New scaffolds for tripeptidomimetics - Toward CXCR4 antagonists inspired by marine peptides

Wednesday March 8
scientific Workshop: Marine bioprospecting - Production of health promoting compounds and novel approaches in biodiscovery
10:30

New scaffolds for tripeptidomimetics - Toward CXCR4 antagonists inspired by marine peptides

Bengt Erik Haug, Professor
University of Bergen, Norway

The CXC chemokine receptor 4 (CXCR4) is a peptidergic 7TM receptor that is implicated in a number of pathological conditions, including HIV, cancer, and rheumatoid arthritis. Consequently, CXCR4 has emerged as an attractive drug target. A number of antagonists of CXCR4 have been described in the literature, including highly potent synthetic derivatives of the polyphemusins, which have been isolated from American horseshoe crabs (Limulus polyphemus).

The lecture will give an overview of the down-sizing of the initial polypeptide hits to smaller peptides through the efforts of several research groups and will focus on our recent work toward the preparation of tripeptidomimetic CXCR4 antagonists based on bicyclic scaffolds.