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Cardiovascular disease

Cardiovascular disease

Adenosine A1 receptor (ADORA1)

In vitro studies identified a biased ADORA1 agonist that could help treat cardiovascular diseases without common side effects. ADORA1 agonists have cardioprotective effects but can cause bradycardia as an on-target adverse effect. A biased ADORA1 ligand designed by linking adenosine-an orthosteric agonist-with a positive allosteric modulator of ADORA1 signaling had a potent agonist effect without also inducing bradycardia-associated signaling. In rat cardiomyoblasts expressing Adora1, the agonist conferred better protection from ischemia than either compound alone and did not decrease isolated rat atrial heart rate. Next steps include demonstrating efficacy across a broader range of cardiovascular models.
Bayer AG has the ADORA1 partial agonist BAY 1067197 in Phase I/II testing to treat heart failure.

SciBX 7(16); doi:10.1038/scibx.2014.459
Published online April 24, 2014

Findings unpatented; unavailable for licensing

Valant, C. et al. Proc. Natl. Acad. Sci. USA; published online March 11, 2014;
Contact: Arthur Christopoulos, Monash University, Parkville,
Victoria, Australia
Contact: Peter J. Scammells, same affiliation as above