Browsing ICR Divisions by author "Eccles, Suzanne"
Now showing items 1-5 of 5
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Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
Mallinger, A; Crumpler, S; Pichowicz, M; Waalboer, D; Stubbs, M; et al. (AMER CHEMICAL SOC, 2015-02-26)WNT signaling is frequently deregulated in malignancy, particularly in colon cancer, and plays a key role in the generation and maintenance of cancer stem cells. We report the discovery and optimization of a 3,4,5-trisubstituted ... -
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
Mallinger, A; Schiemann, K; Rink, C; Stieber, F; Calderini, M; et al. (AMER CHEMICAL SOC, 2016-02-11)The Mediator complex-associated cyclin-dependent kinase CDK8 has been implicated in human disease, particularly in colorectal cancer where it has been reported as a putative oncogene. Here we report the discovery of 109 ... -
Dual blockade of the PI3K/AKT/mTOR (AZD8055) and RAS/MEK/ERK (AZD6244) pathways synergistically inhibits rhabdomyosarcoma cell growth in vitro and in vivo.
Renshaw, J; Taylor, KR; Bishop, R; Valenti, M; De Haven Brandon, A; et al. (AMER ASSOC CANCER RESEARCH, 2013-08-05)PURPOSE: To provide rationale for using phosphoinositide 3-kinase (PI3K) and/or mitogen-activated protein kinase (MAPK) pathway inhibitors to treat rhabdomyosarcomas, a major cause of pediatric and adolescent cancer deaths. ... -
Synthesis and Evaluation of a 2,11-Cembranoid-Inspired Library.
Welford, AJ; Caldwell, JJ; Liu, M; Richards, M; Brown, N; et al. (WILEY-V C H VERLAG GMBH, 2016-04-11)The 2,11-cembranoid family of natural products has been used as inspiration for the synthesis of a structurally simplified, functionally diverse library of octahydroisobenzofuran-based compounds designed to augment a typical ... -
The epidermal growth factor receptor/Erb-B/HER family in normal and malignant breast biology.
Eccles, SA (UPV/EHU Press, 2011-01-01)The EGFR/Erb-B receptor tyrosine kinases each play distinct and complementary roles in normal breast development. The four receptors form both homodimers and heterodimers in response to binding by ligands which show ...