The formyl peptide receptors FPR1 and FPR2 as targets for inflammatory disorders: recent advances in the development of small-molecule agonists

Xiangyan Yi, Eric Tran, Jephthah O. Odiba, Cheng Xue Qin, Rebecca H. Ritchie, Jonathan B. Baell

Research output: Contribution to journalReview ArticleResearchpeer-review

8 Citations (Scopus)

Abstract

Formyl peptide receptors (FPRs) comprise a class of chemoattractant pattern recognition receptors, for which several physiological functions like host-defences, as well as the regulation of inflammatory responses, have been ascribed. With accumulating evidence that agonism of FPR1/FPR2 can confer pro-resolution of inflammation, increased attention from academia and industry has led to the discovery of new and interesting small-molecule FPR1/FPR2 agonists. Focused attention on the development of appropriate physicochemical and pharmacokinetic profiles is yielding synthesis of new compounds with promising in vivo readouts. This review presents an overview of small-molecule FPR1/FPR2 agonist medicinal chemistry developed over the past 20 years, with a particular emphasis on interrogation in the increasingly sophisticated bioassays which have been developed.

Original languageEnglish
Article number115989
Number of pages30
JournalEuropean Journal of Medicinal Chemistry
Volume265
DOIs
Publication statusPublished - 5 Feb 2024

Keywords

  • Biased profiles
  • FPRs
  • Inflammatory disorders
  • Small-molecule agonists
  • Structure-activity relationships

Cite this