Introducing Lasso Peptides as Molecular Scaffolds for Drug Design: Engineering of an Integrin Antagonist

Abstract

Eine Schlinge für Integrine: Lassopeptide sind eine Klasse stabiler bakterieller Peptide, deren einzigartige Merkmale sie vielversprechend für das Wirkstoff-Design machen. Die Übertragung des Epitops des Integrin bindenden Motivs RGD auf die Lassostruktur von Microcin J25 überführt das verknotete Peptid in einen nanomolaren Integrin-Antagonisten (siehe Bild). Künstliche Lassopeptide können also zur Präsentation von Pharmakophoren verwendet werden. Detailed facts of importance to specialist readers are published as ”Supporting Information”. Such documents are peer-reviewed, but not copy-edited or typeset. They are made available as submitted by the authors. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.