This week in therapeutics

Indication

Target/marker/pathway

Summary

Licensing status

Publication and
contact information

Cancer

Colorectal
cancer

Mixed lineage kinase 4 (KIAA1804; MLK4); K-Ras

An in vitro and mouse study suggests inhibiting MLK4 could help treat a subset of colorectal cancers with mutant K-Ras. In vitro, mutant variants of MLK4 had greater kinase activity than the wild-type enzyme. In xenograft mouse models of colorectal cancer driven by mutant K-Ras, knockdown or knockout of MLK4 decreased tumor formation compared with no knockdown or knockout. Next steps include developing small molecule inhibitors of MLK4 and testing them in cell-based and xenograft mouse models of K-Ras-mutant colorectal cancer.

SciBX 6(5); doi:10.1038/scibx.2013.112
Published online Feb. 7, 2013

Patented; licensing status undisclosed

Martini, M. et al. Cancer Res.; published online Jan. 14, 2013;
doi:10.1158/0008-5472.CAN-12-3074
Contact: Alberto Bardelli, University of Torino, Torino, Italy
e-mail:
alberto.bardelli@unito.it