1UNQ
 
 | | High resolution crystal structure of the Pleckstrin Homology Domain Of Protein Kinase B/Akt Bound To Ins(1,3,4,5)-Tetrakisphophate | | Descriptor: | INOSITOL-(1,3,4,5)-TETRAKISPHOSPHATE, RAC-ALPHA SERINE/THREONINE KINASE | | Authors: | Milburn, C.C, Deak, M, Kelly, S.M, Price, N.C, Alessi, D.R, van Aalten, D.M.F. | | Deposit date: | 2003-09-12 | | Release date: | 2004-09-16 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (0.98 Å) | | Cite: | Binding of phosphatidylinositol 3,4,5-trisphosphate to the pleckstrin homology domain of protein kinase B induces a conformational change.
Biochem. J., 375, 2003
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1UNR
 | | Crystal structure of the PH domain of PKB alpha in complex with a sulfate molecule | | Descriptor: | RAC-ALPHA SERINE/THREONINE KINASE, SULFATE ION | | Authors: | Milburn, C.C, Deak, M, Kelly, S.M, Price, N.C, Alessi, D.R, van Aalten, D.M.F. | | Deposit date: | 2003-09-15 | | Release date: | 2004-09-16 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (1.25 Å) | | Cite: | Binding of phosphatidylinositol 3,4,5-trisphosphate to the pleckstrin homology domain of protein kinase B induces a conformational change.
Biochem. J., 375, 2003
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7MYX
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1H10
 | | HIGH RESOLUTION STRUCTURE OF THE PLECKSTRIN HOMOLOGY DOMAIN OF PROTEIN KINASE B/AKT BOUND TO INS(1,3,4,5)-TETRAKISPHOPHATE | | Descriptor: | INOSITOL-(1,3,4,5)-TETRAKISPHOSPHATE, RAC-ALPHA SERINE/THREONINE KINASE | | Authors: | Thomas, C.C, Deak, M, Alessi, D.R, Van Aalten, D.M.F. | | Deposit date: | 2002-07-01 | | Release date: | 2003-06-27 | | Last modified: | 2019-05-22 | | Method: | X-RAY DIFFRACTION (1.4 Å) | | Cite: | High Resolution Structure of the Pleckstrin Homology Domain of Protein Kinase B/Akt Bound to Phosphatidylinositol (3,4,5)-Trisphosphate
Curr.Biol., 12, 2002
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8JOW
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4GV1
 | | PKB alpha in complex with AZD5363 | | Descriptor: | 4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide, GLYCEROL, RAC-alpha serine/threonine-protein kinase | | Authors: | Addie, M, Ballard, P, Bird, G, Buttar, D, Currie, G, Davies, B, Debreczeni, J, Dry, H, Dudley, P, Greenwood, R, Hatter, G, Jestel, A, Johnson, P.D, Kettle, J.G, Lane, C, Lamont, G, Leach, A, Luke, R.W.A, Ogilvie, D, Page, K, Pass, M, Steinbacher, S, Steuber, H, Pearson, S, Ruston, L. | | Deposit date: | 2012-08-30 | | Release date: | 2013-02-27 | | Last modified: | 2017-11-15 | | Method: | X-RAY DIFFRACTION (1.49 Å) | | Cite: | Discovery of 4-Amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363), an Orally Bioavailable, Potent Inhibitor of Akt Kinases.
J.Med.Chem., 56, 2013
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1UNP
 | | Crystal structure of the pleckstrin homology domain of PKB alpha | | Descriptor: | RAC-ALPHA SERINE/THREONINE KINASE | | Authors: | Milburn, C.C, Deak, M, Kelly, S.M, Price, N.C, Alessi, D.R, van Aalten, D.M.F. | | Deposit date: | 2003-09-12 | | Release date: | 2004-09-16 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (1.65 Å) | | Cite: | Binding of phosphatidylinositol 3,4,5-trisphosphate to the pleckstrin homology domain of protein kinase B induces a conformational change.
Biochem. J., 375, 2003
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7NH5
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3QKL
 | | Spirochromane Akt Inhibitors | | Descriptor: | GSK-3 beta peptide, N-{(2S)-3-[(3S)-8',9'-dihydro-1H,3'H-spiro[piperidine-3,7'-pyrano[3,2-e]indazol]-1-yl]-2-hydroxypropyl}-N-(2-ethoxyethyl)-2,6-dimethylbenzenesulfonamide, RAC-alpha serine/threonine-protein kinase | | Authors: | Kallan, N.C, Spencer, K.L, Blake, J.F, Xu, R, Heizer, J, Bencsik, J.R, Mitchell, I.S, Gloor, S.L, Martinson, M, Risom, T, Gross, S.D, Morales, T, Vigers, G.P.A, Brandhuber, B.J, Skelton, N.J. | | Deposit date: | 2011-02-01 | | Release date: | 2011-03-30 | | Last modified: | 2011-07-13 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Discovery and SAR of spirochromane Akt inhibitors.
Bioorg.Med.Chem.Lett., 21, 2011
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2UZR
 | | A transforming mutation in the pleckstrin homology domain of AKT1 in cancer (AKT1-PH_E17K) | | Descriptor: | RAC-alpha serine/threonine-protein kinase | | Authors: | Carpten, J.D, Faber, A.L, Horn, C, Donoho, G.P, Briggs, S.L, Robbins, C.M, Hostetter, G, Boguslawski, S, Moses, T.Y, Savage, S, Uhlik, M, Lin, A, Du, J, Qian, Y.W, Zeckner, D.J, Tucker-Kellogg, G, Touchman, J, Patel, K, Mousses, S, Bittner, M, Schevitz, R, Lai, M.H, Blanchard, K.L, Thomas, J.E. | | Deposit date: | 2007-05-01 | | Release date: | 2007-07-17 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (1.94 Å) | | Cite: | A transforming mutation in the pleckstrin homology domain of AKT1 in cancer.
Nature, 448, 2007
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2UVM
 | | Structure of PKBalpha PH domain in complex with a novel inositol headgroup surrogate, benzene 1,2,3,4-tetrakisphosphate | | Descriptor: | BENZENE-1,2,3,4-TETRAYL TETRAKIS[DIHYDROGEN (PHOSPHATE)], RAC-ALPHA SERINE/THREONINE-PROTEIN KINASE, SODIUM ION | | Authors: | Komander, D, Mills, S.J, Trusselle, M.N, Safrany, S.T, van Aalten, D.M.F, Potter, B.V.L. | | Deposit date: | 2007-03-12 | | Release date: | 2007-04-17 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (1.94 Å) | | Cite: | Novel Inositol Phospholipid Headgroup Surrogate Crystallised in the Pleckstrin Homology Domain of Protein Kinase Balpha.
Acs Chem.Biol., 2, 2007
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3CQW
 | | Crystal Structure of Akt-1 complexed with substrate peptide and inhibitor | | Descriptor: | 5-(5-chloro-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine, Glycogen synthase kinase-3 beta, MANGANESE (II) ION, ... | | Authors: | Pandit, J. | | Deposit date: | 2008-04-03 | | Release date: | 2008-05-27 | | Last modified: | 2021-10-20 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Synthesis and structure based optimization of novel Akt inhibitors
Bioorg.Med.Chem.Lett., 18, 2008
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4EKL
 | | Akt1 with GDC0068 | | Descriptor: | (2S)-2-(4-chlorophenyl)-1-{4-[(5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl]piperazin-1-yl}-3-(propan-2-ylamino)propan-1-one, RAC-alpha serine/threonine-protein kinase | | Authors: | Wu, W.-I, Vigers, G.P.A, Morales, T.H, Brandhuber, B.J. | | Deposit date: | 2012-04-09 | | Release date: | 2012-05-23 | | Last modified: | 2018-01-24 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | An ATP-Site On-Off Switch That Restricts Phosphatase Accessibility of Akt.
Sci.Signal., 5, 2012
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3MVH
 | | Crystal structure of Akt-1-inhibitor complexes | | Descriptor: | GSK3-beta peptide, MANGANESE (II) ION, N-{[(3S)-3-amino-1-(5-ethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrrolidin-3-yl]methyl}-2,4-difluorobenzamide, ... | | Authors: | Pandit, J. | | Deposit date: | 2010-05-04 | | Release date: | 2010-06-02 | | Last modified: | 2021-10-06 | | Method: | X-RAY DIFFRACTION (2.01 Å) | | Cite: | Design of selective, ATP-competitive inhibitors of Akt.
J.Med.Chem., 53, 2010
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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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6NPZ
 | | Crystal structure of Akt1 (aa 123-480) kinase with a bisubstrate | | Descriptor: | GLYCEROL, MANGANESE (II) ION, RAC-alpha serine/threonine-protein kinase, ... | | Authors: | Chu, N, Cole, P.A, Gabelli, S.B. | | Deposit date: | 2019-01-18 | | Release date: | 2019-01-30 | | Last modified: | 2024-07-10 | | Method: | X-RAY DIFFRACTION (2.12 Å) | | Cite: | Akt Kinase Activation Mechanisms Revealed Using Protein Semisynthesis.
Cell, 174, 2018
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6CCY
 | | Crystal structure of Akt1 in complex with a selective inhibitor | | Descriptor: | (5R)-4-(4-{4-[4-fluoro-3-(trifluoromethyl)phenyl]-1-[2-(pyrrolidin-1-yl)ethyl]-1H-imidazol-2-yl}piperidin-1-yl)-5-methyl-5,8-dihydropyrido[2,3-d]pyrimidin-7(6H)-one, RAC-alpha serine/threonine-protein kinase,PIFtide | | Authors: | Wang, Y, Stout, S. | | Deposit date: | 2018-02-07 | | Release date: | 2018-05-02 | | Last modified: | 2018-05-16 | | Method: | X-RAY DIFFRACTION (2.18 Å) | | Cite: | Discovery of chiral dihydropyridopyrimidinones as potent, selective and orally bioavailable inhibitors of AKT.
Bioorg. Med. Chem. Lett., 28, 2018
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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: | 2013-01-02 | | 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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3CQU
 | | Crystal Structure of Akt-1 complexed with substrate peptide and inhibitor | | Descriptor: | Glycogen synthase kinase-3 beta, N-[2-(5-methyl-4H-1,2,4-triazol-3-yl)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine, RAC-alpha serine/threonine-protein kinase | | Authors: | Pandit, J. | | Deposit date: | 2008-04-03 | | Release date: | 2008-05-27 | | Last modified: | 2021-10-20 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | Synthesis and structure based optimization of novel Akt inhibitors
Bioorg.Med.Chem.Lett., 18, 2008
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3QKM
 | | Spirocyclic sulfonamides as AKT inhibitors | | Descriptor: | N-(2-ethoxyethyl)-N-{(2S)-2-hydroxy-3-[(5R)-2-(quinazolin-4-yl)-2,7-diazaspiro[4.5]dec-7-yl]propyl}-2,6-dimethylbenzenesulfonamide, RAC-alpha serine/threonine-protein kinase | | Authors: | Xu, R, Banka, A, Blake, J.F, Mitchell, I.S, Wallace, E.M, Gloor, S.L, Martinson, M, Risom, T, Gross, S.D, Morales, T, Vigers, G.P.A, Brandhuber, B.J, Skelton, N.J. | | Deposit date: | 2011-02-01 | | Release date: | 2011-04-06 | | Last modified: | 2011-07-13 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | Discovery of spirocyclic sulfonamides as potent Akt inhibitors with exquisite selectivity against PKA.
Bioorg.Med.Chem.Lett., 21, 2011
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7NH4
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6HHG
 | | Crystal Structure of AKT1 in Complex with Covalent-Allosteric AKT Inhibitor 27 | | Descriptor: | RAC-alpha serine/threonine-protein kinase, ~{N}-[2-chloranyl-5-[[1-[[4-(5-oxidanylidene-3-phenyl-6~{H}-1,6-naphthyridin-2-yl)phenyl]methyl]piperidin-4-yl]carbamoylamino]phenyl]propanamide | | Authors: | Landel, I, Weisner, J, Mueller, M.P, Scheinpflug, R, Rauh, D. | | Deposit date: | 2018-08-28 | | Release date: | 2019-02-20 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Structural and chemical insights into the covalent-allosteric inhibition of the protein kinase Akt.
Chem Sci, 10, 2019
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6S9W
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6HHJ
 | | Crystal Structure of AKT1 in Complex with Covalent-Allosteric AKT Inhibitor 24b | | Descriptor: | RAC-alpha serine/threonine-protein kinase, ~{N}-[1-methyl-2-oxidanylidene-3-[1-[[4-(5-oxidanylidene-3-phenyl-6~{H}-1,6-naphthyridin-2-yl)phenyl]methyl]piperidin-4-yl]benzimidazol-5-yl]propanamide | | Authors: | Landel, I, Weisner, J, Mueller, M.P, Scheinpflug, R, Rauh, D. | | Deposit date: | 2018-08-28 | | Release date: | 2019-02-20 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Structural and chemical insights into the covalent-allosteric inhibition of the protein kinase Akt.
Chem Sci, 10, 2019
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3QKK
 | | Spirochromane Akt Inhibitors | | Descriptor: | GSK-3 beta peptide, N-(2-ethoxyethyl)-N-{(2S)-2-hydroxy-3-[(2R)-6-hydroxy-4-oxo-3,4-dihydro-1'H-spiro[chromene-2,3'-piperidin]-1'-yl]propyl}-2,6-dimethylbenzenesulfonamide, RAC-alpha serine/threonine-protein kinase | | Authors: | Kallan, N.C, Spencer, K.L, Blake, J.F, Xu, R, Heizer, J, Bencsik, J.R, Mitchell, I.S, Gloor, S.L, Martinson, M, Risom, T, Gross, S.D, Morales, T, Vigers, G.P.A, Brandhuber, B.J, Skelton, N.J. | | Deposit date: | 2011-02-01 | | Release date: | 2011-03-30 | | Last modified: | 2011-07-13 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Discovery and SAR of spirochromane Akt inhibitors.
Bioorg.Med.Chem.Lett., 21, 2011
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