Extract from the Register of European Patents

EP Citations: EP2638044

Cited inInternational search
Type:Patent literature
Publication No.:WO2004029055  [A]
 (BAYER HEALTHCARE AG [DE], et al) [A] 1-17* claim 1 *;
Type:Patent literature
Publication No.:WO2008070150  [ID]
 (BAYER PHARMACEUTICALS CORP [US], et al) [ID] 1-17 * page 80; example 11; claim 1 *;
Type:Patent literature
Publication No.:WO2010034414  [I]
 (BAYER SCHERING PHARMA AG [DE], et al) [I] 1-17 * page 21; example Ia; claim 1 *
Cited inby applicant
Type:Patent literature
Publication No.:US5011472  
Type:Patent literature
Publication No.:US5023252  
Type:Patent literature
Publication No.:WO2008070150  
Type:Non-patent literature
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Type:Non-patent literature
Publication information:   - Organic Reactions, JOHN WILEY
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Publication information:   - POWELL, M. F. ET AL., "Compendium of Excipients for Parenteral Formulations", PDA JOURNAL OF PHARMACEUTICAL SCIENCE & TECHNOLOGY, (1998), vol. 52, no. 5, pages 238 - 311, XP009119027
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Publication information:   - STRICKLEY, R.G, "Parenteral Formulations of Small Molecule Therapeutics Marketed in the United States", PDA JOURNAL OF PHARMACEUTICAL SCIENCE & TECHNOLOGY 1999, (1999), vol. 53, no. 6, pages 324 - 349
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Publication information:   - NEMA, S., "Excipients and Their Use in Injectable Products", PDA JOURNAL OF PHARMACEUTICAL SCIENCE
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Publication information:   - GOODMAN, GILMAN'S, The Pharmacological Basis of Therapeutics, MCGRAW-HILL, (1996), pages 1225 - 1287
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Publication information:   - LOPEZ ET AL., INVEST. OPTHTHALMOL. VIS. SCI., (1996), vol. 37, page 855
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Publication information:   - "Multiple signaling pathways converge on p-catenin in thyroid cancer", ABBOSH, P.H., NEPHEW, K.P., Thyroid, (2005), vol. 15, pages 551 - 561
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Publication information:   - AIELLO, L.P., AVERY, R.L., ARRIGG, P.G., KEYT, B.A., JAMPEL, H.D., SHAH, S.T., PASQUALE, L.R., THIEME, H., IWAMOTO, M.A., PARK, J., "Vascular endothelial growth factor in ocular fluid of patients with diabetic retinopathy and other retinal disorders", N. ENGL. J. MED., (1994), vol. 331, doi:doi:10.1056/NEJM199412013312203, pages 1480 - 1487, XP002690192
DOI: http://dx.doi.org/10.1056/NEJM199412013312203
Type:Non-patent literature
Publication information:   - ALI, I.U., SCHRIML, L.M., DEAN, M. J., "Mutational spectra of PTEN/MMAC1 gene: a tumor suppressor with lipid phosphatase activity", NATL. CANCER LNST., (1999), vol. 91, pages 1922 - 1932
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Publication information:   - BACHMAN, K.E., ARGANI, P., SAMUELS, Y., SILLIMAN, N., PTAK, J., SZABO, S., KONISHI, H., KARAKAS, B., BLAIR, B.G., LIN, C., "The PIK3CA gene is mutated with high frequency in human breast cancers", CANCER BIOL. THERAP., (2004), vol. 3, doi:doi:10.4161/cbt.3.8.994, pages 772 - 775, XP055035716
DOI: http://dx.doi.org/10.4161/cbt.3.8.994
Type:Non-patent literature
Publication information:   - BADER, A.G., KANG, S.;, VOGT, P.K., "Cancer-specific mutations in PIK3CA are oncogenic in vivo", PROC. NATL. ACAD. SCI. U.S.A., (2006), vol. 103, doi:doi:10.1073/PNAS.0510857103, pages 1475 - 1479, XP002687647
DOI: http://dx.doi.org/10.1073/PNAS.0510857103
Type:Non-patent literature
Publication information:   - BARTHWAL, M.K., SATHYANARAYANA, P., KUNDU, C.N., RANA, B., PRADEEP, A., SHARMA, C., WOODGETT, J.R., RANA, A, "Negative Regulation of Mixed Lineage Kinase 3 by Protein Kinase B/AKT Leads to Cell Survival", J. BIOL. CHEM., (2003), vol. 278, pages 3897 - 3902
Type:Non-patent literature
Publication information:   - BÉNISTANT, C., CHAPUIS, H., ROCHE, S., "A specific function for phosphatidylinositol 3-kinase a (p85?-p110?) in cell survival and for phosphatidylinositol 3- kinase p (p85a-p110p) in de novo DNA synthesis of human colon carcinoma cells", ONCOGENE, (2000), vol. 19, doi:doi:10.1038/sj.onc.1203871, pages 5083 - 5090, XP002484274
DOI: http://dx.doi.org/10.1038/sj.onc.1203871
Type:Non-patent literature
Publication information:   - BISSERY, M.-C., NOHYNEK, G., SANDERINK, G.-J., LAVELLE, F., "Docetaxel (Taxotere): a review of preclinical and clinical experience. Part I: preclinical experience", ANTI-CANCER DRUGS, (1995), vol. 6, pages 339 - 355
Type:Non-patent literature
Publication information:   - BRODERICK, D.K., DI, C., PARRETT, T.J., SAMUELS, Y.R., CUMMINS, J.M., MCLENDON, R.E., FULTS, D.W., VELCULESCU, V.E., BIGNER, D.D.,, "Mutations of PIK3CA in anaplastic oligodendrogliomas, high-grade astrocytomas, and medulloblastomas", CANCER RES., (2004), vol. 64, doi:doi:10.1158/0008-5472.CAN-04-1170, pages 5048 - 5050, XP002517093
DOI: http://dx.doi.org/10.1158/0008-5472.CAN-04-1170
Type:Non-patent literature
Publication information:   - BROWN, R.A., SHEPHERD, P.R., "Growth factor regulation of the novel class II phosphoinositide 3-kinases", BIOCHEM. SOC. TRANS., (2001), vol. 29, pages 535 - 537
Type:Non-patent literature
Publication information:   - BRUGGE, J., HUNG, M.-C., MILLS, G.B., "A new mutational aktivation in the P13K pathway", CANCER CELL, (2007), vol. 12, pages 104 - 107
Type:Non-patent literature
Publication information:   - BRUNET, A., BONNI, A., ZIGMOND, M.J., LIN, M.Z., JUO, P., HU, L.S., ANDERSON, M.J., ARDEN, K.C., BLENIS, J., GREENBERG, M.E, "Akt promotes cell survival by phosphorylating and inhibiting a Forkhead transcription factor", CELL, (1999), vol. 96, doi:doi:10.1016/S0092-8674(00)80595-4, pages 857 - 868, XP002922384
DOI: http://dx.doi.org/10.1016/S0092-8674(00)80595-4
Type:Non-patent literature
Publication information:   - BYUN, D.-S., CHO, K., RYU, B.-K., LEE, M.-G., PARK, J.-I., CHAE, K.-S., KIM, H.-J., CHI, S.-G., "Frequent monoallelic deletion of PTEN and its reciprocal association with PIK3CA amplification in gastric carcinoma", INT. J. CANCER, (2003), vol. 104, pages 318 - 327
Type:Non-patent literature
Publication information:   - CAMPBELL, I.G., RUSSELL, S.E., CHOONG, D.Y.H., MONTGOMERY, K.G., CIAVARELLA, M.L., HOOI, C.S.F., CRISTIANO, B.E., PEARSON, R.B., P, "Mutation of the PIK3CA gene in ovarian and breast cancer", CANCER RES., (2004), vol. 64, pages 7678 - 7681
Type:Non-patent literature
Publication information:   - CARDONE, M.H., ROY, N., STENNICKE, H.R., SALVESEN, G.S., FRANKE, T.F., STANBRIDGE, E., FRISCH, S., REED, J.C., "Regulation of cell death protease caspase-9 by phosphorylation", SCIENCE, (1998), vol. 282, pages 1318 - 1321
Type:Non-patent literature
Publication information:   - CHEN, Y.L., LAW, P.-Y., LOH, H.H., "Inhibition of P!3K/Akt signaling: An emerging paradigm for targeted cancer therapy", CURR. MED. CHEM.: ANTI-CANCER AGENTS, (2005), vol. 5, pages 575 - 589, XP009098139
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Publication information:   - CIECHOMSKA, I., PYRZYNSKA, B., KAZMIERCZAK, P., KAMINSKA, B., "Inhibition of Akt kinase signalling and activation of Forkhead are indispensable for up- regulation of FasL expression in apoptosis of glioma cells", ONCOGENE, (2003), vol. 22, pages 7617 - 7627
Type:Non-patent literature
Publication information:   - CROSS, D.A.E., ALESSI, D.R, COHEN, P., ANDJELKOVICH, M., HEMMINGS, B.A., "Inhibition of glycogen synthase kinase-3 by insulin mediated by protein kinase B", NATURE, (1995), vol. 378, doi:doi:10.1038/378785a0, pages 785 - 789, XP002025954
DOI: http://dx.doi.org/10.1038/378785a0
Type:Non-patent literature
Publication information:   - CULLY, M., YOU, H., LEVINE, A.J., MAK, T.W., "Beyond PTEN mutations: the P13K pathway as an integrator of multiple inputs during tumorigenesis", NAT. REV. CANCER, (2006), vol. 6, pages 184 - 192
Type:Non-patent literature
Publication information:   - CZAUDERNA, F., FECHTNER, M., AYGUN, H., ARNOLD, W., KLIPPEL, A., GIESE, K., KAUFMANN, J., "Functional studies of the PI(3)-kinase signalling pathway employing synthetic and expressed siRNA", NUCLEIC ACIDS RES., (2003), vol. 31, doi:doi:10.1093/nar/gkg141, pages 670 - 682, XP002992229
DOI: http://dx.doi.org/10.1093/nar/gkg141
Type:Non-patent literature
Publication information:   - DALY, C, WONG, V., BUROVA, E., WEI, Y., ZABSKI, S., GRIFFITHS, J., LAI, K.-M., LIN, H.C., LOFFE, E., YANCOPOULOS, G.D., "Angiopoietin-1 modulates endothelial cell function and gene expression via the transcription factor FKHR (FOX01", GENES DEV., (2004), vol. 18, pages 1060 - 1071
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Publication information:   - DEL PESO, L., GONZAIEZ-GARCIA, M., PAGE, C., HERRERA, R., NUNEZ, G., "Interleukin-3-induced phosphorylation of BAD through the protein kinase Akt", SCIENCE, (1997), vol. 278, pages 687 - 689, XP002958941
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Publication information:   - DIEHL, J.A., CHENG, M., ROUSSEL, M.F.;, SHERR, C.J., "Glycogen synthase kinase-3b regulates cyclin D1 proteolysis and subcellular localization", GENES DEV., (1998), vol. 12, pages 3499 - 3511
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Publication information:   - DIJKERS, P.F., MEDEMA, R.H., LAMMERS, J.-W.J., KOENDERMAN, L., COFFER, P.J., "Expression of the pro-apoptotic Bcl-2 family member Bim is regulated by the Forkhead transcription factor FKHR-L1", CURR. BIOL., (2000), vol. 10, pages 1201 - 1204
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Publication information:   - DOMIN, J., WATERFIELD, M.D., "Using structure to define the function of phosphoinositide 3-kinase family members", FEBS LETT., (1997), vol. 410, doi:doi:10.1016/S0014-5793(97)00617-0, pages 91 - 95, XP004261759
DOI: http://dx.doi.org/10.1016/S0014-5793(97)00617-0
Type:Non-patent literature
Publication information:   - DOWNES, C.P., GRAY, A., LUCOCQ, J.M., "Probing phosphoinositide functions in signaling and membrane trafficking", TRENDS CELL BIOL., (2005), vol. 15, doi:doi:10.1016/j.tcb.2005.03.008, pages 259 - 268, XP004872259
DOI: http://dx.doi.org/10.1016/j.tcb.2005.03.008
Type:Non-patent literature
Publication information:   - EDELMAN, M.J., GANDARA, D.R., "Promising new agents in the treatment of non-small cell lung cancer", CANCER CHEMOTHERAP. PHARMACOL., (1996), vol. 37, pages 385 - 393
Type:Non-patent literature
Publication information:   - FIGUEROA, C., TARRAS, S., TAYLOR, J., VOJTEK, A.B., "Akt2 negatively regulates assembly of the POSH-MLK-JNK signaling complex", J. BIOL. CHEM., (2003), vol. 278, doi:doi:10.1074/jbc.M307357200, pages 47922 - 47927, XP002996244
DOI: http://dx.doi.org/10.1074/jbc.M307357200
Type:Non-patent literature
Publication information:   - FLEMING, I.N., GRAY, A., DOWNES, C.P., "Regulation of the Rac1-specific exchange factor tiam1 involves both phosphoinositide 3-kinase-dependent and - independent components", BIOCHEM. J., (2000), vol. 351, pages 173 - 182
Type:Non-patent literature
Publication information:   - FUNAKI, M., KATAGIRI, H., INUKAI, K., KIKUCHI, M., ASANO, T., "Structure and function of phosphatidylinositol-3,4 kinase", CELL. SIGNALLING, (2000), vol. 12, pages 135 - 142
Type:Non-patent literature
Publication information:   - GALLIA, G.L., RAND, V., SIU, I.M., EBERHART, C.G., JAMES, C.D., MARIE, S.K.N., OBA-SHINJO, S.M., CARLOTTI, C.G., CABALLERO, O.L.,, "PIK3CA gene mutations in pediatric and adult glioblastoma multiforme", MOL. CANCER RES., (2006), vol. 4, pages 709 - 714
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Publication information:   - GARCIA-ROSTAN, G., COSTA, A.M., PEREIRA-CASTRO, I., SALVATORE, G., HERNANDEZ, R.;, HERMSEM, M.J.A., HERRERO, A., FUSCO, A., CAMESE, "Mutation of the PIK3CA gene in anaplastic thyroid cancer", CANCER RES., (2005), vol. 65, pages 10199 - 10207
Type:Non-patent literature
Publication information:   - GERSHTEIN, E.S., SHATSKAYA, V.A., ERMILOVA, V.D., KUSHLINSKY, N.E., KRASIL'NIKOV, M.A., "Phosphatidylinositol 3-kinase expression in human breast cancer", CLIN. CHIM. ACTA, (1999), vol. 287, pages 59 - 67
Type:Non-patent literature
Publication information:   - GOTTSCHALK, A.R., DOAN, A., NAKAMURA, J.L., STOKOE, D., HAAS-KOGAN, D.A, "Inhibition of phosphatidylinositol-3-kinase causes increased sensitivity to radiation through a PKB-dependent mechanism", INT. J. RADIAT. ONCOL. BIOL. PHYS., (2005), vol. 63, doi:doi:10.1016/j.ijrobp.2005.08.014, pages 1221 - 1227, XP025262460
DOI: http://dx.doi.org/10.1016/j.ijrobp.2005.08.014
Type:Non-patent literature
Publication information:   - GUPTA, A.K., CERNIGLIA, G.J., MICK, R., AHMED, M.S., BAKANAUSKAS, V.J., MUSCHEL, R.J., MCKENNA, W.G., "Radiation sensitization of human cancer cells in vivo by inhibiting the activity of P13K using LY294002", INT. J. RADIAT. ONCOL. BIOL. PHYS., (2003), vol. 56, doi:doi:10.1016/S0360-3016(03)00214-1, pages 846 - 853, XP002327025
DOI: http://dx.doi.org/10.1016/S0360-3016(03)00214-1
Type:Non-patent literature
Publication information:   - HAAS-KOGAN, D., SHALEV, N., WONG, M., MILLS, G., YOUNT, G., STOKOE, D., "Protein kinase B (PKB/Akt) activity is elevated in glioblastoma cells due to mutation of the tumor suppressor PTEN/MMAC", CURR. BIOL., (1998), vol. 8, pages 1195 - 1198
Type:Non-patent literature
Publication information:   - HARTMANN, C., BARTELS, G., GEHLHAAR, C., HOLTKAMP, N., VON DEIMLING, A., "PIK3CA mutations in glioblastoma multiforme", ACTA NEUROPATHOL., (2005), vol. 109, doi:doi:10.1007/s00401-005-1000-1, pages 639 - 642, XP019340738
DOI: http://dx.doi.org/10.1007/s00401-005-1000-1
Type:Non-patent literature
Publication information:   - HENNESSY, B.T., SMITH, D.L., RAM, P.T., LU, Y., MILLS, G.B., "Exploiting the P!3K/AKT Pathway for Cancer Drug Discovery", NAT. REV. DRUG DISC., (2005), vol. 4, pages 988 - 1004
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Publication information:   - HODGKINSON, C.P., SALE, E.M., SALE, G.J., "Characterization of PDK2 activity against Protein Kinase B gamma", BIOCHEMISTRY, (2002), vol. 41, doi:doi:10.1021/bi026065r, pages 10351 - 10359, XP002409946
DOI: http://dx.doi.org/10.1021/bi026065r
Type:Non-patent literature
Publication information:   - HRESKO, R.C., MURATA, H., MUECKLER, M., "Phosphoinositide-dependent Kinase-2 is a distinct protein kinase enriched in a novel cytoskeletal fraction associated with adipocyte plasma membranes", J. BIOL. CHEM., (2003), vol. 278, pages 21615 - 21622
Type:Non-patent literature
Publication information:   - HUANG, C., MA, W.-Y., DONG, Z., "Requirement for phosphatidylinositol 3-kinase in epidermal growth factor-induced AP-1 transactivation and transformation in JB6 P+ cells", MOL. CELL. BIOL., (1996), vol. 16, pages 6427 - 6435
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Publication information:   - HUPP, T.R., LANE, D.P.;, BALL, K.L., "Strategies for manipulating the p53 pathway in the treatment of human cancer", BIOCHEM. J., (2000), vol. 352, pages 1 - 17
Type:Non-patent literature
Publication information:   - LHLE, N.T., WILLIAMS, R., CHOW, S., CHEW, W., BERGGREN, M.I., PAINE-MURRIETA, G., MINION, D.J., HALTER, R.J., WIPF, P., ABRAHAM, R, "Molecular pharmacology and antitumor activity of PX-866, a novel inhibitor of phosphoinositide-3-kinase signaling", MOL. CANCER THER., (2004), vol. 3, pages 763 - 772, XP002532313
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Publication information:   - IKENOUE, T., KANAI, F., HIKIBA, Y., OBATA, T., TANAKA, Y., IMAMURA, J., OHTA, M., JAZAG, A., GULENG, B., TATEISHI, K., "Functional analysis of PIK3CA gene mutations in human colorectal cancer", CANCER RES., (2005), vol. 65, pages 4562 - 4567
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Publication information:   - ISHII, N., MAIER, D., MERLO, A., TADA, M., SAWAMURA, Y.;, DISERENS, A.-C., VAN MEIR, E.G., "Frequent co-alterations of TP53, p16/CDKN2A, pl4ARF, PTEN tumor suppressor genes in human glioma cell lines", BRAIN PATHOL., (1999), vol. 9, pages 469 - 479
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Publication information:   - ITOH, T., TAKENAWA, T., "Phosphoinositide-binding domains. Functional units for temporal and spatial regulation of intracellular signalling", CELL. SIGNALLING, (2002), vol. 14, pages 733 - 743
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Publication information:   - JANSSEN, J.W.G., SCHLEITHOFF, L., BARTRAM, C.R., SCHULZ, A.S., "An oncogenic fusion product of the phosphatidylinositol 3-kinase p85b subunit and HUMORF8, a putative deubiquitinating enzyme", ONCOGENE, (1998), vol. 16, pages 1767 - 1772
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Publication information:   - JIA, S., LIU, Z., ZHANG, S., LIU, P., ZHANG, L., LEE, S.H., ZHANG, J., SIGNORETTI, S., LODA, M., ROBERTS, T.M., "Essential roles of PI(3)K-p110(3 in cell growth, metabolism and tumorigenesis", NATURE, (2008), vol. 454, pages 776 - 779
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Publication information:   - JIA, S., ROBERTS, T.M., ZHAO, J.J., "Should individual P13 kinase isoforms be targeted in cancer?", CURR. OPIN. CELL BIOL., (2009), vol. 21, doi:doi:10.1016/j.ceb.2008.12.007, pages 199 - 208, XP026035452
DOI: http://dx.doi.org/10.1016/j.ceb.2008.12.007
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Publication information:   - JIMENEZ, C., JONES, D.R., RODRIGUEZ-VICIANA, P., GONZALEZ-GARCIA, A., LEONARDO, E., WENNSTROM, S., VON KOBBE, C., TORAN, J.L., R.-, "Identification and characterization of a new oncogene derived from the regulatory subunit of phosphoinositide 3-kinase", EMBO J., (1998), vol. 17, pages 743 - 753
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Publication information:   - JUCKER, M., SUDEL, K., HORN, S., SICKEL, M., WEGNER, W., FIEDLER, W., FELDMAN, R.A., "Expression of a mutated form of the p85a regulatory subunit of phosphatidylinositol 3-kinase in a Hodgkin's lymphoma-derived cell line (CO", LEUKEMIA, (2002), vol. 16, pages 894 - 901
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Publication information:   - KANG, S., BADER, A.G., VOGT, P.K., "Phosphatidylinositol 3-kinase mutations identified in human cancer are oncogenic", PROC. NATL. ACAD. SCI. U.S.A., (2005), vol. 102, pages 802 - 807
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Publication information:   - KANG, S., DENLEY, A., VANHAESEBROECK, B., VOGT, P.K., "Oncogenic transformation induced by the p110b, -g, and -d isoforms of class I phosphoinositide 3-kinase", PROC. NATL. ACAD. SCI. U.S.A., (2006), vol. 103, pages 1289 - 1294
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Publication information:   - KATSO, R., OKKENHAUG, K., AHMADI, K., WHITE, S.;, TIMMS, J., WATERFIELD, M.D., "Cellular function of phosphoinositide 3-kinases: implications for development, immunity, homeostasis, and cancer", ANN. REV. CELL. DEV. BIOL., (2001), vol. 17, pages 615 - 675
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Publication information:   - KIM, A.H., KHURSIGARA, G., SUN, X., FRANKE, T.F., CHAO, M.V., "Akt phosphorylates and negatively regulates apoptosis signal-regulating kinase 1", MOL. CELL. BIOL., (2001), vol. 21, pages 893 - 901
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Publication information:   - KIM, D., DAN, H.C., PARK, S., YANG, L., LIU, Q., KANEKO, S., NING, J., HE, L., YANG, H., SUN, M., "AKT/PKB signaling mechanisms in cancer and chemoresistance", FRONT. BIOSCI., (2005), vol. 10, doi:doi:10.2741/1592, pages 975 - 987, XP009166431
DOI: http://dx.doi.org/10.2741/1592
Type:Non-patent literature
Publication information:   - KLIPPEL, A., KAVANAUGH, W.M., POT, D., WILLIAMS, L.T., "A specific product of phosphatidylinositol 3-kinase directly activates the protein kinase Akt through its pleckstrin homology domain", MOL. CELL. BIOL., (1997), vol. 17, pages 338 - 344
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Publication information:   - KODAKI, T., WOSCHOLSKI, R., HALLBERG, B., RODRIGUEZ-VICIANA, P., DOWNWARD, J., PARKER, P.J., "The activation of phosphatidylinositol 3-kinase by Ras", CURR. BIOL., (1994), vol. 4, doi:doi:10.1016/S0960-9822(00)00177-9, pages 798 - 806, XP024249253
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Type:Non-patent literature
Publication information:   - KOPS, G.J.P.L., DE RUITER, N.D., DE VRIES-SMITS, A.M.M., POWELL, D.R., BOS, J.L., BURGERING, B.M.T, "Direct control of the Forkhead transcription factor AFX by protein kinase B", NATURE, (1999), vol. 398, doi:doi:10.1038/19328, pages 630 - 634, XP000955388
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Publication information:   - LEE, J.T., JR., STEELMAN, L.S., MCCUBREY, J.A., "Phosphatidylinositol 3'-Kinase Activation Leads to Multidrug Resistance Protein-1 Expression and Subsequent Chemoresistance in Advanced Prostate Cancer Cells", CANCER RES., (2004), vol. 64, pages 8397 - 8404
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