Indication

Target/marker/pathway

Summary

Licensing status

Publication and contact information

Cancer

Cancer

Histone deacetylase 1 (HDAC1); HDAC3

In vitro and mouse studies have identified inhibitors selective for HDAC1 and HDAC3 that could help treat cancer. In vitro, the most potent N-hydroxycinnamamide-based derivatives had low nanomolar potency against HDAC1 and HDAC3 and low micromolar potency against other HDACs. In a panel of solid and hematological tumor cells, the most potent and selective dual inhibitor blocked proliferation better than a nonselective HDAC inhibitor. In mice with subcutaneous lymphoma xenografts, the most potent dual inhibitor decreased tumor growth more than a nonselective inhibitor. Next steps include additional structural optimization of the compounds.

SciBX 7(18); doi:10.1038/scibx.2014.519
Published online May 8, 2014

Patent application filed; available for licensing

Li, X. et al. J. Med. Chem.; published online April 2, 2014;
doi:10.1021/jm401877m
Contact: Wenfang Xu, Shandong University, Shandong, China
e-mail:

xuwenf@gmail.com
Contact: Yingjie Zhang, same affiliation as above
e-mail:

zhangyingjie@sdu.edu.cn