Blagg, J., Workman, P. (2014) Chemical biology approaches to target validation in cancer. CURRENT OPINION IN PHARMACOLOGY, 17. pp. 87-100. ISSN 1471-4892

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Abstract

Target validation is a crucial element of drug discovery. Especially given the wealth of potential targets emerging from cancer genome sequencing and functional genetic screens, and also considering the time and cost of downstream drug discovery efforts, it is essential to build confidence in a proposed target, ideally using different technical approaches. We argue that complementary biological and chemical biology strategies are essential for robust target validation. We discuss recent progress in the discovery and application of high quality chemical tools and other chemical biology approaches to target validation in cancer. Among other topical examples, we highlight the emergence of designed irreversible chemical tools to study potential target proteins and oncogenic pathways that were hitherto regarded as poorly druggable.

Item Type:	Article
Authors (ICR Faculty only):	Blagg, Julian and Workman, Paul
All Authors:	Blagg, J., Workman, P.
Additional Information:	ISI Document Delivery No.: AS1MJ Times Cited: 0 Cited Reference Count: 111 Blagg, Julian Workman, Paul Cancer Research [C309/A11566]; Cancer Research UK [C309/A8992]; Cancer Research UK Centre; National Institute of Health Research PW and JB are grateful for major core support from Cancer Research [grant number C309/A11566]. PW is a Cancer Research UK Life Fellow [grant number C309/A8992]. The authors acknowledge funding to The Institute of Cancer Research and The Royal Marsden NHS Foundation Trust as a Cancer Research UK Centre and from the National Institute of Health Research to our Biomedical Research Centre. We apologise to the authors of numerous excellent papers that could not be cited because of space constraints. We thank our many colleagues, collaborators and laboratory staff for valuable discussions. We thank Ann Ford, Kate Trotman and Val Cornwell for excellent administrative support. 0 ELSEVIER SCI LTD OXFORD CURR OPIN PHARMACOL
Uncontrolled Keywords:	SMALL-MOLECULE INHIBITOR CHRONIC LYMPHOCYTIC-LEUKEMIA BREAST-CANCER DRUG DISCOVERY IN-VIVO CHAPERONE INHIBITORS ANTITUMOR-ACTIVITY HSP90 INHIBITORS PROSTATE-CANCER SOLID TUMORS
Research teams:	ICR divisions > Cancer Therapeutics > Clinical Pharmacology & Trials (including Drug Metabolism & Pharmacokinetics Group) ICR divisions > Cancer Therapeutics > Signal Transduction & Molecular Pharmacology ICR divisions > Cancer Therapeutics > Medicinal Chemistry 1 (including Analytical Chemistry and In Silico Chemistry)
Depositing User:	Barry Jenkins
Date Deposited:	04 Dec 2014 08:19
Last Modified:	04 Dec 2014 08:19
URI:	http://publications.icr.ac.uk/id/eprint/13739

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