Thiol-inducible direct fluorescence monitoring of drug release

Org Biomol Chem. 2013 Jan 28;11(4):580-5. doi: 10.1039/c2ob26680f. Epub 2012 Nov 27.

Abstract

A new bifunctional compound NCC, which undergoes thiol-mediated disulfide cleavage after cell entry, produces a red-shifted fluorescent emission in the cytosol and releases free active DNA alkylating agent CLB into the nucleus, and finally leads to DNA damage and cell death.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents, Alkylating / chemistry*
  • Antineoplastic Agents, Alkylating / pharmacology
  • Chlorambucil / chemistry
  • Chlorambucil / pharmacology
  • DNA / genetics
  • DNA / metabolism
  • DNA Damage
  • Disulfides / chemistry
  • Drug Carriers / chemistry*
  • Drug Design
  • HeLa Cells
  • Humans
  • Intracellular Space / drug effects
  • Intracellular Space / metabolism
  • Molecular Imaging
  • Optical Phenomena
  • Spectrometry, Fluorescence
  • Sulfhydryl Compounds / chemistry*

Substances

  • Antineoplastic Agents, Alkylating
  • Disulfides
  • Drug Carriers
  • Sulfhydryl Compounds
  • Chlorambucil
  • DNA