메뉴 건너뛰기




Volumn 13, Issue 5, 2014, Pages 1078-1091

Characterization of the activity of the PI3K/mTOR inhibitor XL765 (SAR245409) in tumor models with diverse genetic alterations affecting the PI3K pathway

Author keywords

[No Author keywords available]

Indexed keywords

CASPASE 3; CASPASE 7; CYCLIN D1; P70S6K PROTEIN; PROTEIN; PROTEIN KINASE B; PROTEIN P110; PROTEIN P110 DELTA; PROTEIN P110BETA; PROTEIN P110GAMMA; PROTEIN S6; SAR 245409; UNCLASSIFIED DRUG; XL 765; ANTINEOPLASTIC AGENT; PHOSPHATIDYLINOSITOL 3 KINASE; PHOSPHATIDYLINOSITOL 3,4,5-TRIPHOSPHATE; POLYPHOSPHOINOSITIDE; PROTEIN KINASE INHIBITOR; QUINOXALINE DERIVATIVE; S6 KINASE; SULFONAMIDE; TARGET OF RAPAMYCIN KINASE; VOXTALISIB;

EID: 84899711229     PISSN: 15357163     EISSN: 15388514     Source Type: Journal    
DOI: 10.1158/1535-7163.MCT-13-0709     Document Type: Article
Times cited : (75)

References (36)
  • 1
  • 2
    • 51849128358 scopus 로고    scopus 로고
    • Class i PI3K in oncogenic cellular transformation
    • Zhao L, Vogt PK. Class I PI3K in oncogenic cellular transformation. Oncogene 2008;27:5486-96.
    • (2008) Oncogene , vol.27 , pp. 5486-5496
    • Zhao, L.1    Vogt, P.K.2
  • 3
    • 46149106818 scopus 로고    scopus 로고
    • The p110beta isoform of phosphoinositide 3-kinase signals downstreamofGprotein-coupled receptors and is functionally redundant with p110gamma
    • Guillermet-Guibert J, Bjorklof K, Salpekar A, Gonella C, Ramadani F, Bilancio A, et al. The p110beta isoform of phosphoinositide 3-kinase signals downstreamofGprotein-coupled receptors and is functionally redundant with p110gamma. Proc Natl Acad Sci U S A 2008;105: 8292-7.
    • (2008) Proc Natl Acad Sci U S A , vol.105 , pp. 8292-8297
    • Guillermet-Guibert, J.1    Bjorklof, K.2    Salpekar, A.3    Gonella, C.4    Ramadani, F.5    Bilancio, A.6
  • 4
    • 0030911052 scopus 로고    scopus 로고
    • Role of phosphoinositide 3-OH kinase in cell transformation and control of the actin cytoskeleton by Ras
    • Rodriguez-Viciana P, Warne PH, Khwaja A, Marte BM, Pappin D, Das P, et al. Role of phosphoinositide 3-OH kinase in cell transformation and control of the actin cytoskeleton by Ras. Cell 1997;89:457-67.
    • (1997) Cell , vol.89 , pp. 457-467
    • Rodriguez-Viciana, P.1    Warne, P.H.2    Khwaja, A.3    Marte, B.M.4    Pappin, D.5    Das, P.6
  • 5
    • 77950516104 scopus 로고    scopus 로고
    • MTOR signaling and drug development in cancer
    • Dancey J. mTOR signaling and drug development in cancer. Nat Rev Clin Oncol 2010;7:209-19.
    • (2010) Nat Rev Clin Oncol , vol.7 , pp. 209-219
    • Dancey, J.1
  • 6
    • 34347220473 scopus 로고    scopus 로고
    • Defining the role of mTOR in cancer
    • Guertin DA, Sabatini DM. Defining the role of mTOR in cancer. Cancer Cell 2007;12:9-22.
    • (2007) Cancer Cell , vol.12 , pp. 9-22
    • Guertin, D.A.1    Sabatini, D.M.2
  • 7
    • 3342895823 scopus 로고    scopus 로고
    • Rictor, a novel binding partner of mTOR, defines a rapamycin-insensitive and raptor-independent pathway that regulates the cytoskeleton
    • Sarbassov DD, Ali SM, Kim DH, Guertin DA, Latek RR, Erdjument- Bromage H, et al. Rictor, a novel binding partner of mTOR, defines a rapamycin-insensitive and raptor-independent pathway that regulates the cytoskeleton. Curr Biol 2004;14:1296-302.
    • (2004) Curr Biol , vol.14 , pp. 1296-1302
    • Sarbassov, D.D.1    Ali, S.M.2    Kim, D.H.3    Guertin, D.A.4    Latek, R.R.5    Erdjument-Bromage, H.6
  • 8
    • 84899855144 scopus 로고    scopus 로고
    • Febuary 2014 search of COSMIC database. Available from
    • Febuary 2014 search of COSMIC database. Available from: http:// www. sanger. ac. uk/genetics/CGP/cosmic/.
  • 9
    • 79953038262 scopus 로고    scopus 로고
    • PTEN loss in the continuum of common cancers, rare syndromes and mouse models
    • Hollander MC, BlumenthalGM,Dennis PA. PTEN loss in the continuum of common cancers, rare syndromes and mouse models. Nat Rev Cancer 2011;11:289-301.
    • (2011) Nat Rev Cancer , vol.11 , pp. 289-301
    • Hollander, M.C.1    Blumenthal, G.M.2    Dennis, P.A.3
  • 10
    • 79956088595 scopus 로고    scopus 로고
    • The long and winding road to rational treatment of cancer associated with LKB1/ AMPK/TSC/mTORC1 signaling
    • van Veelen W, Korsse SE, van de Laar L, Peppelenbosch MP. The long and winding road to rational treatment of cancer associated with LKB1/ AMPK/TSC/mTORC1 signaling. Oncogene 2011;30:2289-303.
    • (2011) Oncogene , vol.30 , pp. 2289-2303
    • Van Veelen, W.1    Korsse, S.E.2    Van De Laar, L.3    Peppelenbosch, M.P.4
  • 11
    • 67649814136 scopus 로고    scopus 로고
    • PI3K/PTEN signaling in angiogenesis and tumorigenesis
    • Jiang BH, Liu LZ. PI3K/PTEN signaling in angiogenesis and tumorigenesis. Adv Cancer Res 2009;102:19-65.
    • (2009) Adv Cancer Res , vol.102 , pp. 19-65
    • Jiang, B.H.1    Liu, L.Z.2
  • 13
    • 53049087363 scopus 로고    scopus 로고
    • Effects of the dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor NVP-BEZ235 on the tumor vasculature: Implications for clinical imaging
    • Schnell CR, Stauffer F, Allegrini PR, O'Reilly T, McSheehy PM, Dartois C, et al. Effects of the dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor NVP-BEZ235 on the tumor vasculature: implications for clinical imaging. Cancer Res 2008;68:6598-607.
    • (2008) Cancer Res , vol.68 , pp. 6598-6607
    • Schnell, C.R.1    Stauffer, F.2    Allegrini, P.R.3    O'Reilly, T.4    McSheehy, P.M.5    Dartois, C.6
  • 14
    • 77956236877 scopus 로고    scopus 로고
    • PI(3)king apart PTEN's role in cancer
    • Zhang S, Yu D. PI(3)king apart PTEN's role in cancer. Clin Cancer Res 2010;16:4325-30.
    • (2010) Clin Cancer Res , vol.16 , pp. 4325-4330
    • Zhang, S.1    Yu, D.2
  • 16
    • 77953411708 scopus 로고    scopus 로고
    • Activated phosphoinositide 3-kinase/AKT signaling confers resistance to trastuzumab but not lapatinib
    • O'Brien NA, Browne BC, Chow L, Wang Y, Ginther C, Arboleda J, et al. Activated phosphoinositide 3-kinase/AKT signaling confers resistance to trastuzumab but not lapatinib. Mol Cancer Ther 2010;9:1489-502.
    • (2010) Mol Cancer Ther , vol.9 , pp. 1489-1502
    • O'Brien, N.A.1    Browne, B.C.2    Chow, L.3    Wang, Y.4    Ginther, C.5    Arboleda, J.6
  • 17
    • 73349129405 scopus 로고    scopus 로고
    • Differential induction of apoptosis in HER2 and EGFR addicted cancers following PI3K inhibition
    • Faber AC, Li D, Song Y, Liang MC, Yeap BY, Bronson RT, et al. Differential induction of apoptosis in HER2 and EGFR addicted cancers following PI3K inhibition. Proc Natl Acad Sci U S A 2009;106: 19503-8.
    • (2009) Proc Natl Acad Sci U S A , vol.106 , pp. 19503-19508
    • Faber, A.C.1    Li, D.2    Song, Y.3    Liang, M.C.4    Yeap, B.Y.5    Bronson, R.T.6
  • 18
    • 79551559942 scopus 로고    scopus 로고
    • Multiple mutations and bypass mechanisms can contribute to development of acquired resistance to MET inhibitors
    • Qi J, McTigue MA, Rogers A, Lifshits E, Christensen JG, Jänne PA, et al. Multiple mutations and bypass mechanisms can contribute to development of acquired resistance to MET inhibitors. Cancer Res 2011;71:1081-91.
    • (2011) Cancer Res , vol.71 , pp. 1081-1091
    • Qi, J.1    McTigue, M.A.2    Rogers, A.3    Lifshits, E.4    Christensen, J.G.5    Jänne, P.A.6
  • 19
    • 84857417355 scopus 로고    scopus 로고
    • Breast Cancer Special feature: Feedback upregulation of HER3 (ErbB3) expression and activity attenuates antitumor effect of PI3K inhibitors
    • Chakrabarty A, Sanchez V, Kuba MG, Rinehart C, Arteaga CL. Breast Cancer Special feature: feedback upregulation of HER3 (ErbB3) expression and activity attenuates antitumor effect of PI3K inhibitors. Proc Natl Acad Sci U S A 2012;109:2718-23.
    • (2012) Proc Natl Acad Sci U S A , vol.109 , pp. 2718-2723
    • Chakrabarty, A.1    Sanchez, V.2    Kuba, M.G.3    Rinehart, C.4    Arteaga, C.L.5
  • 20
    • 63749101351 scopus 로고    scopus 로고
    • Targeting the EGFRand the PKB pathway in cancer
    • Klein S, Levitzki A. Targeting the EGFRand the PKB pathway in cancer. Curr Opin Cell Biol 2009;21:185-93.
    • (2009) Curr Opin Cell Biol , vol.21 , pp. 185-193
    • Klein, S.1    Levitzki, A.2
  • 21
    • 34248198039 scopus 로고    scopus 로고
    • Preferential chemosensitization of PTEN-mutated prostate cells by silencing the Akt kinase
    • Priulla M, Calastretti A, Bruno P, Azzariti A, Paradiso A, Canti G, et al. Preferential chemosensitization of PTEN-mutated prostate cells by silencing the Akt kinase. Prostate 2007;67:782-9.
    • (2007) Prostate , vol.67 , pp. 782-789
    • Priulla, M.1    Calastretti, A.2    Bruno, P.3    Azzariti, A.4    Paradiso, A.5    Canti, G.6
  • 22
    • 79954603804 scopus 로고    scopus 로고
    • Dual targeting of phosphoinositide 3-kinase and mammalian target of rapamycin using NVP-BEZ235 as a novel therapeutic approach in human ovarian carcinoma
    • Santiskulvong C, Konecny GE, Fekete M, Chen KY, Karam A, Mulholland D, et al. Dual targeting of phosphoinositide 3-kinase and mammalian target of rapamycin using NVP-BEZ235 as a novel therapeutic approach in human ovarian carcinoma. Clin Cancer Res 2011;17: 2373-84.
    • (2011) Clin Cancer Res , vol.17 , pp. 2373-2384
    • Santiskulvong, C.1    Konecny, G.E.2    Fekete, M.3    Chen, K.Y.4    Karam, A.5    Mulholland, D.6
  • 23
    • 67749122122 scopus 로고    scopus 로고
    • Targeting PI3K signalling in cancer: Opportunities, challenges and limitations
    • Engelman JA. Targeting PI3K signalling in cancer: opportunities, challenges and limitations. Nat Rev Cancer 2009;9:550-62.
    • (2009) Nat Rev Cancer , vol.9 , pp. 550-562
    • Engelman, J.A.1
  • 24
    • 77955430762 scopus 로고    scopus 로고
    • Allosteric and ATP-competitive kinase inhibitors of mTOR for cancer treatment
    • García-Echeverría C. Allosteric and ATP-competitive kinase inhibitors of mTOR for cancer treatment. Bioorg Med Chem Lett 2010;20: 4308-12.
    • (2010) Bioorg Med Chem Lett , vol.20 , pp. 4308-4312
    • García-Echeverría, C.1
  • 25
    • 34250791359 scopus 로고    scopus 로고
    • Inhibition of the T790M gatekeeper mutant of the epidermal growth factor receptor by EXEL-7647
    • Gendreau SB, Ventura R, Keast P, Laird AD, Yakes FM, Zhang W, et al. Inhibition of the T790M gatekeeper mutant of the epidermal growth factor receptor by EXEL-7647. Clin Cancer Res 2007;13: 3713-23.
    • (2007) Clin Cancer Res , vol.13 , pp. 3713-3723
    • Gendreau, S.B.1    Ventura, R.2    Keast, P.3    Laird, A.D.4    Yakes, F.M.5    Zhang, W.6
  • 27
    • 83355166909 scopus 로고    scopus 로고
    • Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth
    • Yakes FM, Chen J, Tan J, Yamaguchi K, Shi Y, Yu P, et al. Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth. Mol Cancer Ther 2011;10:2298-308.
    • (2011) Mol Cancer Ther , vol.10 , pp. 2298-2308
    • Yakes, F.M.1    Chen, J.2    Tan, J.3    Yamaguchi, K.4    Shi, Y.5    Yu, P.6
  • 29
    • 24744435392 scopus 로고    scopus 로고
    • Activation of mammalian target of rapamycin in transformed B lymphocytes is nutrient dependent but independent of Akt, mitogen-activated protein kinase/extracellular signal-regulated kinase kinase, insulin growth factor-I, and serum
    • Wlodarski P, Kasprzycka M, Liu X, Marzec M, Robertson ES, Slupianek A, et al. Activation of mammalian target of rapamycin in transformed B lymphocytes is nutrient dependent but independent of Akt, mitogen-activated protein kinase/extracellular signal-regulated kinase kinase, insulin growth factor-I, and serum. Cancer Res 2005;65:7800-8.
    • (2005) Cancer Res , vol.65 , pp. 7800-7808
    • Wlodarski, P.1    Kasprzycka, M.2    Liu, X.3    Marzec, M.4    Robertson, E.S.5    Slupianek, A.6
  • 31
    • 63749106157 scopus 로고    scopus 로고
    • Should individual PI3 kinase isoforms be targeted in cancer?
    • Jia S, Roberts TM, Zhao JJ. Should individual PI3 kinase isoforms be targeted in cancer? Curr Opin Cell Biol 2009;21:199-208.
    • (2009) Curr Opin Cell Biol , vol.21 , pp. 199-208
    • Jia, S.1    Roberts, T.M.2    Zhao, J.J.3
  • 32
    • 77954755623 scopus 로고    scopus 로고
    • Predictive biomarkers of sensitivity to the phosphatidylinositol 30 kinase inhibitor GDC-0941 in breast cancer preclinical models
    • O'Brien C, Wallin JJ, Sampath D, GuhaThakurta D, Savage H, Punnoose EA, et al. Predictive biomarkers of sensitivity to the phosphatidylinositol 30 kinase inhibitor GDC-0941 in breast cancer preclinical models. Clin Cancer Res 2010;16:3670-83.
    • (2010) Clin Cancer Res , vol.16 , pp. 3670-3683
    • O'Brien, C.1    Wallin, J.J.2    Sampath, D.3    Guhathakurta, D.4    Savage, H.5    Punnoose, E.A.6
  • 33
    • 79955983369 scopus 로고    scopus 로고
    • The selective class i PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutations
    • Tanaka H, Yoshida M, Tanimura H, Fujii T, Sakata K, Tachibana Y, et al. The selective class I PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutations. Clin Cancer Res 2011;17: 3272-81.
    • (2011) Clin Cancer Res , vol.17 , pp. 3272-3281
    • Tanaka, H.1    Yoshida, M.2    Tanimura, H.3    Fujii, T.4    Sakata, K.5    Tachibana, Y.6
  • 34
    • 84871968444 scopus 로고    scopus 로고
    • PIK3CA mutation H1047R is associated with response to PI3K/ AKT/mTOR signaling pathway inhibitors in early-phase clinical trials
    • Janku F, Wheler JJ, Naing A, Falchook GS, Hong DS, Stepanek VM, et al. PIK3CA mutation H1047R is associated with response to PI3K/ AKT/mTOR signaling pathway inhibitors in early-phase clinical trials. Cancer Res 2013;73:276-84.
    • (2013) Cancer Res , vol.73 , pp. 276-284
    • Janku, F.1    Wheler, J.J.2    Naing, A.3    Falchook, G.S.4    Hong, D.S.5    Stepanek, V.M.6
  • 35
    • 79953052206 scopus 로고    scopus 로고
    • Inhibition of PI3K/mTOR pathways in glioblastoma and implications for combination therapy with temozolomide
    • Prasad G, Sottero T, Yang X, Mueller S, James CD, Weiss WA, et al. Inhibition of PI3K/mTOR pathways in glioblastoma and implications for combination therapy with temozolomide. Neuro Oncol 2011;13: 384-92.
    • (2011) Neuro Oncol , vol.13 , pp. 384-392
    • Prasad, G.1    Sottero, T.2    Yang, X.3    Mueller, S.4    James, C.D.5    Weiss, W.A.6
  • 36
    • 84889102598 scopus 로고    scopus 로고
    • Tumor pharmacokinetics (PK) and pharmacodynamics (PD) of SAR245409 (XL765) and SAR245408 (XL147) administered as single agents to patients with recurrent glioblastoma (GBM): An Ivy foundation early-phase clinical trials consortium study
    • (suppl; abstr 2012)
    • Cloughesy TF, Mischel PS, Omuro AMP, Prados M, Wen PY, Wu B, et al. Tumor pharmacokinetics (PK) and pharmacodynamics (PD) of SAR245409 (XL765) and SAR245408 (XL147) administered as single agents to patients with recurrent glioblastoma (GBM): an Ivy foundation early-phase clinical trials consortium study. J Clin Oncol 2013;31 (suppl; abstr 2012).
    • (2013) J Clin Oncol , pp. 31
    • Cloughesy, T.F.1    Mischel, P.S.2    Omuro, A.M.P.3    Prados, M.4    Wen, P.Y.5    Wu, B.6


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.