title: Drugging Undruggable Molecular Cancer Targets.
abstract: Cancer, more than any other human disease, now has a surfeit of potential molecular targets poised for therapeutic exploitation. Currently, a number of attractive and validated cancer targets remain outside of the reach of pharmacological regulation. Some have been described as undruggable, at least by traditional strategies. In this article, we outline the basis for the undruggable moniker, propose a reclassification of these targets as undrugged, and highlight three general classes of this imposing group as exemplars with some attendant strategies currently being explored to reclassify them. Expanding the spectrum of disease-relevant targets to pharmacological manipulation is central to reducing cancer morbidity and mortality.
authors.affiliation: Fiske Drug Discovery Laboratory, Department of Pharmacology, University of Virginia, Charlottesville, Virginia 22908-0735; email: lazo@virginia.edu , ers7g@virginia.edu.
authors.forename: John S
authors.initials: JS
authors.lastname: Lazo
authors.affiliation: Fiske Drug Discovery Laboratory, Department of Pharmacology, University of Virginia, Charlottesville, Virginia 22908-0735; email: lazo@virginia.edu , ers7g@virginia.edu.
authors.forename: Elizabeth R
authors.initials: ER
authors.lastname: Sharlow
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology* / Q000627:therapeutic use*; D006801:Humans; D058990:Molecular Targeted Therapy / Q000379:methods*; D009369:Neoplasms / Q000188:drug therapy*
chemical_list: D000970:Antineoplastic Agents
keywords: RAS; cancer drug targets; oncogenes; phosphatases; transcription factors