: | 2005-03-01 | | Release date: | 2005-07-26 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | Structural basis of family-wide Rab GTPase recognition by rabenosyn-5.
Nature, 436, 2005
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1Z22
 | | GDP-Bound Rab23 GTPase crystallized in C222(1) space group | | Descriptor: | GUANOSINE-5'-DIPHOSPHATE, MAGNESIUM ION, Ras-related protein Rab-23 | | Authors: | Eathiraj, S, Pan, X, Ritacco, C, Lambright, D.G. | | Deposit date: | 2005-03-07 | | Release date: | 2005-07-26 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (2.06 Å) | | Cite: | Structural basis of family-wide Rab GTPase recognition by rabenosyn-5.
Nature, 436, 2005
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1YZT
 | | GppNHp-Bound Rab21 GTPase at 2.05 A Resolution | | Descriptor: | MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-GUANYLATE ESTER, Ras-related protein Rab-21 | | Authors: | Eathiraj, S, Pan, X, Ritacco, C, Lambright, D.G. | | Deposit date: | 2005-02-28 | | Release date: | 2005-07-26 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (2.05 Å) | | Cite: | Structural basis of family-wide Rab GTPase recognition by rabenosyn-5.
Nature, 436, 2005
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1YVD
 | | GppNHp-Bound Rab22 GTPase | | Descriptor: | MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-GUANYLATE ESTER, Ras-related protein Rab-22A | | Authors: | Eathiraj, S, Pan, X, Ritacco, C, Lambright, D.G. | | Deposit date: | 2005-02-15 | | Release date: | 2005-07-26 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (1.93 Å) | | Cite: | Structural basis of family-wide Rab GTPase recognition by rabenosyn-5.
Nature, 436, 2005
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1Z07
 | | GppNHp-Bound Rab5c G55Q mutant GTPase | | Descriptor: | MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-GUANYLATE ESTER, Ras-related protein Rab-5C | | Authors: | Eathiraj, S, Pan, X, Ritacco, C, Lambright, D.G. | | Deposit date: | 2005-03-01 | | Release date: | 2005-07-26 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (1.81 Å) | | Cite: | Structural basis of family-wide Rab GTPase recognition by rabenosyn-5.
Nature, 436, 2005
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1YU9
 | | GppNHp-Bound Rab4A | | Descriptor: | GTP-binding protein, MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-GUANYLATE ESTER, ... | | Authors: | Eathiraj, S, Pan, X, Ritacco, C, Lambright, D.G. | | Deposit date: | 2005-02-13 | | Release date: | 2005-07-26 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (2.07 Å) | | Cite: | Structural basis of family-wide Rab GTPase recognition by rabenosyn-5.
Nature, 436, 2005
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1Z0K
 | | Structure of GTP-Bound Rab4Q67L GTPase in complex with the central Rab binding domain of Rabenosyn-5 | | Descriptor: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, FYVE-finger-containing Rab5 effector protein rabenosyn-5, GTP-binding protein, ... | | Authors: | Eathiraj, S, Pan, X, Ritacco, C, Lambright, D.G. | | Deposit date: | 2005-03-01 | | Release date: | 2005-07-26 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (1.92 Å) | | Cite: | Structural basis of family-wide Rab GTPase recognition by rabenosyn-5.
Nature, 436, 2005
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