Mechanism of activation and regulation of deubiquitinase activity in MINDY1 and MINDY2

Mol Cell. 2021 Oct 21;81(20):4176-4190.e6. doi: 10.1016/j.molcel.2021.08.024. Epub 2021 Sep 15.

Abstract

Of the eight distinct polyubiquitin (polyUb) linkages that can be assembled, the roles of K48-linked polyUb (K48-polyUb) are the most established, with K48-polyUb modified proteins being targeted for degradation. MINDY1 and MINDY2 are members of the MINDY family of deubiquitinases (DUBs) that have exquisite specificity for cleaving K48-polyUb, yet we have a poor understanding of their catalytic mechanism. Here, we analyze the crystal structures of MINDY1 and MINDY2 alone and in complex with monoUb, di-, and penta-K48-polyUb, identifying 5 distinct Ub binding sites in the catalytic domain that explain how these DUBs sense both Ub chain length and linkage type to cleave K48-polyUb chains. The activity of MINDY1/2 is inhibited by the Cys-loop, and we find that substrate interaction relieves autoinhibition to activate these DUBs. We also find that MINDY1/2 use a non-canonical catalytic triad composed of Cys-His-Thr. Our findings highlight multiple layers of regulation modulating DUB activity in MINDY1 and MINDY2.

Keywords: autoinhibition; conformational change; crystal structure; deubiquitinase; enzyme mechanism; polyubiquitin; protease; proteasome; protein degradation; ubiquitylation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Binding Sites
  • Catalytic Domain
  • Crystallography
  • Deubiquitinating Enzymes / genetics
  • Deubiquitinating Enzymes / metabolism*
  • Enzyme Activation
  • Humans
  • Kinetics
  • Models, Molecular
  • Mutation
  • Polyubiquitin / metabolism*
  • Protein Binding
  • Protein Conformation
  • Scattering, Small Angle
  • Structure-Activity Relationship
  • Ubiquitin Thiolesterase / genetics
  • Ubiquitin Thiolesterase / metabolism*
  • Ubiquitination

Substances

  • Polyubiquitin
  • Deubiquitinating Enzymes
  • MINDY1 protein, human
  • MINDY2 protein, human
  • Ubiquitin Thiolesterase