Development of Highly Potent Inhibitors of the Ras‐Targeting Human Acyl Protein Thioesterases Based on Substrate Similarity Design

Abstract

Ein gemeinsames Erkennungsmotiv aus einer negativ geladenen Gruppe (rot) sechs bis sieben Bindungen entfernt von der (Thio)esterfunktion (grün) und einer positiv geladenen Schwanzgruppe (blau) zehn bis zwölf Bindungen entfernt wurde in zwei nativen Substraten der Acyl-Protein-Thioesterase 1 (APT1) identifiziert (siehe Bild). Diese Ähnlichkeit führte zum Design potenter Inhibitoren des Ras-depalmitoylierenden Enzyms APT1. 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.