Design and synthesis of efficient fluororethylene-peptidomimetic inhibitors of dipeptidyl peptidase III (DPP3)

Harald Podversnik, Shalinee Jha, Peter Macheroux, Rolf Breinbauer*

*Korrespondierende/r Autor/-in für diese Arbeit

Publikation: Beitrag in einer FachzeitschriftArtikelBegutachtung

Abstract

Dipeptidyl peptidase III (DPP3) is a ubiquitously expressed zinc-dependent peptide cutting enzyme and selectively hydrolyses amide bonds to cleave N-terminal dipeptide fragments off of physiologically important oligopeptides. DPP3 has been found in a multitude of different types of cells and appears to be involved in various physiological processes (e.g. nociception, blood pressure control, protein turnover). Using the slowly converted peptide substrate tynorphin (VVYPW) as starting point, we have replaced the scissile bond with a fluoroethylene bioisostere to design ground state inhibitors, which led to the so far most effective peptide-based inhibitor of DPP3.

Originalspracheenglisch
Aufsatznummer116831
FachzeitschriftBioorganic and Medicinal Chemistry
Jahrgang67
DOIs
PublikationsstatusVeröffentlicht - 1 Aug 2022

ASJC Scopus subject areas

  • Biochemie
  • Molekularmedizin
  • Molekularbiologie
  • Pharmazeutische Wissenschaften
  • Wirkstoffforschung
  • Klinische Biochemie
  • Organische Chemie

Fields of Expertise

  • Human- & Biotechnology

Kooperationen

  • BioTechMed-Graz

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