PAC1 receptor antagonists as potential treatments for depression and atherosclerosis associated with chronic stress

National Center For Advancing Translational Sciences

Investigators

Abstract

During this period, hits identified in high-throughput screening were assessed for PAC1R antagonism using a cellular reporter of cAMP. Additional cell-based reporter assays are under development to improve detection of PAC1R antagonists and for initiating structure activity-relationship optimization studies. The Early Translation Branch (ETB) has maintained over 130 active collaborations with both NIH and extramural investigators, facilitating drug discovery efforts across the entire spectrum of human disease. These efforts have led to dozens of high-throughput screens and a number of medicinal chemistry campaigns to further improve on screening hits, providing our collaborators and the general research community with publications and a variety of promising small molecule probes and leads. In addition, the ETB has worked to advance a number of informatic initiatives to make better use of existing drug and disease target information and provide the general public with easily accessible resources, further catalyzing the development of new therapies for human disease.