Now showing items 1-8 of 8

    • Chemosensitivity profiling of osteosarcoma tumour cell lines identifies a model of BRCAness. 

      Holme, H; Gulati, A; Brough, R; Fleuren, EDG; Bajrami, I; Campbell, J; Chong, IY; Costa-Cabral, S; Elliott, R; Fenton, T; Frankum, J; Jones, SE; Menon, M; Miller, R; Pemberton, HN; Postel-Vinay, S; Rafiq, R; Selfe, JL; von Kriegsheim, A; Munoz, AG; Rodriguez, J; Shipley, J; van der Graaf, WTA; Williamson, CT; Ryan, CJ; Pettitt, S; Ashworth, A; Strauss, SJ; Lord, CJ (2018-07-13)
      Osteosarcoma (OS) is an aggressive sarcoma, where novel treatment approaches are required. Genomic studies suggest that a subset of OS, including OS tumour cell lines (TCLs), exhibit genomic loss of heterozygosity (LOH) ...
    • Discovery of Selective Estrogen Receptor Covalent Antagonists for the Treatment of ERαWT and ERαMUT Breast Cancer. 

      Puyang, X; Furman, C; Zheng, GZ; Wu, ZJ; Banka, D; Aithal, K; Agoulnik, S; Bolduc, DM; Buonamici, S; Caleb, B; Das, S; Eckley, S; Fekkes, P; Hao, M-H; Hart, A; Houtman, R; Irwin, S; Joshi, JJ; Karr, C; Kim, A; Kumar, N; Kumar, P; Kuznetsov, G; Lai, WG; Larsen, N; Mackenzie, C; Martin, L-A; Melchers, D; Moriarty, A; Nguyen, T-V; Norris, J; O'Shea, M; Pancholi, S; Prajapati, S; Rajagopalan, S; Reynolds, DJ; Rimkunas, V; Rioux, N; Ribas, R; Siu, A; Sivakumar, S; Subramanian, V; Thomas, M; Vaillancourt, FH; Wang, J; Wardell, S; Wick, MJ; Yao, S; Yu, L; Warmuth, M; Smith, PG; Zhu, P; Korpal, M (2018-09)
      Mutations in estrogen receptor alpha (ERα) that confer resistance to existing classes of endocrine therapies are detected in up to 30% of patients who have relapsed during endocrine treatments. Because a significant ...
    • Immunoassays for the quantification of ALK and phosphorylated ALK support the evaluation of on-target ALK inhibitors in neuroblastoma. 

      Tucker, ER; Tall, JR; Danielson, LS; Gowan, S; Jamin, Y; Robinson, SP; Banerji, U; Chesler, L (2017-08)
      Targeted inhibition of anaplastic lymphoma kinase (ALK) is a successful approach for the treatment of many ALK-aberrant malignancies; however, the presence of resistant mutations necessitates both the development of more ...
    • Preclinical evaluation of the PARP inhibitor BMN-673 for the treatment of ovarian clear cell cancer. 

      Wilkerson, PM; Dedes, KJ; Samartzis, EP; Dedes, I; Lambros, MB; Natrajan, R; Gauthier, A; Piscuoglio, S; Töpfer, C; Vukovic, V; Daley, F; Weigelt, B; Reis-Filho, JS (2017-01)
      PURPOSE:To determine if models of ovarian clear cell carcinomas (OCCCs) harbouring defects in homologous recombination (HR) DNA repair of double strand breaks (DSBs) are sensitive to cisplatin and/or PARP inhibition. ...
    • Significant differences in biological parameters between prodrugs cleavable by carboxypeptidase G2 that generate 3,5-difluoro-phenol and -aniline nitrogen mustards in gene-directed enzyme prodrug therapy systems. 

      Niculescu-Duvaz, I; Scanlon, I; Niculescu-Duvaz, D; Friedlos, F; Martin, J; Marais, R; Springer, CJ (2004-05)
      Nine new nitrogen mustard compounds derived from 2,6-difluoro-4-hydroxy- (3a-e) and 2,6-difluoro-4-amino- (4a-d) aniline were synthesized as potential prodrugs. They were designed to be activated to their corresponding ...
    • Structure-Based Optimization of Potent, Selective, and Orally Bioavailable CDK8 Inhibitors Discovered by High-Throughput Screening. 

      Czodrowski, P; Mallinger, A; Wienke, D; Esdar, C; Pöschke, O; Busch, M; Rohdich, F; Eccles, SA; Ortiz-Ruiz, M-J; Schneider, R; Raynaud, FI; Clarke, PA; Musil, D; Schwarz, D; Dale, T; Urbahns, K; Blagg, J; Schiemann, K (2016-10-07)
      The mediator complex-associated cyclin dependent kinase CDK8 regulates β-catenin-dependent transcription following activation of WNT signaling. Multiple lines of evidence suggest CDK8 may act as an oncogene in the development ...
    • Synthetic Lethal Targeting of ARID1A-Mutant Ovarian Clear Cell Tumors with Dasatinib. 

      Miller, RE; Brough, R; Bajrami, I; Williamson, CT; McDade, S; Campbell, J; Kigozi, A; Rafiq, R; Pemberton, H; Natrajan, R; Joel, J; Astley, H; Mahoney, C; Moore, JD; Torrance, C; Gordan, JD; Webber, JT; Levin, RS; Shokat, KM; Bandyopadhyay, S; Lord, CJ; Ashworth, A (2016-07)
      New targeted approaches to ovarian clear cell carcinomas (OCCC) are needed, given the limited treatment options in this disease and the poor response to standard chemotherapy. Using a series of high-throughput cell-based ...
    • Targeting DNA Repair in Cancer: Beyond PARP Inhibitors. 

      Brown, JS; O'Carrigan, B; Jackson, SP; Yap, TA (2017-01)
      Germline aberrations in critical DNA-repair and DNA damage-response (DDR) genes cause cancer predisposition, whereas various tumors harbor somatic mutations causing defective DDR/DNA repair. The concept of synthetic lethality ...