Skip to main content

Main menu

  • Home
  • Content
    • Current
    • Ahead of print
    • Past Issues
    • JNM Supplement
    • SNMMI Annual Meeting Abstracts
    • Continuing Education
    • JNM Podcasts
  • Subscriptions
    • Subscribers
    • Institutional and Non-member
    • Rates
    • Journal Claims
    • Corporate & Special Sales
  • Authors
    • Submit to JNM
    • Information for Authors
    • Assignment of Copyright
    • AQARA requirements
  • Info
    • Reviewers
    • Permissions
    • Advertisers
  • About
    • About Us
    • Editorial Board
    • Contact Information
  • More
    • Alerts
    • Feedback
    • Help
    • SNMMI Journals
  • SNMMI
    • JNM
    • JNMT
    • SNMMI Journals
    • SNMMI

User menu

  • Subscribe
  • My alerts
  • Log in
  • My Cart

Search

  • Advanced search
Journal of Nuclear Medicine
  • SNMMI
    • JNM
    • JNMT
    • SNMMI Journals
    • SNMMI
  • Subscribe
  • My alerts
  • Log in
  • My Cart
Journal of Nuclear Medicine

Advanced Search

  • Home
  • Content
    • Current
    • Ahead of print
    • Past Issues
    • JNM Supplement
    • SNMMI Annual Meeting Abstracts
    • Continuing Education
    • JNM Podcasts
  • Subscriptions
    • Subscribers
    • Institutional and Non-member
    • Rates
    • Journal Claims
    • Corporate & Special Sales
  • Authors
    • Submit to JNM
    • Information for Authors
    • Assignment of Copyright
    • AQARA requirements
  • Info
    • Reviewers
    • Permissions
    • Advertisers
  • About
    • About Us
    • Editorial Board
    • Contact Information
  • More
    • Alerts
    • Feedback
    • Help
    • SNMMI Journals
  • View or Listen to JNM Podcast
  • Visit JNM on Facebook
  • Join JNM on LinkedIn
  • Follow JNM on Twitter
  • Subscribe to our RSS feeds
Meeting ReportMolecular Targeting Probes - Radioactive & Nonradioactive

18F-BODIPY labeled pegylated peptide probe for PET imaging of MT1-MMP activity in cancers

Takashi Temma, Naoya Kondo, Masahiro Ono and Hideo Saji
Journal of Nuclear Medicine May 2015, 56 (supplement 3) 1127;
Takashi Temma
1Dept of Invest Radiol, NCVC, Suita, Japan
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Naoya Kondo
2Grad Sch of Pharm Sci, Kyoto Univ, Kyoto, Japan
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Masahiro Ono
2Grad Sch of Pharm Sci, Kyoto Univ, Kyoto, Japan
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Hideo Saji
2Grad Sch of Pharm Sci, Kyoto Univ, Kyoto, Japan
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
  • Article
  • Info & Metrics
Loading

Abstract

1127

Objectives Membrane type-1 matrix metalloproteinase (MT1-MMP) plays pivotal roles in tumor metastasis. Thus, we aimed to develop a novel 18F labeled peptide probe for in vivo imaging of MT1-MMP activity. This probe, 18F-MBP, consists of 18F-BODIPY, a MT1-MMP substrate sequence, and PEG. Following MT1-MMP-dependent cleavage of the probe to remove the PEG moiety, the radioactivity would be expected to accumulate in tumor cells due to the high lipophilicity of BODIPY. Here, we evaluated five substrate peptides and four PEGs by in vitro FRET assays and biodistribution experiments to obtain 18F-MBP. Finally, we performed a pre-clinical evaluation of the usefulness of 18F-MBP for in vivo PET imaging of MT1-MMP.

Methods FRET probes consisting of BODIPY 650/665-SE, five substrate peptides, and a fluorescence quencher were synthesized. The resulting probes were incubated with hMT1-MMP protein followed by fluorescence measurement. Cell microscopy was performed using MT1-MMP-positive HT1080 cells with the MMP inhibitor GM6001. 19F-MBPs with four different PEG lengths were evaluated by in vivo fluorescence imaging in tumor bearing mice. Synthesized 18F-BODIPY was reacted with a pegylated peptide to obtain 18F-MBP and PET/CT scans were performed on tumor bearing mice.

Results Fluorescence was increased by hMT1-MMP treatment in four out of five FRET probes tested. Fluorescence of the four probes in HT1080 cells was inhibited by GM6001, indicating MMP-dependent accumulation. The substrate sequence adopted for 18/19F-MBPs was determined from the one FRET probe that showed the highest imaging contrast in vivo. Meanwhile, among the 19F-MBPs tested, 19F-MBP with 2 kDa PEG showed the highest fluorescence in HT1080 tumors. Compared with MT1-MMP-negative A549 tumors, 18F-MBP synthesized with a 78% radiochemical yield from 18F-BODIPY and more than 99% radiochemical purity could clearly depict HT1080 tumors by PET 2 h after injection.

Conclusions We successfully developed 18F-MBP, which is predicted to have useful applications for in vivo evaluation of MT1-MMP activity in tumors.

Previous
Back to top

In this issue

Journal of Nuclear Medicine
Vol. 56, Issue supplement 3
May 1, 2015
  • Table of Contents
  • Index by author
Article Alerts
Sign In to Email Alerts with your Email Address
Email Article

Thank you for your interest in spreading the word on Journal of Nuclear Medicine.

NOTE: We only request your email address so that the person you are recommending the page to knows that you wanted them to see it, and that it is not junk mail. We do not capture any email address.

Enter multiple addresses on separate lines or separate them with commas.
18F-BODIPY labeled pegylated peptide probe for PET imaging of MT1-MMP activity in cancers
(Your Name) has sent you a message from Journal of Nuclear Medicine
(Your Name) thought you would like to see the Journal of Nuclear Medicine web site.
Citation Tools
18F-BODIPY labeled pegylated peptide probe for PET imaging of MT1-MMP activity in cancers
Takashi Temma, Naoya Kondo, Masahiro Ono, Hideo Saji
Journal of Nuclear Medicine May 2015, 56 (supplement 3) 1127;

Citation Manager Formats

  • BibTeX
  • Bookends
  • EasyBib
  • EndNote (tagged)
  • EndNote 8 (xml)
  • Medlars
  • Mendeley
  • Papers
  • RefWorks Tagged
  • Ref Manager
  • RIS
  • Zotero
Share
18F-BODIPY labeled pegylated peptide probe for PET imaging of MT1-MMP activity in cancers
Takashi Temma, Naoya Kondo, Masahiro Ono, Hideo Saji
Journal of Nuclear Medicine May 2015, 56 (supplement 3) 1127;
Twitter logo Facebook logo LinkedIn logo Mendeley logo
  • Tweet Widget
  • Facebook Like
  • Google Plus One
Bookmark this article

Jump to section

  • Article
  • Info & Metrics

Related Articles

  • No related articles found.
  • Google Scholar

Cited By...

  • No citing articles found.
  • Google Scholar

More in this TOC Section

Molecular Targeting Probes - Radioactive & Nonradioactive

  • A general 11C-carboxylation approach mediated by fluoride-desilylation of organosilanes
  • Relationships between tau, atrophy, regional brain activity and connectivity in Alzheimer's disease: a PET/MRI multimodal study
  • Gray matter structural networks related to 18F-THK5351 retention in cognitively normal older adults and early Alzheimer’s disease patients
Show more Molecular Targeting Probes - Radioactive & Nonradioactive

Special MTA: Preclinical Probes for Oncology Posters

  • Preclinical evaluation of somatostatin receptor agonist versus antagonist radioligands for breast cancer imaging
  • Engineering of intrinsically zirconium-89 radiolabeled self-destructing mesoporous silica nanostructures for in vivo tumor vasculature targeting
  • Preclinical evaluation of folate-NOTA-Al[18F] for PET imaging of folate receptor-positive tumors
Show more Special MTA: Preclinical Probes for Oncology Posters

Similar Articles

SNMMI

© 2025 SNMMI

Powered by HighWire