Peptide drugs are on the rise, accounting for 8% of FDA drug approvals over the past five years. The advantages of peptide-based drugs like biocompatibility and – availability, easy uptake (pharmacokinetics) and generally low toxicology make them unique targets for pharmaceutical development. Challenges that need to be carefully addressed to advance these drugs from lead compounds to successful trial candidates include drug delivery, metabolic stability and solubility. This talk gives a brief introduction in the pros and cons of peptide drugs, as well as recent trends and areas of research that improve the drug-like properties of these biomolecules. These concepts are demonstrated on Apelin and Elabela peptides, two endogenous peptide hormones that bind to the APJ receptor. One of the major pitfalls for their past failure as therapeutics is their short half-life in circulation. We show that chemical modification significantly increases their metabolic stability and regulatory bias, suggesting these analogs as powerful therapeutic candidates for the treatment of cardiovascular disease.

Engineered elabela peptides – designing nature-inspired therapeutics for cardiovascular disease

ACS Spring 2022

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.