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Published on: May 12, 2023
Therapeutic potential of functional selectivity in the treatment of heart failure
Gitte Lund Christensen1, Mark Aplin, Jakob Lerche Hansen
1Department of Clinical Biochemistry, Glostrup Research Institute, Glostrup Hospital, DK-2600 Glostrup, Denmark.
Abstract:
Adrenergic and angiotensin receptors are prominent targets in pharmacological alleviation of cardiac remodeling and heart failure, but their use is associated with cardiodepressant side effects. Recent advances in our understanding of seven transmembrane receptor signaling show that it is possible to design ligands with "functional selectivity," acting as agonists on certain signaling pathways while antagonizing others. This represents a major pharmaceutical opportunity to separate desired from adverse effects governed by the same receptor. Accordingly, functionally selective ligands are currently pursued as next-generation drugs for superior treatment of heart failure.
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