Binding site elucidation and structure guided design of macrocyclic IL-17A antagonists
Abstract
Interleukin-17A (IL-17A) is a principal driver of multiple inflammatory and immune disorders. Antibodies that neutralize IL-17A or its receptor (IL-17RA) deliver efficacy in autoimmune diseases, but no small-molecule IL-17A antagonists have yet progressed into clinical trials. Investigation of a series of linear peptide ligands to IL-17A and characterization of their binding site has enabled the design of novel macrocyclic ligands that are themselves potent IL-17A antagonists.
- Publication:
-
Scientific Reports
- Pub Date:
- August 2016
- DOI:
- 10.1038/srep30859
- Bibcode:
- 2016NatSR...630859L