Research ArticleCardiovascular Biology

A peptide of the RGS domain of GRK2 binds and inhibits Gαq to suppress pathological cardiac hypertrophy and dysfunction

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Science Signaling  22 Mar 2016:
Vol. 9, Issue 420, pp. ra30
DOI: 10.1126/scisignal.aae0549

GRK2 against heart failure

Sustained high blood pressure causes the heart walls to thicken to deal with the increased load, a process called cardiac hypertrophy. If left unchecked, cardiac hypertrophy leads to heart failure. A particular part of the kinase and scaffolding protein GRK2 inhibits a G protein that promotes cardiac hypertrophy. Schumacher et al. generated mice that overexpressed a peptide of this inhibitory region of GRK2 in the heart. These mice developed less cardiac hypertrophy and retained greater cardiac function under conditions that cause heart failure. Thus, targeting this peptide to the heart could suppress hypertrophic signaling and prevent heart failure.