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Development of Potent and Selective Agonists for Complement C5a Receptor 1 with In Vivo Activity.

Declan M Gorman1, Xaria X Li1, John D Lee1

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Journal of Medicinal Chemistry
|November 11, 2021
PubMed
Summary

Researchers developed selective C5aR1 agonists, BM213 and BM221, to study immune responses. These novel peptides offer high selectivity for C5aR1, enabling precise investigation of its role in disorders and potential therapeutic applications.

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Area of Science:

  • Immunology
  • Pharmacology
  • Biochemistry

Background:

  • The anaphylatoxin C5a, a complement peptide, is implicated in immune-related disorders.
  • C5a interacts with G protein-coupled receptors (GPCRs) C5aR1 and C5aR2 with equal potency.
  • Existing C5a peptide agonists lack selectivity for C5aR1, limiting research into its specific functions.

Purpose of the Study:

  • To develop novel, potent, and selective peptide agonists for C5a receptor 1 (C5aR1).
  • To create research tools that enable precise interrogation of C5aR1 function distinct from C5aR2.
  • To evaluate the signaling profiles and in vivo efficacy of newly developed C5aR1 agonists.

Main Methods:

  • Design and synthesis of novel peptide agonists targeting C5aR1.
  • Assessment of receptor binding affinity and selectivity (C5aR1 vs. C5aR2, C3aR).
  • Functional assays including calcium mobilization, pERK1/2 and beta-arrestin signaling, cytokine release, and in vivo neutrophil mobilization.
  • Evaluation of antitumor activity in a murine mammary carcinoma model.

Main Results:

  • Developed potent and stable peptide C5aR1 agonists with >1000-fold selectivity for C5aR1 over C3aR and no C5aR2 activity.
  • BM213 demonstrated C5aR1-mediated calcium mobilization and pERK1/2 signaling, but not beta-arrestin recruitment.
  • BM221 showed no signaling bias, while both ligands mimicked C5a function in cytokine release and neutrophil mobilization assays.
  • BM213 exhibited antitumor activity in a preclinical mouse model.

Conclusions:

  • Novel C5aR1-selective peptide agonists (BM213, BM221) have been successfully developed.
  • These agonists provide valuable tools for dissecting C5aR1-specific signaling pathways and biological roles.
  • The findings suggest potential therapeutic applications for C5aR1 modulation in immune disorders and cancer.