P Workman


Affiliation: Institute of Cancer Research
Country: UK


  1. 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). ..
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    Workman P, Burrows F, Neckers L, Rosen N. Drugging the cancer chaperone HSP90: combinatorial therapeutic exploitation of oncogene addiction and tumor stress. Ann N Y Acad Sci. 2007;1113:202-16 pubmed
    ..We stress how basic and translational research has been mutually beneficial and indicate future directions to enhance our understanding of molecular chaperones and their exploitation in cancer and other diseases. ..
  3. Blagg J, Workman P. Chemical biology approaches to target validation in cancer. Curr Opin Pharmacol. 2014;17:87-100 pubmed publisher
    ..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. ..
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    Workman P. Altered states: selectively drugging the Hsp90 cancer chaperone. Trends Mol Med. 2004;10:47-51 pubmed
    ..However, the reason for therapeutic selectivity in cancer cells versus normal cells is unclear. New research now shows that Hsp90 exists in cancer cells in a heightened, activated state that is highly susceptible to inhibition by 17AAG. ..
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    Workman P. Overview: translating Hsp90 biology into Hsp90 drugs. Curr Cancer Drug Targets. 2003;3:297-300 pubmed
    ..The opportunities and challenges involved in translating the fast moving biology of Hsp90 into patient benefit is discussed. ..
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    Workman P. Combinatorial attack on multistep oncogenesis by inhibiting the Hsp90 molecular chaperone. Cancer Lett. 2004;206:149-57 pubmed
    ..This article reviews the current status and future prospects for the exploitation of Hsp90 as a new molecular target for cancer treatment. ..
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    Banerji U, Judson I, Workman P. The clinical applications of heat shock protein inhibitors in cancer - present and future. Curr Cancer Drug Targets. 2003;3:385-90 pubmed
    ..Examples of likely disease targets include chronic myeloid leukaemia, melanoma, breast, ovarian, brain, thyroid, colorectal and prostate cancer. ..
  8. Yap T, Bjerke L, Clarke P, Workman P. Drugging PI3K in cancer: refining targets and therapeutic strategies. Curr Opin Pharmacol. 2015;23:98-107 pubmed publisher
    ..Finally, we envision the future development and use of PI3K inhibitors for the treatment of patients with a range of malignancies. ..
  9. 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. ..

More Information


  1. 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
  2. Workman P, Collins I. Probing the probes: fitness factors for small molecule tools. Chem Biol. 2010;17:561-77 pubmed publisher
  3. Workman P, Davies F. A stressful life (or death): combinatorial proteotoxic approaches to cancer-selective therapeutic vulnerability. Oncotarget. 2011;2:277-80 pubmed
  4. 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. ..
  5. 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. ..
  6. AntolĂ­n 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. ..