Bivalent ligands of CXCR4 with rigid linkers for elucidation of the dimerization state in cells

J Am Chem Soc. 2010 Nov 17;132(45):15899-901. doi: 10.1021/ja107447w. Epub 2010 Oct 25.

Abstract

To date, challenges in the design of bivalent ligands for G protein-coupled receptors (GPCRs) have revealed difficulties stemming from lack of knowledge of the state of oligomerization of the GPCR. The synthetic bivalent ligands with rigid linkers that are presented here can predict the dimer form of CXCR4 and be applied to molecular probes in cancerous cells. This "molecular ruler" approach would be useful in elucidating the details of CXCR4 oligomer formation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Binding, Competitive
  • HeLa Cells
  • Humans
  • Jurkat Cells
  • Ligands
  • Protein Multimerization*
  • Receptors, CXCR4 / antagonists & inhibitors
  • Receptors, CXCR4 / chemistry*

Substances

  • Ligands
  • Receptors, CXCR4