Decoding anaphylatoxins: unveiling the molecular mechanisms of complement receptor activation and signaling

Trends Biochem Sci. 2024 Apr;49(4):280-282. doi: 10.1016/j.tibs.2024.01.001. Epub 2024 Jan 16.

Abstract

Recent advances in cryo-electron microscopy (Cryo-EM) have revolutionized our understanding of the complement C5a/C3a receptors that are crucial in inflammation. A recent report by Yadav et al. has elucidated the activation, ligand binding, selectivity, and signaling bias of these receptors, thereby enhancing structure-guided drug discovery. This paves the way for more effective anti-inflammatory therapies that target these receptors with unprecedented precision.

Keywords: GPCR receptors C5aR1 and C3aR; agonist binding; anaphylatoxins C5a and C3a; receptor activation; selectivity; signaling bias.

MeSH terms

  • Anaphylatoxins* / chemistry
  • Anaphylatoxins* / metabolism
  • Complement C3a / metabolism
  • Complement C5a* / metabolism
  • Cryoelectron Microscopy
  • Receptors, Complement / metabolism

Substances

  • Anaphylatoxins
  • Complement C5a
  • Complement C3a
  • Receptors, Complement