This week in therapeutics

Indication

Target/marker/pathway

Summary

Licensing status

Publication and contact information

Cancer

Cancer

Choline kinase-a (CHKA)

In vitro studies identified a CHKA inhibitor that could help treat cancers. An asymmetrical, biscationic inhibitor of CHKA that interacts with the choline-binding site exclusively and opens an adjacent binding site had about 200-fold selectivity for CHKA over CHKB. In human cervical carcinoma cells, the inhibitor induced apoptosis and decreased cell proliferation compared with vehicle. Next steps include testing the inhibitor in vivo and improving selectivity.

SciBX 7(6); doi:10.1038/scibx.2014.165
Published online Feb. 13, 2014

Patent application filed; available for licensing

Ruiz, B. et al. J. Med. Chem.;
published online Jan. 4, 2014;
doi:10.1021/jm401665x
Contact: Ana Conejo-García, University of Granada, Granada, Spain
e-mail:
aconejo@ugr.es