Indication

Target/marker/pathway

Summary

Licensing status

Publication and contact information

Cancer

Cancer

TTK protein kinase (TTK; MPS1)

In vitro and cell culture studies identified an orally bioavailable small molecule inhibitor of MPS1 that could help treat cancer. In vitro SAR studies based on a 1H-pyrrolo[3,2-c]pyridine scaffold yielded a selective MPS1 inhibitor with an in vitro IC50 value of 0.04 mM that was stable in mouse and human microsomes. In a mouse xenograft model of human colon carcinoma, the inhibitor decreased MPS1 activity compared with no treatment. Next steps include testing drug candidates in mouse xenograft models of human breast cancer dependent on high MPS1 activity.

SciBX 7(2); doi:10.1038/scibx.2014.50
Published online Jan. 16, 2014

Patented; licensed by the Cancer Research Technology Pioneer Fund

Naud, S. et al. J. Med. Chem.; published online Nov. 20, 2013;
doi:10.1021/jm401395s
Contact: Julian Blagg, The Institute of Cancer Research, London, U.K.
e-mail:
julian.blagg@icr.ac.uk

Contact: Rob L.M. van Montfort, same affiliation as above
e-mail:
rob.vanmontfort@icr.ac.uk