This week in therapeutics

Indication

Target/marker/pathway

Summary

Licensing status

Publication and contact information

Cancer

Cancer

Phosphodiesterase d subunit (PDEd); Ras

Mouse studies suggest inhibiting an interaction between Ras and the PDEd subunit could help treat cancer. PDEd binds lipid-modified Ras and facilitates Ras relocalization and activation. An in vitro high throughput screen and subsequent SAR study identified deltarasin as a small molecule inhibitor of the Ras-PDEd interaction. In a mouse xenograft model for human pancreatic cancer, deltarasin decreased tumor growth compared with vehicle. Next steps include identifying new chemotypes that target the PDEd-Ras binding site and developing a drug candidate based on deltarasin.

SciBX 6(23); doi:10.1038/scibx.2013.574
Published online June 13, 2013

Compound class is patented; available for licensing

Zimmerman, G. et al. Nature; published online May 22, 2013;
doi:10.1038/nature12205
Contact: Herbert Waldmann, Max Planck Institute of Molecular Physiology, Dortmund, Germany
e-mail:
herbert.waldmann@mpi-dortmund.mpg.de

Contact: Philippe I.H. Bastiaens, same affiliation as above
e-mail:
philippe.bastiaens@mpi-dortmund.mpg.de

Contact: Alfred Wittinghofer, same affiliation as above
e-mail:
alfred.wittinghofer@mpi-dortmund.mpg.de