Article thumbnail

Triazine-Based Tool Box for Developing Peptidic PET Imaging Probes: Syntheses, Microfluidic Radiolabeling, and Structure− Activity Evaluation

By 

Abstract

ABSTRACT: This study was aimed at developing a triazine-based modular platform for targeted PET imaging. We synthesized mono- or bis-cyclo(RGDfK) linked triazine-based conjugates specifically targeting integrin αvβ3 receptors. The core molecules could be easily linked to targeting peptide and radiolabeled bifunctional chelator. The spacer core molecule was synthesized in 2 or 3 steps in 64−80 % yield, and the following conjugation reactions with cyclo(RGDfK) peptide or bifunctional chelator were accomplished using “click ” chemistry or amidation reactions. The DOTA-TZ-Bis-cyclo(RGDfK) 13 conjugate was radiolabeled successfully with 64Cu(OAc)2 using a microfluidic method, resulting in higher specific activity with above 95 % labeling yields compared to conventional radiolabeling (SA ca. 850 vs 600 Ci/mmol). The dimeric cyclo(RGDfK) peptide was found to display significant bivalency effect using I125-Echistatin binding assay with IC50 value as 178.5 ± 57.1 nM, which displayed a 3.6-fold enhancement of binding affinity compared to DOTA-TZ-cyclo(RGDfK) 14 conjugate on U87MG human glioblastoma cell. Biodistribution of al

Year: 2016
OAI identifier: oai:CiteSeerX.psu:10.1.1.775.9320
Provided by: CiteSeerX
Download PDF:
Sorry, we are unable to provide the full text but you may find it at the following location(s):
  • ftp://ftp.ncbi.nlm.nih.gov/pub... (external link)
  • ftp://ftp.ncbi.nlm.nih.gov/pub... (external link)
  • http://citeseerx.ist.psu.edu/v... (external link)

  • To submit an update or takedown request for this paper, please submit an Update/Correction/Removal Request.

    Suggested articles