Indication

Target/marker/pathway

Summary

Licensing status

Publication and contact information

Cancer

Sarcoma

Protein kinase Cb (PRKCB)

In vitro and mouse studies suggest PRKCB inhibitors could help treat Ewing's sarcoma. PRKCB was overexpressed in primary Ewing's sarcomas compared with primary medulloblastomas and other pediatric tumor types. In Ewing's sarcoma cell lines, PRKCB small hairpin RNA or enzastaurin decreased proliferation and survival compared with scrambled control shRNA or vehicle. In mice with xenograft Ewing's sarcoma tumors, PRKCB shRNA or enzastaurin decreased tumor volume compared with scrambled control shRNA or vehicle. Next steps could include testing PRKCB inhibition in animal models of metastatic Ewing's sarcoma.
Arxxant ruboxistaurin, a synthetic PRKCB inhibitor from Eli Lilly and Co., is in registration to treat diabetic retinopathy.
Enzastaurin (LY31765), an inhibitor of PRKCB and protein kinase B (PKB; PKBA; AKT; AKT1) from Eli Lilly, is in Phase III
testing to treat B cell lymphoma.

SciBX 5(37); doi:10.1038/scibx.2012.981
Published online Sept. 20, 2012

Patent and licensing status unavailable

Surdez, D. et al. Cancer Res.;
published online Aug. 30, 2012;
doi:10.1158/0008-5472.CAN-12-0371
Contact: Franck Tirode, Curie Institute, Paris, France
e-mail:
franck.tirode@curie.fr