Indomethacin-guided cancer selective prodrug conjugate activated by histone deacetylase and tumour-associated protease

Chem Commun (Camb). 2016 Aug 2;52(64):9965-8. doi: 10.1039/c6cc04255d.

Abstract

An indomethacin-guided drug delivery conjugate (IGDDC) has been designed by utilizing cancer associated elevated HDAC and CTSL activities as consecutive demasking ventures for drug activation. IGDDC exhibited preferential uptake by COX-2 positive cells both in vitro and ex vivo highlighting indomethacin's role in designing new cancer-specific drug delivery frameworks.

MeSH terms

  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / chemistry*
  • Cell Survival / drug effects
  • Cell Survival / physiology
  • Cyclooxygenase Inhibitors / administration & dosage
  • Cyclooxygenase Inhibitors / chemistry
  • Dose-Response Relationship, Drug
  • Drug Delivery Systems / methods*
  • HCT116 Cells
  • HeLa Cells
  • Hep G2 Cells
  • Histone Deacetylases* / administration & dosage
  • Humans
  • Indomethacin / administration & dosage
  • Indomethacin / chemistry*
  • Peptide Hydrolases* / administration & dosage
  • Prodrugs / administration & dosage
  • Prodrugs / chemistry*

Substances

  • Antineoplastic Agents
  • Cyclooxygenase Inhibitors
  • Prodrugs
  • Peptide Hydrolases
  • Histone Deacetylases
  • Indomethacin