Selective accumulation of [62Zn]-labeled glycoconjugated porphyrins as multi-functional positron emission tomography tracers in cancer cells

Masato Tamura, Hirofumi Matsui, Shiho Hirohara, Kiyomi Kakiuchi, Masao Tanihara, Naruto Takahashi, Kozi Nakai, Yasukazu Kanai, Hiroshi Watabe, Jun Hatazawa

Research output: Contribution to journalArticle

11 Citations (Scopus)

Abstract

Positron-emission tomography (PET) can be used to visualize active stage cancer. Fluorine-18 ([18F])-labeled 2-([18F])2-deoxy-2- fluoroglucose (([18F])-FDG), which accumulates in glucose-dependent tissues, is a good cancer-targeting tracer. However, ([18F])-FDG is obscured in glucose-dependent normal tissues. In this study, we assessed the cancer-selective accumulation of zinc-labeled glycoconjugated 5,10,15,20-tetrakis(pentafluorophenyl)porphyrin (ZnGlc1-4), both in vitro and in vivo. Experiments using both normal and cancer cells confirmed the relationship between cancer cell-selective accumulation and the substitution numbers and orientations of glycoconjugated porphyrins. ZnGlctrans-2 accumulated at greater levels in cancer cells compared with other glycoconjugated porphyrins. PET imaging showed that ZnGlctrans-2 accumulated in tumor.

Original languageEnglish
Pages (from-to)2563-2570
Number of pages8
JournalBioorganic and Medicinal Chemistry
Volume22
Issue number8
DOIs
Publication statusPublished - 2014 Apr 15

Keywords

  • Cancer selective accumulation
  • Positron emission tomography

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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