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Discovery and structure-activity relationships of small molecules that block the human immunoglobulin G-human neonatal Fc receptor (hIgG-hFcRn) protein-protein interaction.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2013 Mar 01; Vol. 23 (5), pp. 1253-6. Date of Electronic Publication: 2013 Jan 11. - Publication Year :
- 2013
-
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.<br /> (Copyright © 2013 Elsevier Ltd. All rights reserved.)
- Subjects :
- Drug Evaluation, Preclinical
Histocompatibility Antigens Class I immunology
Humans
Immunoglobulin G immunology
Ligands
Protein Interaction Domains and Motifs drug effects
Receptors, Fc immunology
Structure-Activity Relationship
Histocompatibility Antigens Class I metabolism
Immunoglobulin G metabolism
Quinoxalines pharmacology
Receptors, Fc antagonists & inhibitors
Receptors, Fc metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 23
- Issue :
- 5
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 23375228
- Full Text :
- https://doi.org/10.1016/j.bmcl.2013.01.014