Peptide derivatized lamellar aggregates as target-specific MRI contrast agents

Chembiochem. 2007 May 25;8(8):950-5. doi: 10.1002/cbic.200700077.

Abstract

The relaxivity behaviour and the structural characterization of new supramolecular aggregates (bilayer structures and micelles) obtained by combining two different amphiphilic monomers are reported. One monomer, (C18)(2)DTPAGlu-Gd, contains a very stable gadolinium complex, and the other, DSPE-PEG(2000)-CCK8, contains the bioactive CCK8 peptide. Samples that contained only DSPE-PEG(2000)-CCK8, or up to 50 % (C18)(2)DTPAGlu-Gd, aggregated as double-layer structures (lamellar aggregates) with a thickness of approximately 80-100 A, as evaluated by SANS measurement and Cryo-TEM imaging. A transition to micelle formation was observed when the amount of (C18)(2)DTPAGlu-Gd in the aggregate was increased. These were rod-like micelles approximately 40 A in radius and >200 A in length. The proton relaxivities for both lamellar aggregates and rod-like micelles were the same (17.2 mM(-1) s(-1)), although the values were the results of different combinations of local and global contributions. The in vitro target selectivity of aggregates that contained the CCK-8 peptide was demonstrated by using nuclear medicine techniques.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cholecystokinin / chemistry
  • Contrast Media / chemistry*
  • Gadolinium / chemistry*
  • Macromolecular Substances / chemistry
  • Magnetic Resonance Imaging / methods*
  • Micelles*
  • Molecular Structure
  • Organometallic Compounds / chemistry*
  • Particle Size
  • Peptide Fragments / chemistry
  • Peptides / chemical synthesis
  • Peptides / chemistry*
  • Sensitivity and Specificity
  • Structure-Activity Relationship

Substances

  • Contrast Media
  • Macromolecular Substances
  • Micelles
  • Organometallic Compounds
  • Peptide Fragments
  • Peptides
  • cholecystokinin 8
  • Cholecystokinin
  • Gadolinium