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

  • Molecules. 2018 Jan 13;23(1):158. doi: 10.3390/molecules23010158.
Sofia Vasilakaki  1 ,  Oleksandr Pastukhov  2 ,  Thomas Mavromoustakos  3 ,  Andrea Huwiler  4 ,  George Kokotos  5
Affiliations
  • 1. Laboratory of Organic Chemistry, Department of Chemistry, National and Kapodistrian University of Athens, Panepistimiopolis, Athens 15771, Greece. [email protected].
  • 2. Institute of Pharmacology, University of Bern, Bern 3010, Switzerland. [email protected].
  • 3. Laboratory of Organic Chemistry, Department of Chemistry, National and Kapodistrian University of Athens, Panepistimiopolis, Athens 15771, Greece. [email protected].
  • 4. Institute of Pharmacology, University of Bern, Bern 3010, Switzerland. [email protected].
  • 5. Laboratory of Organic Chemistry, Department of Chemistry, National and Kapodistrian University of Athens, Panepistimiopolis, Athens 15771, Greece. [email protected].
PMID: 29342835 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.
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