Development of Ubiquitin-Based Probe for Metalloprotease Deubiquitinases

Angew Chem Int Ed Engl. 2019 Oct 7;58(41):14477-14482. doi: 10.1002/anie.201906790. Epub 2019 Aug 28.

Abstract

Deubiquitinases (DUBs) are a family of enzymes that regulate the ubiquitin signaling cascade by removing ubiquitin from specific proteins in response to distinct signals. DUBs that belong to the metalloprotease family (metalloDUBs) contain Zn2+ in their active sites and are an integral part of distinct cellular protein complexes. Little is known about these enzymes because of the lack of specific probes. Described here is a Ub-based probe that contains a ubiquitin moiety modified at its C-terminus with a Zn2+ chelating group based on 8-mercaptoquinoline, and a modification at the N-terminus with either a fluorescent tag or a pull-down tag. The probe is validated using Rpn11, a metalloDUB found in the 26S proteasome complex. This probe binds to metalloDUBs and efficiently pulled down overexpressed metalloDUBs from a HeLa cell lysate. Such probes may be used to study the mechanism of metalloDUBs in detail and allow better understanding of their biochemical processes.

Keywords: biological activity; chelates; metalloenzymes; ubiquitin; zinc.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Chelating Agents / chemical synthesis*
  • Deubiquitinating Enzymes / chemistry
  • Deubiquitinating Enzymes / metabolism*
  • HeLa Cells
  • Humans
  • Models, Molecular
  • Protein Conformation
  • Ubiquitin / chemistry*
  • Ubiquitin / metabolism
  • Zinc / chemistry*

Substances

  • Chelating Agents
  • Ubiquitin
  • Deubiquitinating Enzymes
  • Zinc