During this period, the collaborative team has worked to characterize the lead molecules for this project in in vivo proof-of-concept models, and in vivo testing is underway. 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.
| Agoulnik, Alexander I; Agoulnik, Irina U; Hu, Xin et al. (2017) Synthetic non-peptide low molecular weight agonists of the relaxin receptor 1. Br J Pharmacol 174:977-989 |
| Kaftanovskaya, Elena M; Soula, Mariluz; Myhr, Courtney et al. (2017) Human Relaxin Receptor Is Fully Functional in Humanized Mice and Is Activated by Small Molecule Agonist ML290. J Endocr Soc 1:712-725 |
| Kocan, Martina; Sarwar, Mohsin; Ang, Sheng Y et al. (2017) ML290 is a biased allosteric agonist at the relaxin receptor RXFP1. Sci Rep 7:2968 |
| Hu, Xin; Myhr, Courtney; Huang, Zaohua et al. (2016) Structural Insights into the Activation of Human Relaxin Family Peptide Receptor 1 by Small-Molecule Agonists. Biochemistry 55:1772-83 |
