Chk1 Inhibitors for Novel Cancer Treatment

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 16, 12 Issues, 2016

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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Michelle Prudhomme
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex

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Chk1 Inhibitors for Novel Cancer Treatment

Anti-Cancer Agents in Medicinal Chemistry, 6(4): 377-388.

Author(s): Zhi-Fu Tao and Nan-Horng Lin.

Affiliation: Cancer Research, Global Pharmaceutical Research&Development, Abbott Laboratories, Abbott Park, IL 60064, USA


Chemo- and radiotherapies that target DNA are the mainstay of cancer treatment. In response to DNA damage, cells are arrested in multiple checkpoints in the cell cycle to allow the damaged DNA to be repaired before progressing into mitosis. Normal cells are arrested in the G1 phase mediated by the p53 tumor suppressor, and p53-deficient cancer cells are arrested in the S or G2 phase. Checkpoint kinase 1 (Chk 1) is a serine / threonine protein kinase and a key mediator in the DNA damage-induced checkpoint network. When the G2 or S checkpoint is abrogated by the inhibition of Chk1, p53-deficient cancer cells undergo mitotic catastrophe and eventually apoptosis, whereas normal cells are still arrested in the G1 phase. Thus, Chk1 inhibitors can preferentially potentiate the efficacy of DNA damaging agents in cancer cells, and Chk1 is an attractive therapeutic target for cancer treatment, especially since approximately 50% of all human cancers are p53-deficient. This review discusses the rationale of Chk1 as an anticancer target, the structural basis for designing Chk1 inhibitors, and recently disclosed Chk1 inhibitors.


Chk1 inhibitor, Anticancer agent, DNA-damaging agent, Adjuvant therapy, DNA damage, Cell cycle, checkpoint, Kinase, Singnal transduction.

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Article Details

Volume: 6
Issue Number: 4
First Page: 377
Last Page: 388
Page Count: 12
DOI: 10.2174/187152006777698132
Price: $58

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