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Discovery of highly potent and selective small-molecule reversible Factor D inhibitors demonstrating alternative complement pathway inhibition in vivo

Lorthiois, Edwige and Anderson, Karen and Vulpetti, Anna and Rogel, Olivier and Cumin, Frederic and Ostermann, Nils and Mac Sweeney, Aengus and Delgado, Omar and Liao, Sha-Mei and Randl, Stefan and Ruedisser, Simon and De Erkenez, Andrea and Yang, Louis and Hartwieg, Constanze and Argikar, Upendra and Newton, Ronald and Kansara, Viralbhai and Flohr, Stefanie and Hommel, Ulrich and 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

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