Indication

Target/marker/pathway

Summary

Licensing status

Publication and contact information

Cancer

Cancer

TTK protein kinase (TTK; MPS1)

In vitro and rat studies suggest a new class of MPS1 inhibitors could help treat cancer. Ttk knockdown has previously been shown to reduce survival and induce apoptosis in cancer cells. Chemical synthesis, SAR and in vitro testing identified several indazole analogs as selective, potent, nanomolar inhibitors of MPS1. Two lead compounds inhibited proliferation of a human lung cancer cell line at nanomolar IC50 values and exhibited modest oral bioavailability in rats. Future studies could include improving the bioavailability of the lead compounds.

SciBX 6(20); doi:10.1038/scibx.2013.490
Published online May 23, 2013

Patent and licensing status unavailable

Kusakabe, K.-i. et al. J. Med. Chem.; published online May 1, 2013;
doi:10.1021/jm4000215
Contact: Ken-ichi Kusakabe, Shionogi Pharmaceutical Research Center, Osaka, Japan
e-mail:
ken-ichi.kusakabe@shionogi.co.jp