This week in therapeutics

Indication

Target/marker/pathway

Summary

Licensing status

Publication and contact information

Cancer

Prostate cancer

Enhancer of zeste homolog 2 (EZH2); protein kinase B (PKB; PKBA; AKT; AKT1)

Cell culture studies suggest inhibiting the histone methyltransferase EZH2 could help treat prostate cancer. In androgen-independent prostate cancer cells, EZH2 methyltransferase activity and AKT-dependent phosphorylation of EZH2 were required for activation of target genes associated with castration-resistant disease. Next steps could include designing EZH2 inhibitors that block enzymatic activity and prevent AKT-mediated activation or testing the AKT plus EZH2 inhibitors in preclinical models of androgen-independent prostate cancer.

SciBX 6(1); doi:10.1038/scibx.2013.11
Published online Jan. 10, 2013

Patent and licensing status undisclosed

Xu, K. et al. Science; published online Dec. 14, 2012;
doi:10.1126/science.1227604
Contact: Myles Brown, Dana-Farber Cancer Institute, Boston, Mass.
e-mail:
myles_brown@dfci.harvard.edu

Contact: X. Shirley Liu, same affiliation as above
e-mail:
xsliu@jimmy.harvard.edu