Now showing items 21-24 of 24

    • RNAi screen reveals synthetic lethality between cyclin G-associated kinase and FBXW7 by inducing aberrant mitoses. 

      Dolly, SO; Gurden, MD; Drosopoulos, K; Clarke, P; de Bono, J; Kaye, S; Workman, P; Linardopoulos, S (2017-09)
      F-box and WD40 repeat domain-containing 7 (FBXW7) is an E3 ubiquitin ligase involved in the ubiquitination and degradation of multiple oncogenic substrates. The tumour suppressor function is frequently lost in multiple ...
    • A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease. 

      Dale, T; Clarke, PA; Esdar, C; Waalboer, D; Adeniji-Popoola, O; Ortiz-Ruiz, M-J; Mallinger, A; Samant, RS; Czodrowski, P; Musil, D; Schwarz, D; Schneider, K; Stubbs, M; Ewan, K; Fraser, E; TePoele, R; Court, W; Box, G; Valenti, M; de Haven Brandon, A; Gowan, S; Rohdich, F; Raynaud, F; Schneider, R; Poeschke, O; Blaukat, A; Workman, P; Schiemann, K; Eccles, SA; Wienke, D; Blagg, J (2015-12)
      There is unmet need for chemical tools to explore the role of the Mediator complex in human pathologies ranging from cancer to cardiovascular disease. Here we determine that CCT251545, a small-molecule inhibitor of the WNT ...
    • Small-molecule targeting of brachyury transcription factor addiction in chordoma. 

      Sharifnia, T; Wawer, MJ; Chen, T; Huang, Q-Y; Weir, BA; Sizemore, A; Lawlor, MA; Goodale, A; Cowley, GS; Vazquez, F; Ott, CJ; Francis, JM; Sassi, S; Cogswell, P; Sheppard, HE; Zhang, T; Gray, NS; Clarke, PA; Blagg, J; Workman, P; Sommer, J; Hornicek, F; Root, DE; Hahn, WC; Bradner, JE; Wong, KK; Clemons, PA; Lin, CY; Kotz, JD; Schreiber, SL (2019-02)
      Chordoma is a primary bone cancer with no approved therapy1. The identification of therapeutic targets in this disease has been challenging due to the infrequent occurrence of clinically actionable somatic mutations in ...
    • 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 ...