SYNTHESIS OF NOVEL PEPTIDE NUCLEIC ACID-PEPTIDE CHIMERA FOR NON-INVASIVE IMAGING OF CANCER

Abstract

A chelator-peptide-PNA-peptide chimera specific for KRAS has been prepared by continuous solid phase coupling with a C-terminal insulin-like growth factor 1 (IGF1) ligand, d(cys-ser-lys-cys), and N-terminal bis(s-benzoyl thioglycoloyl) diaminopropanoate chelator for radionuclide labeling. The probe was purified by RP-HPLC and characterized by MALDI-TOF mass spectroscopy. The probe was labeled with ^{99 m}Tc and ⁶⁴Cu. Both labeled probes accumulated in human pancreatic cancer xenografts in immunocompromised mice. Control experiments with mismatch chimeras and control xenografts will be necessary to determine the specificity of this molecular diagnostic strategy.

Keywords:

• Antisense
• Imaging
• KRAS
• Oncogene
• Peptide Nucleic Acid
• Positron
• Radionuclide