Synthesis and evaluation of a bimodal CXCR4 antagonistic peptide

Bioconjug Chem. 2011 May 18;22(5):859-64. doi: 10.1021/bc2000947. Epub 2011 Apr 19.


The antagonistic Ac-TZ14011 peptide, which binds to the chemokine receptor 4, has been labeled with a multifunctional single attachment point reagent that contains a DTPA chelate and a fluorescent dye with Cy5.5 spectral properties. Flow cytometry and confocal microscopy showed that the bimodal labeled peptide gave a specific receptor binding that is similar to monofunctionalized peptide derivatives. Therefore, the newly developed bimodal peptide derivative can be used in multimodal imaging applications.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Chelating Agents / chemistry*
  • Flow Cytometry
  • Fluorescent Dyes / chemistry*
  • Humans
  • Mice
  • Microscopy, Confocal
  • Molecular Conformation
  • Pentetic Acid / chemistry*
  • Peptides / chemical synthesis
  • Peptides / chemistry
  • Peptides / pharmacology*
  • Receptors, CXCR4 / antagonists & inhibitors*


  • Chelating Agents
  • Fluorescent Dyes
  • Peptides
  • Receptors, CXCR4
  • Pentetic Acid