Deubiquitinases as potential anti-cancer targets for gold(III) complexes

Chem Commun (Camb). 2013 Jun 7;49(45):5153-5. doi: 10.1039/c3cc41766b.

Abstract

A panel of [Au(III)(C^N)(R2NCS2)](+) (HC^N = 2-phenylpyridine) complexes displayed significant deubiquitinases (DUBs) inhibitory activity; one of these complexes showed selective in vitro cytotoxicity towards breast cancer cells correlated to high cellular uptake of gold, and induced cell-cycle arrest, apoptosis, and anti-angiogenic property that could be related to DUB inhibitory activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology*
  • Breast Neoplasms / drug therapy
  • Breast Neoplasms / enzymology
  • Cell Line, Tumor
  • Cysteine Endopeptidases / chemistry
  • Cysteine Endopeptidases / metabolism
  • Female
  • HeLa Cells
  • Humans
  • Molecular Sequence Data
  • Molecular Targeted Therapy
  • Neoplasms / drug therapy*
  • Neoplasms / enzymology*
  • Organogold Compounds / chemistry*
  • Organogold Compounds / pharmacology*
  • Pyridines / chemistry
  • Pyridines / pharmacology
  • Ubiquitin Thiolesterase / antagonists & inhibitors
  • Ubiquitin Thiolesterase / chemistry
  • Ubiquitin Thiolesterase / metabolism

Substances

  • Antineoplastic Agents
  • Organogold Compounds
  • Pyridines
  • UCHL1 protein, human
  • 2-phenylpyridine
  • UCHL3 protein, human
  • UCHL5 protein, human
  • Ubiquitin Thiolesterase
  • Cysteine Endopeptidases