New drug discovery strategies produce libraries of potential treatment targets Interview with:

Professor Neil Carragher Principal Investigator Drug Discovery Institute of Genetics and Molecular Medicine University of Edinburgh

Prof. Neil Carragher

Professor Neil Carragher
Principal Investigator Drug Discovery
Institute of Genetics and Molecular Medicine
University of Edinburgh What is the background for this study? What are the main findings?

Prof. Carragher: The aim of the study was to generate novel small molecule inhibitors that target breast cancers using a strategy which we named: “dual ligand based phenotypic screening”. From initial derivation of a small chemical library based on a promiscuous kinase inhibitor PP1, iterative screening across a suite of breast cancer phenotypic assays guided chemical design towards the novel compound eCF506. eCF506 is a highly potent, orally bioavailable and specific inhibitor of Src Kinase. What should readers take away from your report?

Response: The dual ligand based phenotypic screening strategy employed in this program was extremely efficient resulting in the rapid development of a novel drug candidate (eCF506) with excellent physiochemical properties in under 3 years. eCF506 is the first drug candidate of a second generation of Src inhibitors that does not target Abl and will not only help understand the complexity of some cancers but also the development of safer combination therapies which target Src activity. What recommendations do you have for future research as a result of this study?

Response: New drug discovery strategies which guide chemical design using robust cell based phenotypic assays provides an unbiased approach to the design of novel targeted therapeutics. Derivation of small high quality chemical libraries based on known ligands or other chemical starting points accelerates the development of highly potent candidate drugs from cell based phenotypic screens. Is there anything else you would like to add?

Response: Dr Asier Unciti-Broceta and Prof Neil Carragher from the Cancer Research UK: Edinburgh Centre, University of Edinburgh co-led the study and say “this candidate drug will need to undergo further preclinical testing before it can be taken forward into clinical trials but these early findings are very promising. The results provides further support for more rapid and cost-effective drug discovery approaches which can be conducted in both academic and industry groups to deliver more effective medicines at reduced costs for patients and healthcare providers.” Thank you for your contribution to the community.


Craig Fraser, John C. Dawson, Reece Dowling, Douglas R. Houston, Jason T. Weiss, Alison F. Munro, Morwenna Muir, Lea Harrington, Scott P. Webster, Margaret C. Frame, Valerie G. Brunton, E. Elizabeth Patton, Neil O. Carragher, Asier Unciti-Broceta. \

.Journal of Medicinal Chemistry, 2016; DOI:10.1021/acs.jmedchem.6b00065

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