GRK5: Big-hearted Target

A team of U.S. and U.K. researchers has uncovered a new role for G protein-coupled receptor kinase 5 in pathological cardiac hypertrophy, providing a first mechanistic target for this indication.1 It behaves more like an histone deacetylase kinase than a G protein-coupled receptor kinase, activating histone deacetylase 5 and triggering a signaling cascade that results in cardiac hypertrophy.

The finding, reported in the Proceedings of the National Academy of Sciences, may make it possible to treat hypertrophy with kinase inhibitors. In contrast to current therapeutic strategies that address more general conditions such as hypertension or ischemia, which can lead to cardiac hypertrophy, this research provides the potential to treat the condition directly at its mechanistic root.

However, the effectiveness of such a therapeutic strategy will depend on whether the function of G protein-coupled receptor kinase 5 (GRK5) is unique in hypertrophy or is redundant with other histone deacetylase kinases (HDAC kinases).

The team of scientists from Thomas Jefferson University and University College London was led by Walter Koch, VP of research in medicine, professor of medicine and director of the Center for Translational

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