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  • 标题:Binding site elucidation and structure guided design of macrocyclic IL-17A antagonists
  • 本地全文:下载
  • 作者:Shenping Liu ; Leslie A. Dakin ; Li Xing
  • 期刊名称:Scientific Reports
  • 电子版ISSN:2045-2322
  • 出版年度:2016
  • 卷号:6
  • 期号:1
  • DOI:10.1038/srep30859
  • 语种:English
  • 出版社:Springer Nature
  • 摘要: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.
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