Affordable Access

deepdyve-link
Publisher Website

Development of an Activatable Fluorescent Probe for Prostate Cancer Imaging.

Authors
  • Yogo, Takao
  • Umezawa, Keitaro
  • Kamiya, Mako1
  • Hino, Rumi2
  • Urano, Yasuteru3
  • 1 PRESTO, Japan Science and Technology Agency , 4-1-8 Honcho, Kawaguchi, Saitama 332-0012, Japan. , (Japan)
  • 2 Department of Sports and Health Science, Daito Bunka University , 560 Iwadono, Higashimathuyama, Saitama 355-8501, Japan. , (Japan)
  • 3 AMED-CREST, Japan Agency for Medical Research and Development , 1-7-1 Otemachi, Chiyoda-ku, Tokyo 100-0004, Japan. , (Japan)
Type
Published Article
Journal
Bioconjugate Chemistry
Publisher
American Chemical Society
Publication Date
Aug 16, 2017
Volume
28
Issue
8
Pages
2069–2076
Identifiers
DOI: 10.1021/acs.bioconjchem.7b00233
PMID: 28691803
Source
Medline
License
Unknown

Abstract

Technology to visualize small prostate cancers is urgently needed because of the difficulty of discriminating prostate cancer from normal tissue with the naked eye, and a fluorescence imaging method would be advantageous. Here, we describe the design and synthesis of a fluorogenic probe (Ac-KQLR-HMRG) that is activated by hepsin and matriptase (proteases over-expressed in prostate cancer). Ac-KQLR-HMRG exhibited significant turn-on fluorogenicity in the presence of hepsin (180-fold) and matriptase (80-fold) and allowed specific fluorescence imaging of various prostate cancer cell line in vitro. In addition, the probe enabled rapid imaging (within 1-10 min) of small prostate cancer nodules in mouse models of disseminated peritoneal tumor and orthotopic tumor.

Report this publication

Statistics

Seen <100 times