Design and Synthesis of Novel Ultralong-Acting Peptides as EDP-EBP Interaction Inhibitors for Pulmonary Fibrosis Treatment

J Med Chem. 2024 Apr 25;67(8):6624-6637. doi: 10.1021/acs.jmedchem.4c00067. Epub 2024 Apr 8.

Abstract

The increased remodeling of the extracellular matrix (ECM) in pulmonary fibrosis (PF) generates bioactive ECM fragments called matricryptins, which include elastin-derived peptides (EDPs). The interaction between EDPs and their receptors, including elastin-binding protein (EBP), plays a crucial role in exacerbating fibrosis. Here, we present LXJ-02 for the first time, a novel ultralong-acting inhibitor that disrupts the EDPs/EBP peptide-protein interaction, promoting macrophages to secrete matrix metalloproteinase-12 (MMP-12), and showing great promise as a stable peptide. MMP-12 has traditionally been implicated in promoting inflammation and fibrosis in various acute and chronic diseases. However, we reveal a novel role of LXJ-02 that activates the macrophage-MMP-12 axis to increase MMP-12 expression and degrade ECM components like elastin. This leads to the preventing of PF while also improving EDP-EBP interaction. LXJ-02 effectively reverses PF in mouse models with minimal side effects, holding great promise as an excellent therapeutic agent for lung fibrosis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Drug Design*
  • Elastin* / chemistry
  • Elastin* / metabolism
  • Humans
  • Macrophages / drug effects
  • Macrophages / metabolism
  • Male
  • Matrix Metalloproteinase 12 / metabolism
  • Mice
  • Mice, Inbred C57BL
  • Peptides / chemical synthesis
  • Peptides / chemistry
  • Peptides / pharmacology
  • Pulmonary Fibrosis* / drug therapy
  • Pulmonary Fibrosis* / metabolism
  • Pulmonary Fibrosis* / pathology
  • Receptors, Cell Surface*

Substances

  • Elastin
  • elastin-binding proteins
  • Matrix Metalloproteinase 12
  • Peptides
  • Receptors, Cell Surface