Inhibitors of checkpoint kinases: From discovery to the clinic

J. W. Janetka, S. Ashwell, S. Zabludoff, P. Lyne

Research output: Contribution to journalReview articlepeer-review

58 Scopus citations


Checkpoint kinase 1 (CHK1) is a member of the serine/threonine kinase family. CHK1 functions as a regulatory kinase in cell-cycle progression and is the main effector of the DNA-damage response within the cell. Over the past few years, a large number of novel inhibitors of CHK1 have been discovered that encompass an enormous area of chemical space and diversity and, in more recent reports, many of these inhibitors have been demonstrated preclinically to sensitize tumors to a wide variety of DNA-damaging agents. This review focuses on advances reported both in the literature and at conferences from 2005 to date concerning the chemical design and optimization of checkpoint kinase inhibitors for the treatment of cancer.

Original languageEnglish
Pages (from-to)473-486
Number of pages14
JournalCurrent Opinion in Drug Discovery and Development
Issue number4
StatePublished - Jul 2007


  • Checkpoint kinase
  • DNA damage
  • Kinase inhibitor
  • Potentiation
  • Sensitization


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