Artificial macrocycles as IL-17A/IL-17RA antagonists

Wenjia Wang, Matthew R. Groves, Alexander Domling*

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

9 Citations (Scopus)

Abstract

Interleukin 17(A) is a pro-inflammatory cytokine involved in several auto-immune and inflammatory diseases. Current antagonists against IL-17(A) or its receptor (IL-17RA) that show efficacy in clinical trials are monoclonal antibodies (mAbs). However, recently designed artificial macrocycles are potent IL-17A/IL-17RA antagonists. Based on co-crystal structures, a better understanding of the biological activity and SAR of the macrocycles has been gained, demonstrating that they can compete with mAbs for difficult targets such as PPIs.

Original languageEnglish
Pages (from-to)22-26
Number of pages5
JournalMedChemCommun
Volume9
Issue number1
DOIs
Publication statusPublished - Jan-2018

Keywords

  • DRUG DISCOVERY
  • BINDING-SITE
  • T-CELLS
  • INTERLEUKIN-17
  • RECEPTOR
  • INFLAMMATION
  • IL-17A
  • COMBINATION
  • AUTOIMMUNE
  • CYTOKINES

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