Dual-function CXCR4 Antagonist Polyplexes to Deliver Gene Therapy and Inhibit Cancer Cell Invasion

Angew Chem Int Ed Engl. 2012 Aug 27;51(35):8740-3. doi: 10.1002/anie.201203463. Epub 2012 Jul 31.

Abstract

A bicyclam-based biodegradable polycation with CXCR4 antagonistic activity was developed with potential for combined drug/gene cancer therapies. The dual-function polycation prevents cancer cell invasion by inhibiting CXCL12 stimulated CXCR4 activation, while at the same time efficiently and safely delivers plasmid DNA into cancer cells.

Publication types

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

MeSH terms

  • Cell Line, Tumor
  • Cell Movement / drug effects
  • Cell Survival / drug effects
  • Chemokine CXCL12 / agonists
  • Chemokine CXCL12 / metabolism
  • Gene Transfer Techniques
  • Hep G2 Cells
  • Heterocyclic Compounds / chemical synthesis
  • Heterocyclic Compounds / chemistry*
  • Heterocyclic Compounds / toxicity
  • Humans
  • RNA Interference
  • RNA, Small Interfering / chemistry
  • RNA, Small Interfering / metabolism
  • Receptors, CXCR4 / antagonists & inhibitors*
  • Receptors, CXCR4 / genetics
  • Receptors, CXCR4 / metabolism

Substances

  • Chemokine CXCL12
  • Heterocyclic Compounds
  • RNA, Small Interfering
  • Receptors, CXCR4
  • plerixafor octahydrochloride