Home | UVM Innovations / Available Technologies /

A First-in-Class Anti-Hypertensive Therapy | UVM Innovations | University of Vermont

A First-in-Class Anti-Hypertensive Therapy

UVM Reference Number: C454

Summary:

Synthetic peptides for the treatment of resistant hypertension and acute hypertensive crisis

Background:

Despite the number of available treatments, nearly one-third of the over 73 million patients with hypertension respond poorly to current treatment options. This presents a significant commercial opportunity for new therapies with novel mechanisms of action. The cGMP-dependent protein kinase (PKG) has long been identified as a master regulator of vasodilation and target for drug development, but previous attempts have failed to develop a cGMP-independent activator.

Technology Overview:

Researchers at the University of Vermont are developing a library of synthetic peptides (S-tides) that are first-in-class agonists of PKG1α with the potential to treat resistant hypertension and acute hypertensive crisis. S-tides are rationally designed peptides, which bind to and activate PKG1α with nanomolar efficacy, leading to 20-50% blood pressure reductions when administered to rats. S-tides may have immediate clinical utility as an IV-administered drug for acute hypertensive crisis or may serve as a platform for the development of orally available therapeutics for the treatment of resistant hypertension and other diseases that involve PKG biology.

Benefits:

First-in-class peptide therapeutic for hypertension.
cGMP independent activation of a master regulator of vasodilation.
Activates PKG with nanomolar efficacy.
S-tides provide a framework for ligand and structure-based virtual screening of small molecules.

Applications:

Chronic hypertension and acute hypertension crisis.
Treatment of other diseases that involve PKG, such as CHF, PAH, kidney disease, GI dysfunction and genitourinary disorders.