Indication

Target/marker/pathway

Summary

Licensing status

Publication and contact information

Cardiovascular disease

Cardiomyopathy; heart failure

MAP kinase 1 (MAPK1; ERK-2)

Rodent studies suggest inhibiting ERK-2 phosphorylation at threonine 188 could help prevent pathological cardiac hypertrophy. In rat cardiomyocytes, overexpression of a dominant-negative mutant ERK-2 that blocks ERK phosphorylation at threonine 188 decreased drug-induced hypertrophy compared with overexpression of wild-type ERK-2 and did not trigger apoptosis. In mice subjected to transverse aortic constriction, the dominant-negative ERK-2 prevented pathological cardiac hypertrophy and remodeling without causing adverse effects on cardiac function and cardiomyocyte survival. Next steps include developing strategies to specifically inhibit ERK phosphorylation at threonine 188.
Phenylephrine is a generic over-the-counter decongestant.

SciBX 6(16); doi:10.1038/scibx.2013.389
Published online April 25, 2013

Patent pending; available for licensing

Ruppert, C. et al. Proc. Natl. Acad. Sci. USA; published online April 15, 2013;
doi:10.1073/pnas.1221999110
Contact: Kristina Lorenz, University of Wuerzburg, Wuerzburg, Germany
e-mail:
lorenz@toxi.uni-wuerzburg.de

Contact: Martin J. Lohse, same affiliation as above
e-mail:
lohse@toxi.uni-wuerzburg.de