Analytical Technology and Screening Team
Team Leader: Dr Wynne Aherne
Location: Haddow Laboratories, Sutton
Section: Section of Cancer Therapeutics (including the Cancer Research UK Centre for Cancer Therapeutics)
One of the key steps in target-directed cancer drug discovery is the identification of small molecule compounds (hits) that inhibit the activity of validated target proteins. This can be achieved by high-throughput screening of large compound collections using appropriate biochemical and cell-based assay formats that report the activity of the drug target. The role of the Analytical Technology and Screening Team is to establish, validate and run screens on selected cancer drug targets to carry out the initial characterisation of the hits obtained. Presently, we have a file of over 100,000 compounds. Once progressible compound series have been identified, the Team is involved in supporting medicinal chemistry aimed at understanding and improving the pharmaceutical properties of the hits generated. In addition, mechanistic endpoint assays are developed to support the Centre's drug discovery projects into clinical evaluation. These assays include, high-throughput phenotypic assays based on standard ELISA methodology and high content imaging assays based on the use of the InCell analyser. Current cancer drug targets being exploited include a number of kinases, ATPases and protein:protein interactions as well as signalling pathways and transcription factors.
Aims
- To identify and evaluate compounds with activity against novel cancer drug targets using high-throughput screening and related hit generation approaches
- To develop assays for the measurement of mechanism-based endpoints for pharmacodynamic studies throughout the drug discovery process.
In the Section of Cancer Therapeutics (including the Cancer Research UK Centre for Cancer Therapeutics)
