Heptares Therapeutics has teamed up with the University of Cambridge to discover molecules that modulate a cardiovascular target. The project builds on work at Cambridge to understand the role apelin receptors play in cardiovascular conditions including ischemic heart disease and discover a selective antagonist of the target.
Entering into the collaboration gives Heptares access to a group run by Dr. Anthony Davenport, a researcher at Cambridge with an interest in G-protein-coupled receptors (GPCRs)—Heptares’ specialty—and apelin peptides. These peptides are found in vascular and cardiac endothelial cells. And, research suggests, they play a role in multiple cardiac functions and conditions.
Apelin receptors are upregulated in atherosclerosis, and downregulated in dilated cardiomyopathy and ischemic heart disease. Research by Davenport’s group has also found apelins increase the heart’s ability to contract.
Buoyed by these findings, Davenport’s team connected with a group at the university’s chemistry department to work on modulating the target. The teams have discovered a selective antagonist of the apelin receptor. Teaming with Heptares is intended to further advance research into apelin.
“We have made great strides in recent years to increase our understanding of the role of the apelin receptor system and its involvement in cardiovascular diseases. It is an exciting target and we are delighted to be advancing this research with Heptares to better understand the role of apelin and related peptides with a view to informing the optimal way of targeting the apelin system for treating cardiovascular diseases,” Davenport said in a statement.
The collaboration is the second Heptares has started under ORBIT, a three-year, £5 million ($6 million) initiative to broaden use of its GPCR structure-based drug design capabilities. Heptares is also working with Imperial College London to research an orphan receptor linked to asthma, inflammatory bowel disease and other immune disorders. Both projects fit into Heptares’ work to identify new links between GPCRs and disease, and design molecules to hit the targets.
Heptares’ GPCR capabilities have helped it to land a $400 million buyout bid from Sosei and a string of pacts with biopharma companies, including Allergan, AstraZeneca and Pfizer.