Current Project Portfolio
Section: Cancer Research UK Cancer Therapeutics Unit
Mitotic Kinase Inhibitors
Projects are underway to design and synthesise selective, orally bioavailable small molecule inhibitors of mitotic kinases that have an oncogenic role in defined cancer patient populations. This work is in collaboration with Dr Spiros Linardopoulos (also in the Breakthrough Breast Cancer Research Centre) and Dr Richard Bayliss and Dr Rob van Montfort in the Section of Structural Biology.
WNT Pathway Inhibitors
A cell-based phenotypic screen has been successfully used to identify drug like chemical matter that blocks the WNT pathway in a specific manner. Medicinal chemistry driven progression of this chemical matter is underway in collaboration with Merck Serono and Professor Trevor Dale at The University of Cardiff.
Fragment-based Hit Discovery
In collaboration with Dr Rob van Montfort and Dr Nathan Brown we have established libraries of low molecular weight fragments to enable hit discovery. Subsequent hit follow-up is enabled using high-throughput X-ray crystal structure analyses coupled with biophysical techniques.
In Silico Target Design and Selection
In collaboration with Dr Nathan Brown and Dr Bissan Al-Lazikani we are building a state of the art suite of in silico tools to enable fast and effective small molecule target design and target selection. These in silico tools include virtual screening and scaffold hopping protocols, clustering algorithms and isostere replacement tools. In addition, we have a major interest in the integration of chemical and biological datasets to educate the selection of appropriate biological targets, biomarkers and drug discovery approaches.