메뉴 건너뛰기




Volumn 7, Issue 11, 2012, Pages

RAD001 Enhances the Potency of BEZ235 to Inhibit mTOR Signaling and Tumor Growth

Author keywords

[No Author keywords available]

Indexed keywords

1 (1 CYANO 1 METHYLETHYL) 3 METHYL 8 (3 QUINOLINYL)IMIDAZO[4,5 C]QUINOLIN 2(1H,3H) ONE; EPIDERMAL GROWTH FACTOR RECEPTOR 2; EVEROLIMUS; K RAS PROTEIN; MAMMALIAN TARGET OF RAPAMYCIN; PHOSPHATIDYLINOSITOL 3,4,5 TRISPHOSPHATE 3 PHOSPHATASE; PROTEIN KINASE LKB1; VON HIPPEL LINDAU PROTEIN;

EID: 84869122157     PISSN: None     EISSN: 19326203     Source Type: Journal    
DOI: 10.1371/journal.pone.0048548     Document Type: Article
Times cited : (27)

References (25)
  • 1
    • 34347220473 scopus 로고    scopus 로고
    • Defining the Role of mTOR in Cancer
    • Guertin DA, Sabatini DM, (2007) Defining the Role of mTOR in Cancer. Cancer Cell 12: 9-22.
    • (2007) Cancer Cell , vol.12 , pp. 9-22
    • Guertin, D.A.1    Sabatini, D.M.2
  • 2
    • 33745307617 scopus 로고    scopus 로고
    • Ras, PI(3)K and mTOR signalling controls tumour cell growth
    • Shaw RJ, Cantley LC, (2006) Ras, PI(3)K and mTOR signalling controls tumour cell growth. Nature 441: 424-430.
    • (2006) Nature , vol.441 , pp. 424-430
    • Shaw, R.J.1    Cantley, L.C.2
  • 3
    • 58649114084 scopus 로고    scopus 로고
    • mTOR complex 2 is required for the development of prostate cancer induced by Pten loss in mice
    • Guertin DA, Stevens DM, Saitoh M, Kinkel S, Crosby K, et al. (2009) mTOR complex 2 is required for the development of prostate cancer induced by Pten loss in mice. Cancer Cell 15: 148-159.
    • (2009) Cancer Cell , vol.15 , pp. 148-159
    • Guertin, D.A.1    Stevens, D.M.2    Saitoh, M.3    Kinkel, S.4    Crosby, K.5
  • 4
    • 77649286736 scopus 로고    scopus 로고
    • Genetic dissection of the oncogenic mTOR pathway reveals druggable addiction to translational control via 4EBP-eIF4E
    • Hsieh AC, Costa M, Zollo O, Davis C, Feldman ME, et al. (2010) Genetic dissection of the oncogenic mTOR pathway reveals druggable addiction to translational control via 4EBP-eIF4E. Cancer Cell 17: 249-261 S1535-6108(10)00039-5 [pii];10.1016/j.ccr.2010.01.021 [doi].
    • (2010) Cancer Cell , vol.17 , pp. 249-261
    • Hsieh, A.C.1    Costa, M.2    Zollo, O.3    Davis, C.4    Feldman, M.E.5
  • 5
    • 32044465506 scopus 로고    scopus 로고
    • TOR signaling in growth and metabolism
    • Wullschleger S, Loewith R, Hall MN, (2006) TOR signaling in growth and metabolism. Cell 124: 471-484 S0092-8674(06)00108-5 [pii];10.1016/j.cell.2006.01.016 [doi].
    • (2006) Cell , vol.124 , pp. 471-484
    • Wullschleger, S.1    Loewith, R.2    Hall, M.N.3
  • 6
    • 77950516104 scopus 로고    scopus 로고
    • mTOR signaling and drug development in cancer
    • Dancey J, (2010) mTOR signaling and drug development in cancer. Nat Rev Clin Oncol 7: 209-219 nrclinonc.2010.21 [pii];10.1038/nrclinonc.2010.21 [doi].
    • (2010) Nat Rev Clin Oncol , vol.7 , pp. 209-219
    • Dancey, J.1
  • 7
    • 79953204005 scopus 로고    scopus 로고
    • Blocking the mTOR pathway: A drug discovery perspective
    • Garcia-Echeverria C, (2011) Blocking the mTOR pathway: A drug discovery perspective. Biochemical Society Transactions 39: 451-455.
    • (2011) Biochemical Society Transactions , vol.39 , pp. 451-455
    • Garcia-Echeverria, C.1
  • 8
    • 79955785100 scopus 로고    scopus 로고
    • Pushing the envelope in the mTOR pathway: the second generation of inhibitors
    • Vilar E, Perez-Garcia J, Tabernero J, (2011) Pushing the envelope in the mTOR pathway: the second generation of inhibitors. Mol Cancer Ther 10: 395-403 1535-7163.MCT-10-0905 [pii];10.1158/1535-7163.MCT-10-0905 [doi].
    • (2011) Mol Cancer Ther , vol.10 , pp. 395-403
    • Vilar, E.1    Perez-Garcia, J.2    Tabernero, J.3
  • 9
    • 77953091045 scopus 로고    scopus 로고
    • Structure of the human mTOR complex I and its implications for rapamycin inhibition
    • Yip CK, Murata K, Walz T, Sabatini DM, Kang SA, (2010) Structure of the human mTOR complex I and its implications for rapamycin inhibition. Mol Cell 38: 768-774 S1097-2765(10)00379-5 [pii];10.1016/j.molcel.2010.05.017 [doi].
    • (2010) Mol Cell , vol.38 , pp. 768-774
    • Yip, C.K.1    Murata, K.2    Walz, T.3    Sabatini, D.M.4    Kang, S.A.5
  • 10
    • 33646023695 scopus 로고    scopus 로고
    • Prolonged rapamycin treatment inhibits mTORC2 assembly and Akt/PKB
    • Sarbassov DD, Ali SM, Sengupta S, Sheen JH, Hsu PP, et al. (2006) Prolonged rapamycin treatment inhibits mTORC2 assembly and Akt/PKB. Mol Cell 22: 159-168 S1097-2765(06)00218-8 [pii];10.1016/j.molcel.2006.03.029 [doi].
    • (2006) Mol Cell , vol.22 , pp. 159-168
    • Sarbassov, D.D.1    Ali, S.M.2    Sengupta, S.3    Sheen, J.H.4    Hsu, P.P.5
  • 11
    • 51049109033 scopus 로고    scopus 로고
    • Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity
    • Maira S-M, Stauffer F, Brueggen J, Furet P, Schnell C, et al. (2008) Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity. Molecular Cancer Therapeutics 7: 1851-1863.
    • (2008) Molecular Cancer Therapeutics , vol.7 , pp. 1851-1863
    • Maira, S.-M.1    Stauffer, F.2    Brueggen, J.3    Furet, P.4    Schnell, C.5
  • 12
    • 33646382364 scopus 로고    scopus 로고
    • A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma
    • Fan QW, Knight ZA, Goldenberg DD, Yu W, Mostov KE, et al. (2006) A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma. Cancer Cell 9: 341-349 S1535-6108(06)00116-4 [pii];10.1016/j.ccr.2006.03.029 [doi].
    • (2006) Cancer Cell , vol.9 , pp. 341-349
    • Fan, Q.W.1    Knight, Z.A.2    Goldenberg, D.D.3    Yu, W.4    Mostov, K.E.5
  • 13
    • 56249147509 scopus 로고    scopus 로고
    • Rapamycin differentially inhibits S6Ks and 4E-BP1 to mediate cell-type-specific repression of mRNA translation
    • Choo AY, Yoon SO, Kim SG, Roux PP, Blenis J, (2008) Rapamycin differentially inhibits S6Ks and 4E-BP1 to mediate cell-type-specific repression of mRNA translation. Proc Natl Acad Sci U S A 105: 17414-17419 0809136105 [pii];10.1073/pnas.0809136105 [doi].
    • (2008) Proc Natl Acad Sci U S A , vol.105 , pp. 17414-17419
    • Choo, A.Y.1    Yoon, S.O.2    Kim, S.G.3    Roux, P.P.4    Blenis, J.5
  • 14
    • 61349141302 scopus 로고    scopus 로고
    • Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2
    • Feldman ME, Apsel B, Uotila A, Loewith R, Knight ZA, et al. (2009) Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2. PLoS Biol 7: e38 08-PLBI-RA-4959 [pii];10.1371/journal.pbio.1000038 [doi].
    • (2009) PLoS Biol , vol.7
    • Feldman, M.E.1    Apsel, B.2    Uotila, A.3    Loewith, R.4    Knight, Z.A.5
  • 15
    • 67650312583 scopus 로고    scopus 로고
    • Ku-0063794 is a specific inhibitor of the mammalian target of rapamycin (mTOR)
    • Garcia-Martinez JM, Moran J, Clarke RG, Gray A, Cosulich SC, et al. (2009) Ku-0063794 is a specific inhibitor of the mammalian target of rapamycin (mTOR). Biochem J 421: 29-42 BJ20090489 [pii];10.1042/BJ20090489 [doi].
    • (2009) Biochem J , vol.421 , pp. 29-42
    • Garcia-Martinez, J.M.1    Moran, J.2    Clarke, R.G.3    Gray, A.4    Cosulich, S.C.5
  • 17
    • 65549145048 scopus 로고    scopus 로고
    • An ATP-competitive mammalian target of rapamycin inhibitor reveals rapamycin-resistant functions of mTORC1
    • Thoreen CC, Kang SA, Chang JW, Liu Q, Zhang J, et al. (2009) An ATP-competitive mammalian target of rapamycin inhibitor reveals rapamycin-resistant functions of mTORC1. J Biol Chem 284: 8023-8032 M900301200 [pii];10.1074/jbc.M900301200 [doi].
    • (2009) J Biol Chem , vol.284 , pp. 8023-8032
    • Thoreen, C.C.1    Kang, S.A.2    Chang, J.W.3    Liu, Q.4    Zhang, J.5
  • 18
    • 68049137608 scopus 로고    scopus 로고
    • Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin
    • Yu K, Toral-Barza L, Shi C, Zhang WG, Lucas J, et al. (2009) Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin. Cancer Res 69: 6232-6240 0008-5472.CAN-09-0299 [pii];10.1158/0008-5472.CAN-09-0299 [doi].
    • (2009) Cancer Res , vol.69 , pp. 6232-6240
    • Yu, K.1    Toral-Barza, L.2    Shi, C.3    Zhang, W.G.4    Lucas, J.5
  • 19
    • 79958816470 scopus 로고    scopus 로고
    • The combination of RAD001 and NVP-BEZ235 exerts synergistic anticancer activity against non-small cell lung cancer in vitro and in vivo
    • Xu CX, Li Y, Yue P, Owonikoko TK, Ramalingam SS, et al. (2011) The combination of RAD001 and NVP-BEZ235 exerts synergistic anticancer activity against non-small cell lung cancer in vitro and in vivo. PLoS One 6: e20899 10.1371/journal.pone.0020899 [doi];PONE-D-11-05608 [pii].
    • (2011) PLoS One , vol.6
    • Xu, C.X.1    Li, Y.2    Yue, P.3    Owonikoko, T.K.4    Ramalingam, S.S.5
  • 20
    • 84862895179 scopus 로고    scopus 로고
    • mTOR Inhibitors Synergize on Regression, Reversal of Gene Expression, and Autophagy in Hepatocellular Carcinoma
    • Thomas HE, Mercer CA, Carnevalli LS, Park J, Andersen JB, et al. (2012) mTOR Inhibitors Synergize on Regression, Reversal of Gene Expression, and Autophagy in Hepatocellular Carcinoma. Sci Transl Med scitranslmed.3003923 [pii];10.1126/scitranslmed.3003923 [doi].
    • (2012) Sci Transl Med
    • Thomas, H.E.1    Mercer, C.A.2    Carnevalli, L.S.3    Park, J.4    Andersen, J.B.5
  • 21
    • 67650488269 scopus 로고    scopus 로고
    • Synergistic drug combinations tend to improve therapeutically relevant selectivity
    • Lehar J, Krueger AS, Avery W, Heilbut AM, Johansen LM, et al. (2009) Synergistic drug combinations tend to improve therapeutically relevant selectivity. Nat Biotechnol 27: 659-666 nbt.1549 [pii];10.1038/nbt.1549 [doi].
    • (2009) Nat Biotechnol , vol.27 , pp. 659-666
    • Lehar, J.1    Krueger, A.S.2    Avery, W.3    Heilbut, A.M.4    Johansen, L.M.5
  • 22
    • 33845762340 scopus 로고    scopus 로고
    • Multi-target therapeutics: when the whole is greater than the sum of the parts
    • Zimmermann GR, Lehar J, Keith CT, (2007) Multi-target therapeutics: when the whole is greater than the sum of the parts. Drug Discov Today 12: 34-42 S1359-6446(06)00469-7 [pii];10.1016/j.drudis.2006.11.008 [doi].
    • (2007) Drug Discov Today , vol.12 , pp. 34-42
    • Zimmermann, G.R.1    Lehar, J.2    Keith, C.T.3
  • 23
    • 76049123027 scopus 로고    scopus 로고
    • Specific apoptosis induction by the dual PI3K/mTor inhibitor NVP-BEZ235 in HER2 amplified and PIK3CA mutant breast cancer cells
    • Brachmann SM, Hofmann I, Schnell C, Fritsch C, Wee S, et al. (2009) Specific apoptosis induction by the dual PI3K/mTor inhibitor NVP-BEZ235 in HER2 amplified and PIK3CA mutant breast cancer cells. Proc Natl Acad Sci U S A 106: 22299-22304 0905152106 [pii];10.1073/pnas.0905152106 [doi].
    • (2009) Proc Natl Acad Sci U S A , vol.106 , pp. 22299-22304
    • Brachmann, S.M.1    Hofmann, I.2    Schnell, C.3    Fritsch, C.4    Wee, S.5
  • 24
    • 57349194139 scopus 로고    scopus 로고
    • Effective use of PI3K and MEK inhibitors to treat mutant Kras G12D and PIK3CA H1047R murine lung cancers
    • Engelman JA, Chen L, Tan X, Crosby K, Guimaraes AR, et al. (2008) Effective use of PI3K and MEK inhibitors to treat mutant Kras G12D and PIK3CA H1047R murine lung cancers. Nat Med 14: 1351-1356 nm.1890 [pii];10.1038/nm.1890 [doi].
    • (2008) Nat Med , vol.14 , pp. 1351-1356
    • Engelman, J.A.1    Chen, L.2    Tan, X.3    Crosby, K.4    Guimaraes, A.R.5
  • 25
    • 75749146563 scopus 로고    scopus 로고
    • Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors
    • Zhang J, Adrian FJ, Jahnke W, Cowan-Jacob SW, Li AG, et al. (2010) Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors. Nature 463: 501-506 nature08675 [pii];10.1038/nature08675 [doi].
    • (2010) Nature , vol.463 , pp. 501-506
    • Zhang, J.1    Adrian, F.J.2    Jahnke, W.3    Cowan-Jacob, S.W.4    Li, A.G.5


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.