Positron emission tomography imaging of drug-induced tumor apoptosis with a caspase-triggered nanoaggregation probe

Bin Shen, Jongho Jeon, Mikael Palner, Deju Ye, Adam Shuhendler, Frederick T Chin, Jianghong Rao

Research output: Contribution to journalJournal articleResearchpeer-review

Abstract

Drug Design: An (18)F-labeled caspase-3-sensitive nanoaggregation positron emission tomography tracer was prepared and evaluated for imaging the caspase-3 activity in doxorubicin-treated tumor xenografts. Enhanced retention of the (18)F activity in apoptotic tumors is achieved through intramolecular macrocyclization and in situ aggregation upon caspase-3 activation (see picture).

Original languageEnglish
JournalAngewandte Chemie International Edition
Volume52
Issue number40
Pages (from-to)10511-10514
ISSN1433-7851
DOIs
Publication statusPublished - 27. Sept 2013
Externally publishedYes

Bibliographical note

Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Keywords

  • Animals
  • Apoptosis/drug effects
  • Benzothiazoles/chemistry
  • Caspase 3/metabolism
  • Diagnostic Imaging/methods
  • Fluorine Radioisotopes/chemistry
  • HeLa Cells
  • Heterografts
  • Humans
  • Mice
  • Molecular Structure
  • Nanostructures/chemistry
  • Neoplasms/diagnostic imaging
  • Oligopeptides/chemistry
  • Positron-Emission Tomography/methods
  • Radiopharmaceuticals

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