Recognition of substrate degrons by E3 ubiquitin ligases and modulation by small-molecule mimicry strategies

• Published in: Current opinion in structural biology Vol. 44; pp. 101 - 110
• Main Authors: Lucas, Xavier, Ciulli, Alessio
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 01.06.2017
• Subjects: Amino Acid Sequence; Animals; Humans; Protein Binding - drug effects; Proteolysis - drug effects; Small Molecule Libraries - pharmacology; Ubiquitin-Protein Ligases - chemistry; Ubiquitin-Protein Ligases - metabolism

[Display omitted] •E3 ligases recruit substrates for proteasomal degradation by recognition of degrons.•Crystal structures reveal the structural basis and mechanism of degron recognition.•Small-molecule degron mimetics can prevent or re-direct substrate recognition.•Small-molecule inducible degrons...