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
|
|
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: | 2024-10-16 | 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
|
|
7MYX
| |
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
|
|
8JOW
| |
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: | 2024-10-16 | 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
|
|
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
|
|
8UW9
| Structure of AKT1(E17K) with compound 4 | Descriptor: | 1,2-ETHANEDIOL, CHLORIDE ION, N-({4-[(2P)-2-(2-aminopyridin-3-yl)-5-phenyl-3H-imidazo[4,5-b]pyridin-3-yl]phenyl}methyl)-2-(2-fluoro-4-formyl-3-hydroxyphenyl)acetamide, ... | Authors: | Craven, G.B, Taunton, J. | Deposit date: | 2023-11-06 | Release date: | 2024-09-04 | Method: | X-RAY DIFFRACTION (1.9 Å) | Cite: | Mutant-selective AKT1 inhibitors via lysine targeting and neo-zinc chelation To Be Published
|
|
7NH5
| |
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
|
|
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: | 2024-10-16 | Method: | X-RAY DIFFRACTION (1.94 Å) | Cite: | A transforming mutation in the pleckstrin homology domain of AKT1 in cancer. Nature, 448, 2007
|
|
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
|
|
8UW7
| Structure of AKT1(WT) with compound 3 | Descriptor: | 1,2-ETHANEDIOL, 4-{2-[({4-[(2P)-2-(2-aminopyridin-3-yl)-5-phenyl-3H-imidazo[4,5-b]pyridin-3-yl]phenyl}methyl)amino]ethyl}-2-hydroxybenzaldehyde, NB41, ... | Authors: | Craven, G.B, Taunton, J. | Deposit date: | 2023-11-06 | Release date: | 2024-09-04 | Method: | X-RAY DIFFRACTION (1.972 Å) | Cite: | Mutant-selective AKT1 inhibitors via lysine targeting and neo-zinc chelation To Be Published
|
|
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
|
|
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
|
|
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: | 2024-10-16 | Method: | X-RAY DIFFRACTION (2.01 Å) | Cite: | Design of selective, ATP-competitive inhibitors of Akt. J.Med.Chem., 53, 2010
|
|
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
|
|
8UVY
| Structure of AKT1(E17K) with compound 3 | Descriptor: | 1,2-ETHANEDIOL, 4-{2-[({4-[(2P)-2-(2-aminopyridin-3-yl)-5-phenyl-3H-imidazo[4,5-b]pyridin-3-yl]phenyl}methyl)amino]ethyl}-2-hydroxybenzaldehyde, NB41, ... | Authors: | Craven, G.B, Taunton, J. | Deposit date: | 2023-11-05 | Release date: | 2024-09-04 | Method: | X-RAY DIFFRACTION (2.11 Å) | Cite: | Mutant-selective AKT1 inhibitors via lysine targeting and neo-zinc chelation To Be Published
|
|
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: | 2024-10-16 | Method: | X-RAY DIFFRACTION (2.12 Å) | Cite: | Akt Kinase Activation Mechanisms Revealed Using Protein Semisynthesis. Cell, 174, 2018
|
|
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
|
|
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
|
|
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
|
|
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
|
|
8UW2
| Structure of AKT1(E17K) with compound 3 (zinc-free) | Descriptor: | 1,2-ETHANEDIOL, 4-{2-[({4-[(2P)-2-(2-aminopyridin-3-yl)-5-phenyl-3H-imidazo[4,5-b]pyridin-3-yl]phenyl}methyl)amino]ethyl}-2-hydroxybenzaldehyde, NB41, ... | Authors: | Craven, G.B, Taunton, J. | Deposit date: | 2023-11-05 | Release date: | 2024-09-04 | Last modified: | 2024-10-16 | Method: | X-RAY DIFFRACTION (2.2 Å) | Cite: | Mutant-selective AKT1 inhibitors via lysine targeting and neo-zinc chelation To Be Published
|
|
6S9W
| |