News & Events

When

Date - September 10, 2021
1:00 pm - 2:00 pm

What

Senior Director
Center for Drug Discovery
RTI International
Talk Title: Development of Small Molecule APJ Agonists for the Treatment of Heart Failure

Abstract:

The apelin (APJ) receptor has emerged as a novel target for a number of important diseases but most specifically cardiovascular disease resulting from myocardial infarction and increased fibrosis . APJ is a class A GPCR that is activated by two distinct classes of peptides – apelin and ELABELA. These endogenous peptides are labile and not suitable for chronic dosing in patients suffering from cardiovascular disease. To date, small molecule ligands of the apelin receptor have been underreported. Our team has performed a comprehensive effort spanning assay development through screening, medicinal chemistry optimization,  and functional evaluation of the resulting series of APJ agonists in vivo.  This seminar will provide an overview of the academic drug discovery process from target identification through candidate selection for IND studies.