rdf:type |
|
lifeskim:mentions |
umls-concept:C0011923,
umls-concept:C0022115,
umls-concept:C0162638,
umls-concept:C0220781,
umls-concept:C0220825,
umls-concept:C0243071,
umls-concept:C0291573,
umls-concept:C1515655,
umls-concept:C1879547,
umls-concept:C1883254,
umls-concept:C2347885
|
pubmed:issue |
19
|
pubmed:dateCreated |
2006-8-25
|
pubmed:abstractText |
A non-peptide-based isatin sulfonamide analog, WC-II-89, was synthesized and its inhibition toward recombinant human caspase-3 and other caspases was determined. This compound showed high potency for inhibiting caspase-3 and -7, and high selectivity against caspases-1, -6, and -8. [(18)F]WC-II-89 was synthesized via a nucleophilic substitution of the corresponding mesylate precursor in high yield and radiochemical purity. Biodistribution studies using [(18)F]WC-II-89 revealed higher uptake in liver and spleen of cycloheximide-treated rats, an animal model of apoptosis, relative to control animals. Western blot analysis confirmed the presence of activated caspase-3 in the liver and spleen of cycloheximide-treated animals. MicroPET imaging studies revealed a high uptake of the radiotracer in the liver of a cycloheximide-treated rat relative to the untreated control. These data suggest that [(18)F]WC-II-89 is a potential radiotracer for imaging caspase-3 activation in tissues undergoing apoptosis.
|
pubmed:grant |
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/CASP3 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/CASP7 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Casp3 protein, rat,
http://linkedlifedata.com/resource/pubmed/chemical/Caspase 3,
http://linkedlifedata.com/resource/pubmed/chemical/Caspase 7,
http://linkedlifedata.com/resource/pubmed/chemical/Caspases,
http://linkedlifedata.com/resource/pubmed/chemical/Fluorine Radioisotopes,
http://linkedlifedata.com/resource/pubmed/chemical/Isatin,
http://linkedlifedata.com/resource/pubmed/chemical/Radiopharmaceuticals,
http://linkedlifedata.com/resource/pubmed/chemical/Recombinant Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Sulfonamides
|
pubmed:status |
MEDLINE
|
pubmed:month |
Oct
|
pubmed:issn |
0960-894X
|
pubmed:author |
|
pubmed:issnType |
Print
|
pubmed:day |
1
|
pubmed:volume |
16
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
5041-6
|
pubmed:dateRevised |
2010-4-12
|
pubmed:meshHeading |
pubmed-meshheading:16891117-Animals,
pubmed-meshheading:16891117-Apoptosis,
pubmed-meshheading:16891117-Caspase 3,
pubmed-meshheading:16891117-Caspase 7,
pubmed-meshheading:16891117-Caspases,
pubmed-meshheading:16891117-Fluorine Radioisotopes,
pubmed-meshheading:16891117-Isatin,
pubmed-meshheading:16891117-Liver,
pubmed-meshheading:16891117-Positron-Emission Tomography,
pubmed-meshheading:16891117-Radionuclide Imaging,
pubmed-meshheading:16891117-Radiopharmaceuticals,
pubmed-meshheading:16891117-Rats,
pubmed-meshheading:16891117-Recombinant Proteins,
pubmed-meshheading:16891117-Spleen,
pubmed-meshheading:16891117-Sulfonamides,
pubmed-meshheading:16891117-Tissue Distribution
|
pubmed:year |
2006
|
pubmed:articleTitle |
Synthesis, radiolabeling, and in vivo evaluation of an 18F-labeled isatin analog for imaging caspase-3 activation in apoptosis.
|
pubmed:affiliation |
Division of Radiological Sciences, Washington University School of Medicine, 510 South Kingshighway Boulevard, St. Louis, MO 63110, USA.
|
pubmed:publicationType |
Journal Article,
Research Support, N.I.H., Extramural
|