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, the NCGC completed primary screening of the PAC1 assay, and hit validation is currently underway. Selective hits and chemotypes are under evaluation in neurite growth assay with the aim of rank order series for initiating structure activity-relationship optimization studies. As a center, the NCGC has fostered and 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 NCGC 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.