Inhibitory effect of b-AP15 on the 20S proteasome

Biomolecules. 2014 Oct 14;4(4):931-9. doi: 10.3390/biom4040931.

Abstract

The 26S proteasome is a cellular proteolytic complex containing 19S regulatory particles and the 20S core proteasome. It was reported that the small molecule b-AP15 targets the proteasome by inhibiting deubiquitination of the 19S regulatory particles of the proteasome complex. An investigation of b-AP15 on the 20S proteasome core suggested that this compound can also inhibit the 20S proteasome with a potency equivalent to that found to inhibit the 19S regulatory particles.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Green Fluorescent Proteins / genetics
  • Green Fluorescent Proteins / metabolism
  • HeLa Cells / drug effects
  • Humans
  • Inhibitory Concentration 50
  • Piperidones / chemistry
  • Piperidones / pharmacology*
  • Protease Inhibitors / pharmacology*
  • Proteasome Endopeptidase Complex / metabolism*
  • Ubiquitin / genetics
  • Ubiquitin / metabolism

Substances

  • 3,5-bis((4-nitrophenyl)methylidene)-1-prop-2-enoylpiperidin-4-one
  • Piperidones
  • Protease Inhibitors
  • Ubiquitin
  • Green Fluorescent Proteins
  • Proteasome Endopeptidase Complex
  • 26S proteasome non-ATPase regulatory subunit 13