Now showing items 1-7 of 7

    • EGFR feedback-inhibition by Ran-binding protein 6 is disrupted in cancer. 

      Oldrini, B; Hsieh, W-Y; Erdjument-Bromage, H; Codega, P; Carro, MS; Curiel-García, A; Campos, C; Pourmaleki, M; Grommes, C; Vivanco, I; Rohle, D; Bielski, CM; Taylor, BS; Hollmann, TJ; Rosenblum, M; Tempst, P; Blenis, J; Squatrito, M; Mellinghoff, IK (2017-12-11)
      Transport of macromolecules through the nuclear pore by importins and exportins plays a critical role in the spatial regulation of protein activity. How cancer cells co-opt this process to promote tumorigenesis remains ...
    • Inhibitors in AKTion: ATP-competitive vs allosteric. 

      Lazaro, G; Kostaras, E; Vivanco, I (2020-06)
      Aberrant activation of the PI3K pathway is one of the commonest oncogenic events in human cancer. AKT is a key mediator of PI3K oncogenic function, and thus has been intensely pursued as a therapeutic target. Multiple AKT ...
    • A kinase-independent function of AKT promotes cancer cell survival. 

      Vivanco, I; Chen, ZC; Tanos, B; Oldrini, B; Hsieh, W-Y; Yannuzzi, N; Campos, C; Mellinghoff, IK (2014-12-31)
      The serine-threonine kinase AKT regulates proliferation and survival by phosphorylating a network of protein substrates. In this study, we describe a kinase-independent function of AKT. In cancer cells harboring gain-of-function ...
    • Mathematical modeling identifies optimum lapatinib dosing schedules for the treatment of glioblastoma patients. 

      Stein, S; Zhao, R; Haeno, H; Vivanco, I; Michor, F (2018-01-02)
      Human primary glioblastomas (GBM) often harbor mutations within the epidermal growth factor receptor (EGFR). Treatment of EGFR-mutant GBM cell lines with the EGFR/HER2 tyrosine kinase inhibitor lapatinib can effectively ...
    • Orally bioavailable CDK9/2 inhibitor shows mechanism-based therapeutic potential in MYCN-driven neuroblastoma. 

      Poon, E; Liang, T; Jamin, Y; Walz, S; Kwok, C; Hakkert, A; Barker, K; Urban, Z; Thway, K; Zeid, R; Hallsworth, A; Box, G; Ebus, ME; Licciardello, MP; Sbirkov, Y; Lazaro, G; Calton, E; Costa, BM; Valenti, M; De Haven Brandon, A; Webber, H; Tardif, N; Almeida, GS; Christova, R; Boysen, G; Richards, MW; Barone, G; Ford, A; Bayliss, R; Clarke, PA; De Bono, J; Gray, NS; Blagg, J; Robinson, SP; Eccles, SA; Zheleva, D; Bradner, JE; Molenaar, J; Vivanco, I; Eilers, M; Workman, P; Lin, CY; Chesler, L (2020-11)
      The undruggable nature of oncogenic Myc transcription factors poses a therapeutic challenge in neuroblastoma, a pediatric cancer in which MYCN amplification is strongly associated with unfavorable outcome. Here, we show ...
    • A systematic molecular and pharmacologic evaluation of AKT inhibitors reveals new insight into their biological activity. 

      Kostaras, E; Kaserer, T; Lazaro, G; Heuss, SF; Hussain, A; Casado, P; Hayes, A; Yandim, C; Palaskas, N; Yu, Y; Schwartz, B; Raynaud, F; Chung, Y-L; Cutillas, PR; Vivanco, I (2020-08)
      <h4>Background</h4>AKT, a critical effector of the phosphoinositide 3-kinase (PI3K) signalling cascade, is an intensely pursued therapeutic target in oncology. Two distinct classes of AKT inhibitors have been in clinical ...
    • Targeting molecular addictions in cancer. 

      Vivanco, I (2014-11)
      Cancer cells depend on a finite number of critical signals for their survival. Oncogene addiction, that is, the acquired dependence of a cancer cell on the activity of a single oncogenic gene product, has been the basis ...