Indication

Target/marker/pathway

Summary

Licensing status

Publication and contact information

Cancer

Cancer

G protein-coupled receptor 39
(GPR39); smoothened (SMO)

In vitro studies suggest agonizing GPR39 could inhibit the hedgehog pathway to help treat cancer. A cell-based screen for hedgehog pathway inhibitors identified cyclohexyl-methyl aminopyrimidines (CMAPs) that inhibited the pathway downstream of SMO. In mouse cells with an active hedgehog pathway, siRNA targeting Gpr39 attenuated CMAP-induced loss of cellular viability. In the mouse cell lines, overexpression of Gpr39 increased CMAP-induced loss of cellular viability compared with wild-type expression. Next steps include identifying specific hedgehog-dependent cancers that express GPR39.
Heptares Therapeutics Ltd. has a GPR39 agonist in preclinical testing to treat diabetes.

SciBX 7(16); doi:10.1038/scibx.2014.455
Published online April 24, 2014

Patent status undisclosed; available for licensing

Bassilana, F. et al. Nat. Chem. Biol.; published online March 16, 2014;
doi:10.1038/nchembio.1481
Contact: Sarah J. Luchansky, Novartis Institutes for BioMedical Research, Cambridge, Mass.
e-mail:

sarah.luchansky@novartis.com
Contact: Rishi K. Jain, same affiliation as above
e-mail:

rishi.jain@novartis.com