This week in therapeutics

Indication

Target/marker/pathway

Summary

Licensing status

Publication and contact information

Cancer

Colorectal cancer

b-Catenin (CTNNB1); yes-associated protein 1
(YAP1); v-yes-1 Yamaguchi sarcoma viral oncogene homolog 1 (YES1; Yes)

Studies in cancer cell lines suggest inhibiting YES1 could help treat CTNNB1-driven colon cancers. In a panel of colon cancer cell lines with high CTNNB1 activity, YAP1 knockdown decreased proliferation compared with no knockdown. In CTNNB1-driven colon cancer cell lines, knockdown of YES1, which phosphorylates YAP1 to regulate its transcriptional activity, or nonspecific inhibition of YES1 with Sprycel dasatinib decreased proliferation compared with no knockdown or inhibition. Next steps include designing clinical studies to test whether inhibiting YES1 has a therapeutic benefit and setting up screens to identify YES1 inhibitors.
Bristol-Myers Squibb Co. markets Sprycel to treat acute lymphoblastic leukemia (ALL) and chronic myelogenous leukemia (CML).

SciBX 6(1); doi:10.1038/scibx.2013.6
Published online Jan. 10, 2013

Patent application filed; available for licensing

Rosenbluh, J. et al. Cell; published online Dec. 13, 2012;
doi:10.1016/j.cell.2012.11.026
Contact: William C. Hahn, Dana-Farber Cancer Institute, Boston, Mass.
e-mail:
william_hahn@dfci.harvard.edu