Published March 2012 | Version v1
Journal article

Synthesis, radiometal labeling and in vitro evaluation of a targeted PPIX derivative

  • 1. Department of Chemistry, University of Western Ontario, 1151 Richmond Street, London, Ontario, N6A 5B7 (Canada)
  • 2. Department of Medical Biophysics, University of Western Ontario, 1151 Richmond Street, London, Ontario, N6A 5B7 (Canada)
  • 3. London Regional Cancer Program, 790 Commissioners Road East, London, Ontario, N6A 4L6 (Canada)
  • 4. Department of Surgery, University of Western Ontario, 1151 Richmond Street, London, Ontario, N6A 5B7 (Canada)
  • 5. Department of Oncology, University of Western Ontario, 1151 Richmond Street, London, Ontario, N6A 5B7 (Canada)
  • 6. Department of Medical Imaging, University of Western Ontario, 1151 Richmond Street, London, Ontario, N6A 5B7 (Canada)

Description

In pursuit of a single molecule with potential applications for both in vitro fluorescence microscopy and in vivo PET imaging, novel targeted 69/71Ga/68Ga-protoporphyrin IX (PPIX) probes were developed. Optical analysis, fluorescence microscopy and radiolabeling with gallium-68 were performed to confirm potential applications. The use of a targeted-PPIX ring, in conjunction with 69/71Ga or 68Ga, eliminates the need for the attachment of multiple imaging tags, allowing for either in vitro fluorescent-based evaluation or in vivo nuclear-based imaging. - Highlights: ► Synthesized and characterized αvβ3 targeted 69/71Ga/68Ga-PPIX analogues. ► Gallium chelation does not quench fluorescence. ► In vitro fluorescence microscopy indicates specific uptake of tracer. ► Gallium-68 labeling of PPIX is optimal in a microwave reactor.

Availability note (English)

Available from http://dx.doi.org/10.1016/j.apradiso.2011.11.054

Additional details

Identifiers

DOI
10.1016/j.apradiso.2011.11.054;
PII
S0969-8043(11)00608-7;

Publishing Information

Journal Title
Applied Radiation and Isotopes
Journal Volume
70
Journal Issue
3
Journal Page Range
p. 505-511
ISSN
0969-8043
CODEN
ARISEF

Optional Information

Copyright
Copyright (c) 2011 Elsevier Science B.V., Amsterdam, The Netherlands, All rights reserved.