This week in therapeutics

Indication

Target/marker/pathway

Summary

Licensing status

Publication and
contact information

Cancer

Cancer

Tankyrase TRF1-interacting ankyrin-related ADP-ribose polymerase (TNKS)

An SAR study identified TNKS inhibitors that could help treat cancer. Rational design studies led to a series of compounds that blocked two substrate-binding pockets formed by TNKS dimers. In vitro, the best of those compounds inhibited TNKS with an IC50 value of 8 nM and prevented wingless-type MMTV integration site (WNT) pathway signaling in cell culture. Next steps include designing and testing more biologically stable derivatives of high-affinity TNKS inhibitors.

SciBX 6(5); doi:10.1038/scibx.2013.111
Published online Feb. 7, 2013

Patent and licensing status undisclosed

Bregman, H. et al. J. Med. Chem.; published online Jan. 14, 2013;
doi:10.1021/jm301607v
Contact: Xin Huang, Amgen Inc., Cambridge, Mass.
e-mail:
hxin@amgen.com