Small Peptides Able to Suppress Prostaglandin E₂ Generation in Renal Mesangial Cells

Molecules. 2018 Jan 13;23(1):158. doi: 10.3390/molecules23010158.

Abstract

Peptide drug discovery may play a key role in the identification of novel medicinal agents. Here, we present the development of novel small peptides able to suppress the production of PGE₂ in mesangial cells. The new compounds were generated by structural alterations applied on GK115, a novel inhibitor of secreted phospholipase A₂, which has been previously shown to reduce PGE₂ synthesis in rat renal mesangial cells. Among the synthesized compounds, the tripeptide derivative 11 exhibited a nice dose-dependent suppression of PGE₂ production, similar to that observed for GK115.

Keywords: inhibitors; mesangial cells; peptides; prostaglandin E2; secreted phospholipase A2.

MeSH terms

  • Animals
  • Binding Sites
  • Catalytic Domain
  • Cells, Cultured
  • Dinoprostone / biosynthesis*
  • Mesangial Cells / drug effects*
  • Mesangial Cells / metabolism*
  • Models, Molecular
  • Molecular Conformation
  • Peptides / chemical synthesis
  • Peptides / chemistry
  • Peptides / pharmacology*
  • Phospholipases A2 / chemistry
  • Phospholipases A2 / metabolism
  • Protein Binding
  • Rats

Substances

  • Peptides
  • Phospholipases A2
  • Dinoprostone