title: Positron emission tomography imaging of drug-induced tumor apoptosis with a caspase-triggered nanoaggregation probe.
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).
authors.affiliation: Department of Radiology, Molecular Imaging Program at Stanford, Stanford University School of Medicine, Stanford, CA 94305-5484 (USA).
authors.forename: Bin
authors.initials: B
authors.lastname: Shen
authors.forename: Jongho
authors.initials: J
authors.lastname: Jeon
authors.forename: Mikael
authors.initials: M
authors.lastname: Palner
authors.forename: Deju
authors.initials: D
authors.lastname: Ye
authors.forename: Adam
authors.initials: A
authors.lastname: Shuhendler
authors.forename: Frederick T
authors.initials: FT
authors.lastname: Chin
authors.forename: Jianghong
authors.initials: J
authors.lastname: Rao
mesh_terms: D000818:Animals; D017209:Apoptosis / Q000187:drug effects*; D052160:Benzothiazoles / Q000737:chemistry; D053148:Caspase 3 / Q000378:metabolism*; D003952:Diagnostic Imaging / Q000379:methods*; D005462:Fluorine Radioisotopes / Q000737:chemistry; D006367:HeLa Cells; D064593:Heterografts; D006801:Humans; D051379:Mice; D015394:Molecular Structure; D049329:Nanostructures / Q000737:chemistry*; D009369:Neoplasms / Q000000981:diagnostic imaging* / Q000188:drug therapy / Q000201:enzymology / Q000473:pathology; D009842:Oligopeptides / Q000737:chemistry; D049268:Positron-Emission Tomography / Q000379:methods*; D019275:Radiopharmaceuticals
chemical_list: D052160:Benzothiazoles; C000602832:C-SNAT compound; D005462:Fluorine Radioisotopes; D009842:Oligopeptides; D019275:Radiopharmaceuticals; D053148:Caspase 3
keywords: apoptosis; caspase-3; cyclization; drug design; positron emission tomography