Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
3
pubmed:dateCreated
2004-3-11
pubmed:abstractText
Cyclooxygenase-2 (COX-2) plays an important role in angiogenesis and cancer progression. Since many tumor cells exhibit COX-2 expression, functional imaging of COX-2 expression using celebrex (CBX, a COX-2 inhibitor) may provide not only a non-invasive, reproducible, quantifiable alternative to biopsies, but it also greatly complements pharmacokinetic studies by correlating clinical responses with biological effects. Moreover, molecular endpoints of anti-COX-2 therapy could also be assessed effectively. This study aimed at measuring uptake of Tc-EC-CBX in COX-2 expression in tumor-bearing animal models. In vitro Western blot analysis and cellular uptake assays were used to examine the feasibility of using Tc-EC-CBX to measure COX-2 activity. Tissue distribution studies of Tc-EC-CBX were evaluated in tumor-bearing rodents at 0.5-4 h. Dosimetric absorption was then estimated. Planar scintigraphy was performed in mice, rats and rabbits bearing tumors. In vitro cellular uptake indicated that cells with higher COX-2 expression (A549 and 13762) had higher uptake of Tc-EC-CBX than lower COX-2 expression (H226). In vivo biodistribution of Tc-EC-CBX in tumor-bearing rodents showed increased tumor:tissue ratios as a function of time. In vitro and biodistribution studies demonstrated the possibility of using Tc-EC-CBX to assess COX-2 expression. Planar images confirmed that the tumors could be visualized with Tc-EC-CBX from 0.5 to 4 h in tumor-bearing animal models. We conclude that Tc-EC-CBX may be useful to assess tumor COX-2 expression. This may be useful in the future for selecting patients for treatment with anti-COX-2 agents.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Mar
pubmed:issn
0959-4973
pubmed:author
pubmed:issnType
Print
pubmed:volume
15
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
255-63
pubmed:dateRevised
2007-11-14
pubmed:meshHeading
pubmed-meshheading:15014359-Animals, pubmed-meshheading:15014359-Cell Line, Tumor, pubmed-meshheading:15014359-Cyclooxygenase 2, pubmed-meshheading:15014359-Dose-Response Relationship, Drug, pubmed-meshheading:15014359-Female, pubmed-meshheading:15014359-Gene Expression Regulation, Enzymologic, pubmed-meshheading:15014359-Humans, pubmed-meshheading:15014359-Isoenzymes, pubmed-meshheading:15014359-Male, pubmed-meshheading:15014359-Membrane Proteins, pubmed-meshheading:15014359-Mice, pubmed-meshheading:15014359-Prostaglandin-Endoperoxide Synthases, pubmed-meshheading:15014359-Pyrazoles, pubmed-meshheading:15014359-Radionuclide Imaging, pubmed-meshheading:15014359-Rats, pubmed-meshheading:15014359-Rats, Inbred F344, pubmed-meshheading:15014359-Sulfonamides, pubmed-meshheading:15014359-Technetium, pubmed-meshheading:15014359-Xenograft Model Antitumor Assays
pubmed:year
2004
pubmed:articleTitle
Assessment of cyclooxygense-2 expression with 99mTc-labeled celebrex.
pubmed:affiliation
Division of Diagnostic Imaging, University of Texas M D Anderson Cancer Center, Houston, TX 77030, USA. dyang@di.mdacc.tmc.edu
pubmed:publicationType
Journal Article, Research Support, U.S. Gov't, P.H.S., Research Support, Non-U.S. Gov't