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); TNKS2

In vitro and mouse studies identified a TNKS and TNKS2 dual inhibitor that could be useful for treating cancer. TNKS and TNKS2 regulate multiple cancer-associated pathways. In vitro, the lead molecule selectively inhibited TNKS and TNKS2 with IC50 values of 46 nM and 25 nM, respectively. In mice, the lead molecule showed good bioavailability following intraperitoneal and oral administration. Next steps include developing a strategy to stratify patients with cancer based on their expression of TNKS and TNKS2.

SciBX 6(14); doi:10.1038/scibx.2013.334
Published online April 11, 2013

Patent application filed covering composition of matter; licensing negotiations ongoing

Voronkov, A. et al. J. Med. Chem.; published online March 11, 2013;
doi:10.1021/jm4000566
Contact: Stefan Krauss, Oslo University Hospital, Oslo, Norway
e-mail:
stefan.krauss@rr-research.no

Contact: Jens P. Morth, same affiliation as above
e-mail:
j.p.morth@ncmm.uio.no

Contact: Jo Waaler, same affiliation as above
e-mail:
jo.waaler@rr-research.no