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WEE1 inhibitors
Friday 10 June 2016
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Examples
MK-1775
Target
WEE1 is a nuclear kinase belonging to the Ser/Thr family of protein kinases in the fission yeast Schizosaccharomyces pombe (S. pombe). It has a molecular mass of 96 kDa and it is a key regulator of cell cycle progression. It influences cell size by inhibiting the entry into mitosis, through inhibiting Cdk1. It has homologues in many other organisms, including mammals.
The mitosis promoting factor MPF also regulates DNA-damage induced apoptosis. Negative regulation of MPF by WEE1 causes aberrant mitosis and thus resistance to DNA-damage induced apoptosis.
Kruppel-like factor 2 (KLF2 ) negatively regulates human WEE1, thus increasing sensitivity to DNA-damage induced apoptosis in cancer cells.
See also
WEE1
References
MK-1775, a Potent Wee1 Inhibitor, Synergizes with Gemcitabine to Achieve Tumor Regressions, Selectively in p53-Deficient Pancreatic Cancer Xenografts.
http://m.clincancerres.aacrjournals.org/content/17/9/2799.long?view=long&pmid;=21389100