Affiliation: Institute of Cancer Research
- Rye C, Chessum N, Lamont S, Pike K, Faulder P, Demeritt J, et al. Discovery of 4,6-disubstituted pyrimidines as potent inhibitors of the heat shock factor 1 (HSF1) stress pathway and CDK9. Medchemcomm. 2016;7:1580-1586 pubmed..00 ?M). Optimisation of cellular SAR led to an inhibitor with improved potency (25, 15 nM) in the HSF1 phenotypic assay. The 4,6-pyrimidine 25 was also shown to have high potency against the CDK9 enzyme (3 nM). ..
- Workman P, Clarke P, Raynaud F, Van Montfort R. Drugging the PI3 kinome: from chemical tools to drugs in the clinic. Cancer Res. 2010;70:2146-57 pubmed publisher..The challenges and outlook for drugging the PI3 kinome are discussed in the more general context of the role of structural biology and chemical biology in innovative drug discovery. ..
- Workman P, Aboagye E, Balkwill F, Balmain A, Bruder G, Chaplin D, et al. Guidelines for the welfare and use of animals in cancer research. Br J Cancer. 2010;102:1555-77 pubmed publisher....
- Workman P, Collins I. Probing the probes: fitness factors for small molecule tools. Chem Biol. 2010;17:561-77 pubmed publisher....
- Workman P, Davies F. A stressful life (or death): combinatorial proteotoxic approaches to cancer-selective therapeutic vulnerability. Oncotarget. 2011;2:277-80 pubmed
- Banerji U, Workman P. Critical parameters in targeted drug development: the pharmacological audit trail. Semin Oncol. 2016;43:436-45 pubmed publisher..The PhAT is critical in making go-no-go decisions in the development of currently studied drugs and will continue to be relevant to discovery and development of future generations of anticancer agents. ..
- Blagg J, Workman P. Choose and Use Your Chemical Probe Wisely to Explore Cancer Biology. Cancer Cell. 2017;32:9-25 pubmed publisher..We discuss current challenges with the selection and use of chemical probes, and suggest how biologists can and should be more discriminating in the probes they employ. ..
- Antolín A, Tym J, Komianou A, Collins I, Workman P, Al Lazikani B. Objective, Quantitative, Data-Driven Assessment of Chemical Probes. Cell Chem Biol. 2018;25:194-205.e5 pubmed publisher..Probe Miner represents a valuable resource to aid the identification of potential chemical probes, particularly when used alongside expert curation. ..