Structural basis for RING-Cys-Relay E3 ligase activity and its role in axon integrity

Nat Chem Biol. 2020 Nov;16(11):1227-1236. doi: 10.1038/s41589-020-0598-6. Epub 2020 Aug 3.

Abstract

MYCBP2 is a ubiquitin (Ub) E3 ligase (E3) that is essential for neurodevelopment and regulates axon maintenance. MYCBP2 transfers Ub to nonlysine substrates via a newly discovered RING-Cys-Relay (RCR) mechanism, where Ub is relayed from an upstream cysteine to a downstream substrate esterification site. The molecular bases for E2-E3 Ub transfer and Ub relay are unknown. Whether these activities are linked to the neural phenotypes is also unclear. We describe the crystal structure of a covalently trapped E2~Ub:MYCBP2 transfer intermediate revealing key structural rearrangements upon E2-E3 Ub transfer and Ub relay. Our data suggest that transfer to the dynamic upstream cysteine, whilst mitigating lysine activity, requires a closed-like E2~Ub conjugate with tempered reactivity, and Ub relay is facilitated by a helix-coil transition. Furthermore, neurodevelopmental defects and delayed injury-induced degeneration in RCR-defective knock-in mice suggest its requirement, and that of substrate esterification activity, for normal neural development and programmed axon degeneration.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adaptor Proteins, Signal Transducing / metabolism
  • Animals
  • Axons / metabolism*
  • Binding Sites
  • Cysteine / metabolism*
  • Female
  • Gene Knock-In Techniques
  • Humans
  • Lysine / metabolism
  • Mice
  • Mice, Inbred C57BL / embryology
  • Mice, Transgenic
  • Models, Molecular
  • Molecular Conformation
  • Protein Binding
  • Protein Conformation
  • RING Finger Domains*
  • Signal Transduction
  • Structure-Activity Relationship
  • Ubiquitin / metabolism*
  • Ubiquitin-Conjugating Enzymes / metabolism*
  • Ubiquitin-Protein Ligases / metabolism*
  • Ubiquitination

Substances

  • Adaptor Proteins, Signal Transducing
  • Ubiquitin
  • Ubiquitin-Conjugating Enzymes
  • MYCBP2 protein, human
  • Ubiquitin-Protein Ligases
  • Lysine
  • Cysteine