Iso-ADP-Ribose Fluorescence Polarization Probe for the Screening of RNF146 WWE Domain Inhibitors

ACS Chem Biol. 2024 Feb 16;19(2):300-307. doi: 10.1021/acschembio.3c00512. Epub 2024 Jan 18.

Abstract

Poly-ADP-ribosylation is an important protein post-translational modification with diverse biological consequences. After binding poly-ADP-ribose on axis inhibition protein 1 (AXIN1) through its WWE domain, RING finger protein 146 (RNF146) can ubiquitinate AXIN1 and promote its proteasomal degradation and thus the oncogenic WNT signaling. Therefore, inhibiting the RNF146 WWE domain is a potential antitumor strategy. However, due to a lack of suitable screening methods, no inhibitors for this domain have been reported. Here, we developed a fluorescence polarization (FP)-based competition assay for the screening of RNF146 WWE inhibitors. This assay relies on a fluorescently tagged iso-ADP-ribose tracer compound, TAMRA-isoADPr. We report the design and synthesis of this tracer compound and show that it is a high-affinity tracer for the RNF146 WWE domain. This provides a convenient assay and will facilitate the development of small-molecule inhibitors for the RNF146 WWE domain.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Adenosine Diphosphate Ribose* / metabolism
  • Poly Adenosine Diphosphate Ribose* / chemistry
  • Poly Adenosine Diphosphate Ribose* / metabolism
  • Protein Processing, Post-Translational
  • Wnt Signaling Pathway

Substances

  • Adenosine Diphosphate Ribose
  • Poly Adenosine Diphosphate Ribose