Inhibiting the Protein Ubiquitination Cascade by Ubiquitin-Mimicking Short Peptides

• Published in: Organic letters Vol. 14; no. 22; pp. 5760 - 5763
• Main Authors: Zhao, Bo, Choi, Chan Hee J, Bhuripanyo, Karan, Villhauer, Eric B, Zhang, Keya, Schindelin, Hermann, Yin, Jun
• Format: Journal Article
• Language: English
• Published: United States American Chemical Society 16.11.2012
• Subjects: Molecular Structure; Peptides - metabolism; Ubiquitin - metabolism; Ubiquitin-Conjugating Enzymes - metabolism; Ubiquitination - drug effects

Short heptapeptides were identified to function as ubiquitin (UB) mimics that are activated by E1 and form thioester conjugates with E1, E2, and HECT type E3 enzymes. The activities (k cat/K 1/2) of E1 with the UB-mimicking peptides are 130–1,400-fold higher than the equally long peptide with the na...