Lorthiois, Edwige, Anderson, Karen, Vulpetti, Anna, Rogel, Olivier, Cumin, Frederic, Ostermann, Nils, Mac Sweeney, Aengus, Delgado, Omar, Liao, Sha-Mei, Randl, Stefan, Ruedisser, Simon, De Erkenez, Andrea, Yang, Louis, Hartwieg, Constanze, Argikar, Upendra, Newton, Ronald, Kansara, Viralbhai, Flohr, Stefanie, Hommel, Ulrich, Jaffee, Bruce and Maibaum, Juergen Klaus (2017) Discovery of highly potent and selective small-molecule reversible Factor D inhibitors demonstrating alternative complement pathway inhibition in vivo. Journal of medicinal chemistry.

Abstract

The combination of structure-based drug design and lead optimization has led to the discovery of non-covalent reversible and selective human Factor D inhibitors. Compound 27 was shown to block complement alternative pathway activation in vitro and demonstrated in vivo efficacy in animal models after oral administration.

Item Type:	Article
Keywords:	Alternative Complement Pathway, Factor D inhibitors, S1 serine protease, structure-based drug design, MAC deposition, age-related macular degeneration.
Date Deposited:	18 Jul 2017 00:45
Last Modified:	18 Jul 2017 00:45
URI:	https://oak.novartis.com/id/eprint/32174