2WXK
 
 | | The crystal structure of the murine class IA PI 3-kinase p110delta in complex with INK666. | | 分子名称: | 3-(2-amino-1,3-benzothiazol-6-yl)-1-{[2-(4-methylpiperazin-1-yl)quinolin-3-yl]methyl}-1H-pyrazolo[3,4-d]pyrimidin-4-amine, PHOSPHATIDYLINOSITOL-4,5-BISPHOSPHATE 3-KINASE CATALYTIC SUBUNIT DELTA ISOFORM | | 著者 | Berndt, A, Miller, S, Williams, O, Lee, D.D, Houseman, B.T, Pacold, J.I, Gorrec, F, Hon, W.-C, Liu, Y, Rommel, C, Gaillard, P, Ruckle, T, Schwarz, M.K, Shokat, K.M, Shaw, J.P, Williams, R.L. | | 登録日 | 2009-11-09 | | 公開日 | 2010-01-12 | | 最終更新日 | 2023-12-20 | | 実験手法 | X-RAY DIFFRACTION (2.9 Å) | | 主引用文献 | The P110D Structure: Mechanisms for Selectivity and Potency of New Pi(3)K Inhibitors
Nat.Chem.Biol., 6, 2010
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2WXN
 | | The crystal structure of the murine class IA PI 3-kinase p110delta in complex with DL07. | | 分子名称: | 3-{[4-amino-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]ethynyl}phenol, PHOSPHATIDYLINOSITOL-4,5-BISPHOSPHATE 3-KINASE CATALYTIC SUBUNIT DELTA ISOFORM | | 著者 | Berndt, A, Miller, S, Williams, O, Lee, D.D, Houseman, B.T, Pacold, J.I, Gorrec, F, Hon, W.-C, Liu, Y, Rommel, C, Gaillard, P, Ruckle, T, Schwarz, M.K, Shokat, K.M, Shaw, J.P, Williams, R.L. | | 登録日 | 2009-11-09 | | 公開日 | 2010-01-12 | | 最終更新日 | 2023-12-20 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | The P110D Structure: Mechanisms for Selectivity and Potency of New Pi(3)K Inhibitors
Nat.Chem.Biol., 6, 2010
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2WXL
 | | The crystal structure of the murine class IA PI 3-kinase p110delta in complex with ZSTK474. | | 分子名称: | 2-(difluoromethyl)-1-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)-1H-benzimidazole, PHOSPHATIDYLINOSITOL-4,5-BISPHOSPHATE 3-KINASE CATALYTIC SUBUNIT DELTA ISOFORM | | 著者 | Berndt, A, Miller, S, Williams, O, Lee, D.D, Houseman, B.T, Pacold, J.I, Gorrec, F, Hon, W.-C, Liu, Y, Rommel, C, Gaillard, P, Ruckle, T, Schwarz, M.K, Shokat, K.M, Shaw, J.P, Williams, R.L. | | 登録日 | 2009-11-09 | | 公開日 | 2010-01-12 | | 最終更新日 | 2023-12-20 | | 実験手法 | X-RAY DIFFRACTION (1.99 Å) | | 主引用文献 | The P110D Structure: Mechanisms for Selectivity and Potency of New Pi(3)K Inhibitors
Nat.Chem.Biol., 6, 2010
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2WXH
 | | The crystal structure of the murine class IA PI 3-kinase p110delta in complex with SW14. | | 分子名称: | 2-{[4-amino-3-(3-fluoro-4-hydroxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]methyl}-5-methyl-3-(2-methylphenyl)quinazolin-4(3H)-one, PHOSPHATIDYLINOSITOL-4,5-BISPHOSPHATE 3-KINASE CATALYTIC SUBUNIT DELTA ISOFORM | | 著者 | Berndt, A, Miller, S, Williams, O, Lee, D.D, Houseman, B.T, Pacold, J.I, Gorrec, F, Hon, W.-C, Liu, Y, Rommel, C, Gaillard, P, Ruckle, T, Schwarz, M.K, Shokat, K.M, Shaw, J.P, Williams, R.L. | | 登録日 | 2009-11-09 | | 公開日 | 2010-01-12 | | 最終更新日 | 2023-12-20 | | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | | 主引用文献 | The P110D Structure: Mechanisms for Selectivity and Potency of New Pi(3)K Inhibitors
Nat.Chem.Biol., 6, 2010
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2WXQ
 | | The crystal structure of the murine class IA PI 3-kinase p110delta in complex with AS15. | | 分子名称: | 2-{[3-(2-METHOXYPHENYL)-4-OXO-3,4,5,6,7,8-HEXAHYDROQUINAZOLIN-2-YL]SULFANYL}-N-QUINOXALIN-6-YLACETAMIDE, PHOSPHATIDYLINOSITOL-4,5-BISPHOSPHATE 3-KINASE CATALYTIC SUBUNIT DELTA ISOFORM | | 著者 | Berndt, A, Miller, S, Williams, O, Lee, D.D, Houseman, B.T, Pacold, J.I, Gorrec, F, Hon, W.-C, Liu, Y, Rommel, C, Gaillard, P, Ruckle, T, Schwarz, M.K, Shokat, K.M, Shaw, J.P, Williams, R.L. | | 登録日 | 2009-11-09 | | 公開日 | 2010-01-12 | | 最終更新日 | 2023-12-20 | | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | | 主引用文献 | The P110D Structure: Mechanisms for Selectivity and Potency of New Pi(3)K Inhibitors
Nat.Chem.Biol., 6, 2010
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2WXG
 | | The crystal structure of the murine class IA PI 3-kinase p110delta in complex with SW13. | | 分子名称: | 2-{[4-amino-3-(3-fluoro-5-hydroxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]methyl}-5-methyl-3-(2-methylphenyl)quinazolin-4(3H)-one, PHOSPHATIDYLINOSITOL-4,5-BISPHOSPHATE 3-KINASE CATALYTIC SUBUNIT DELTA ISOFORM | | 著者 | Berndt, A, Miller, S, Williams, O, Lee, D.D, Houseman, B.T, Pacold, J.I, Gorrec, F, Hon, W.-C, Liu, Y, Rommel, C, Gaillard, P, Ruckle, T, Schwarz, M.K, Shokat, K.M, Shaw, J.P, Williams, R.L. | | 登録日 | 2009-11-09 | | 公開日 | 2010-01-12 | | 最終更新日 | 2023-12-20 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | The P110D Structure: Mechanisms for Selectivity and Potency of New Pi(3)K Inhibitors
Nat.Chem.Biol., 6, 2010
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3IHY
 | | Human PIK3C3 crystal structure | | 分子名称: | Phosphatidylinositol 3-kinase catalytic subunit type 3 | | 著者 | Siponen, M.I, Tresaugues, L, Arrowsmith, C.H, Berglund, H, Bountra, C, Collins, R, Edwards, A.M, Flodin, S, Flores, A, Graslund, S, Hammarstrom, M, Johansson, A, Johansson, I, Karlberg, T, Kotenyova, T, Kotzsch, A, Kragh Nielsen, T, Moche, M, Nyman, T, Persson, C, Roos, A.K, Sagemark, J, Schueler, H, Schutz, P, Thorsell, A.G, Van Den Berg, S, Weigelt, J, Welin, M, Wisniewska, M, Nordlund, P, Structural Genomics Consortium (SGC) | | 登録日 | 2009-07-31 | | 公開日 | 2009-10-13 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Human PIK3C3 crystal structure
TO BE PUBLISHED
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3HHM
 | | Crystal structure of p110alpha H1047R mutant in complex with niSH2 of p85alpha and the drug wortmannin | | 分子名称: | (1S,6BR,9AS,11R,11BR)-9A,11B-DIMETHYL-1-[(METHYLOXY)METHYL]-3,6,9-TRIOXO-1,6,6B,7,8,9,9A,10,11,11B-DECAHYDRO-3H-FURO[4, 3,2-DE]INDENO[4,5-H][2]BENZOPYRAN-11-YL ACETATE, Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha isoform, ... | | 著者 | Amzel, L.M, Vogelstein, B, Gabelli, S.B, Mandelker, D. | | 登録日 | 2009-05-15 | | 公開日 | 2009-09-29 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | A frequent kinase domain mutation that changes the interaction between PI3K{alpha} and the membrane.
Proc.Natl.Acad.Sci.USA, 106, 2009
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3HIZ
 | | Crystal structure of p110alpha H1047R mutant in complex with niSH2 of p85alpha | | 分子名称: | Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | | 著者 | Amzel, L.M, Vogelstein, B, Gabelli, S.B, Mandelker, D. | | 登録日 | 2009-05-20 | | 公開日 | 2009-09-29 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (3.3 Å) | | 主引用文献 | A frequent kinase domain mutation that changes the interaction between PI3K{alpha} and the membrane.
Proc.Natl.Acad.Sci.USA, 106, 2009
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3IBE
 | | Crystal Structure of a Pyrazolopyrimidine Inhibitor Bound to PI3 Kinase Gamma | | 分子名称: | 1-(4-{4-morpholin-4-yl-1-[1-(pyridin-3-ylcarbonyl)piperidin-4-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-yl}phenyl)-3-pyridin-4-ylurea, Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, SULFATE ION | | 著者 | Bard, J, Svenson, K. | | 登録日 | 2009-07-15 | | 公開日 | 2009-09-01 | | 最終更新日 | 2023-09-06 | | 実験手法 | X-RAY DIFFRACTION (2.798 Å) | | 主引用文献 | ATP-Competitive Inhibitors of the Mammalian Target of Rapamycin: Design and Synthesis of Highly Potent and Selective Pyrazolopyrimidines.
J.Med.Chem., 52, 2009
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3ENE
 | | Complex of PI3K gamma with an inhibitor | | 分子名称: | 1-methyl-3-naphthalen-2-yl-1H-pyrazolo[3,4-d]pyrimidin-4-amine, Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma isoform | | 著者 | Apsel, B, Blair, J.A, Gonzalez, B.Z, Nazif, T.M, Feldman, M.E, Williams, R.L, Shokat, K.M, Knight, Z.A. | | 登録日 | 2008-09-25 | | 公開日 | 2008-10-14 | | 最終更新日 | 2023-11-01 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases
Nat.Chem.Biol., 4, 2008
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2V4L
 | | complex of human phosphoinositide 3-kinase catalytic subunit gamma (p110 gamma) with PIK-284 | | 分子名称: | 3-[4-AMINO-1-(1-METHYLETHYL)-1H-PYRAZOLO[3,4-D]PYRIMIDIN-3-YL]PHENOL, PHOSPHATIDYLINOSITOL-4,5-BISPHOSPHATE 3-KINASE CATALYTIC SUBUNIT GAMMA ISOFORM | | 著者 | Apsel, B, Gonzalez, B, Blair, J.A, Nazif, T.M, Feldman, M.E, Williams, R.L, Shokat, K.M, Knight, Z.A. | | 登録日 | 2008-09-25 | | 公開日 | 2008-10-14 | | 最終更新日 | 2023-12-13 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | Targeted Polypharmacology: Discovery of Dual Inhibitors of Tyrosine and Phosphoinositide Kinases.
Nat.Chem.Biol., 4, 2008
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3DPD
 | | Achieving multi-isoform PI3K inhibition in a series of substituted 3,4-Dihydro-2H-benzo[1,4]oxazines | | 分子名称: | 5,5-dimethyl-2-morpholin-4-yl-5,6-dihydro-1,3-benzothiazol-7(4H)-one, Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma isoform | | 著者 | Ceska, T.A. | | 登録日 | 2008-07-08 | | 公開日 | 2008-08-26 | | 最終更新日 | 2023-11-01 | | 実験手法 | X-RAY DIFFRACTION (2.85 Å) | | 主引用文献 | Achieving multi-isoform PI3K inhibition in a series of substituted 3,4-dihydro-2H-benzo[1,4]oxazines
Bioorg.Med.Chem.Lett., 18, 2008
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3DBS
 | | Structure of PI3K gamma in complex with GDC0941 | | 分子名称: | 2-(1H-indazol-4-yl)-6-{[4-(methylsulfonyl)piperazin-1-yl]methyl}-4-morpholin-4-yl-thieno[3,2-d]pyrimidine, Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma isoform | | 著者 | Wiesmann, C, Ultsch, M. | | 登録日 | 2008-06-02 | | 公開日 | 2008-06-17 | | 最終更新日 | 2023-11-01 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer
J.Med.Chem., 51, 2008
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3CSF
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3CST
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2RD0
 | | Structure of a human p110alpha/p85alpha complex | | 分子名称: | Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | | 著者 | Huang, C, Gabelli, S.B, Amzel, L.M. | | 登録日 | 2007-09-20 | | 公開日 | 2007-12-25 | | 最終更新日 | 2024-02-21 | | 実験手法 | X-RAY DIFFRACTION (3.05 Å) | | 主引用文献 | The structure of a human p110alpha/p85alpha complex elucidates the effects of oncogenic PI3Kalpha mutations.
Science, 318, 2007
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2CHZ
 | | A pharmacological map of the PI3-K family defines a role for p110alpha in signaling: The structure of complex of phosphoinositide 3-kinase gamma with inhibitor PIK-93 | | 分子名称: | N-(5-(4-CHLORO-3-(2-HYDROXY-ETHYLSULFAMOYL)- PHENYLTHIAZOLE-2-YL)-ACETAMIDE, PHOSPHATIDYLINOSITOL-4,5-BISPHOSPHATE 3-KINASE CATALYTIC SUBUNIT GAMMA ISOFORM | | 著者 | Knight, Z.A, Gonzalez, B, Feldman, M.E, Zunder, E.R, Goldenberg, D.D, Williams, O, Loewith, R, Stokoe, D, Balla, A, Toth, B, Balla, T, Weiss, W.A, Williams, R.L, Shokat, K.M. | | 登録日 | 2006-03-16 | | 公開日 | 2006-05-22 | | 最終更新日 | 2023-12-13 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | A Pharmacological Map of the Pi3-K Family Defines a Role for P110Alpha in Signaling
Cell(Cambridge,Mass.), 125, 2006
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2CHX
 | | A pharmacological map of the PI3-K family defines a role for p110alpha in signaling: The structure of complex of phosphoinositide 3-kinase gamma with inhibitor PIK-90 | | 分子名称: | N-(2,3-DIHYDRO-7,8-DIMETHOXYIMIDAZO[1,2-C] QUINAZOLIN-5-YL)NICOTINAMIDE, PHOSPHATIDYLINOSITOL-4,5-BISPHOSPHATE 3-KINASE CATALYTIC SUBUNIT GAMMA ISOFORM | | 著者 | Knight, Z.A, Gonzalez, B, Feldman, M.E, Zunder, E.R, Goldenberg, D.D, Williams, O, Loewith, R, Stokoe, D, Balla, A, Toth, B, Balla, T, Weiss, W.A, Williams, R.L, Shokat, K.M. | | 登録日 | 2006-03-16 | | 公開日 | 2006-05-22 | | 最終更新日 | 2023-12-13 | | 実験手法 | X-RAY DIFFRACTION (2.5 Å) | | 主引用文献 | A Pharmacological Map of the Pi3-K Family Defines a Role for P110Alpha in Signaling
Cell(Cambridge,Mass.), 125, 2006
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2CHW
 | | A pharmacological map of the PI3-K family defines a role for p110 alpha in signaling: The structure of complex of phosphoinositide 3- kinase gamma with inhibitor PIK-39 | | 分子名称: | 2-((9H-PURIN-6-YLTHIO)METHYL)-5-CHLORO-3-(2-METHOXYPHENYL)QUINAZOLIN-4(3H)-ONE, PHOSPHATIDYLINOSITOL-4,5-BISPHOSPHATE 3-KINASE CATALYTIC SUBUNIT GAMMA ISOFORM | | 著者 | Knight, Z.A, Gonzalez, B, Feldman, M.E, Zunder, E.R, Goldenberg, D.D, Williams, O, Loewith, R, Stokoe, D, Balla, A, Toth, B, Balla, T, Weiss, W.A, Williams, R.L, Shokat, K.M. | | 登録日 | 2006-03-16 | | 公開日 | 2006-05-22 | | 最終更新日 | 2023-12-13 | | 実験手法 | X-RAY DIFFRACTION (2.6 Å) | | 主引用文献 | A Pharmacological Map of the Pi3-K Family Defines a Role for P110Alpha in Signaling
Cell(Cambridge,Mass.), 125, 2006
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2A4Z
 | | Crystal Structure of human PI3Kgamma complexed with AS604850 | | 分子名称: | (5E)-5-[(2,2-DIFLUORO-1,3-BENZODIOXOL-5-YL)METHYLENE]-1,3-THIAZOLIDINE-2,4-DIONE, Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit, gamma isoform | | 著者 | Camps, M, Ruckle, T, Ji, H, Ardissone, V, Rintelen, F, Shaw, J, Ferrandi, C, Chabert, C, Gillieron, C, Francon, B, Martin, T, Gretener, D, Perrin, D, Leroy, D, Vitte, P.-A, Hirsch, E, Wymann, M.P, Cirillo, R, Schwarz, M.K, Rommel, C. | | 登録日 | 2005-06-30 | | 公開日 | 2005-09-20 | | 最終更新日 | 2023-10-25 | | 実験手法 | X-RAY DIFFRACTION (2.9 Å) | | 主引用文献 | Blockade of PI3Kgamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis
NAT.MED. (N.Y.), 11, 2005
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2A5U
 | | Crystal Structure of human PI3Kgamma complexed with AS605240 | | 分子名称: | (5E)-5-(QUINOXALIN-6-YLMETHYLENE)-1,3-THIAZOLIDINE-2,4-DIONE, Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit, gamma isoform | | 著者 | Camps, M, Ruckle, T, Ji, H, Ardissone, V, Rintelen, F, Shaw, J, Ferrandi, C, Chabert, C, Gillieron, C, Francon, B, Martin, T, Gretener, D, Perrin, D, Leroy, D, Vitte, P.-A, Hirsch, E, Wymann, M.P, Cirillo, R, Schwarz, M.K, Rommel, C. | | 登録日 | 2005-07-01 | | 公開日 | 2005-09-20 | | 最終更新日 | 2023-10-25 | | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | | 主引用文献 | Blockade of PI3Kgamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis
NAT.MED. (N.Y.), 11, 2005
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1HE8
 | | Ras G12V - PI 3-kinase gamma complex | | 分子名称: | MAGNESIUM ION, PHOSPHATIDYLINOSITOL 3-KINASE CATALYTIC SUBUNIT, GAMMA ISOFORM, ... | | 著者 | Pacold, M.E, Suire, S, Perisic, O, Lara-Gonzalez, S, Davis, C.T, Hawkins, P.T, Walker, E.H, Stephens, L, Eccleston, J.F, Williams, R.L. | | 登録日 | 2000-11-20 | | 公開日 | 2001-01-08 | | 最終更新日 | 2023-12-13 | | 実験手法 | X-RAY DIFFRACTION (3 Å) | | 主引用文献 | Crystal Structure and Functional Analysis of Ras Binding to its Effector Phosphoinositide 3-Kinase Gamma
Cell(Cambridge,Mass.), 103, 2000
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1E7V
 | | Structure determinants of phosphoinositide 3-kinase inhibition by wortmannin, LY294002, quercetin, myricetin and staurosporine | | 分子名称: | 2-MORPHOLIN-4-YL-7-PHENYL-4H-CHROMEN-4-ONE, PHOSPHATIDYLINOSITOL 3-KINASE CATALYTIC SUBUNIT | | 著者 | Walker, E.H, Pacold, M.E, Perisic, O, Stephens, L, Hawkins, P.T, Wymann, M.P, Williams, R.L. | | 登録日 | 2000-09-08 | | 公開日 | 2000-11-17 | | 最終更新日 | 2023-12-13 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Structural determinants of phosphoinositide 3-kinase inhibition by wortmannin, LY294002, quercetin, myricetin, and staurosporine.
Mol.Cell, 6, 2000
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1E7U
 | | Structure determinants of phosphoinositide 3-kinase inhibition by wortmannin, LY294002, quercetin, myricetin and staurosporine | | 分子名称: | (1S,6BR,9AS,11R,11BR)-9A,11B-DIMETHYL-1-[(METHYLOXY)METHYL]-3,6,9-TRIOXO-1,6,6B,7,8,9,9A,10,11,11B-DECAHYDRO-3H-FURO[4, 3,2-DE]INDENO[4,5-H][2]BENZOPYRAN-11-YL ACETATE, PHOSPHATIDYLINOSITOL 3-KINASE CATALYTIC SUBUNIT | | 著者 | Walker, E.H, Perisic, O, Ried, C, Stephens, L, Williams, R.L. | | 登録日 | 2000-09-08 | | 公開日 | 2000-11-17 | | 最終更新日 | 2023-12-13 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Structural Determinations of Phosphoinositide 3-Kinase Inhibition by Wortmannin, Ly294002, Quercetin, Myricetin and Staurosporine
Mol.Cell, 6, 2000
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