2. Academic Validation
  3. Discovery and structure-activity relationships of small molecules that block the human immunoglobulin G-human neonatal Fc receptor (hIgG-hFcRn) protein-protein interaction

Discovery and structure-activity relationships of small molecules that block the human immunoglobulin G-human neonatal Fc receptor (hIgG-hFcRn) protein-protein interaction

  • Bioorg Med Chem Lett. 2013 Mar 1;23(5):1253-6. doi: 10.1016/j.bmcl.2013.01.014.
Zhaolin Wang 1,  Cara Fraley,  Adam R Mezo
Affiliations

Affiliation

  • 1 Biogen Idec Hemophilia, 9 Fourth Avenue, Waltham, MA 02451, USA.
PMID: 23375228 DOI: 10.1016/j.bmcl.2013.01.014
Abstract

The neonatal Fc receptor, FcRn, prolongs the half-life of IgG in the serum and represents a potential therapeutic target for the treatment of autoimmune disease. Small molecules that block the protein-protein interactions of human IgG-human FcRn may lower pathogenic autoantibodies and provide effective treatment. A novel class of quinoxalines has been discovered as antagonists of the IgG:FcRn protein-protein interaction through optimization of a hit derived from a virtual ligand-based screen.

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