Abstract:
INTRODUCTION:The α(V)β(3) integrin is a well-known transmembrane receptor involved in tumor invasion, angiogenesis and metastasis. Our aim was to evaluate a novel positron emission tomography (PET) probe, (64)Cu-cyclam-RAFT-c(-RGDfK-)(4), for noninvasive visualization and quantification of α(V)β(3) integrin expression. METHODS:RAFT-c(-RGDfK-)(4), a tetrameric cyclic Arg-Gly-Asp (RGD)-based peptide, was conjugated with a bifunctional chelator, 1,4,8,11-tetraazacyclotetradecane (cyclam), radiolabeled with the positron emitter (64)Cu and evaluated in vitro by cell binding and competitive inhibition assays and in vivo by biodistribution and receptor blocking studies, and PET imaging. The following cell lines, human embryonic kidney HEK293(β(1)) [α(V)β(3)-negative] and HEK293(β(3)) [α(V)β(3)-overexpressing] and human glioblastoma U87MG [naturally expressing α(V)β(3)], together with their subcutaneous xenografts in athymic nude mice, were used for the present study. The expression levels of α(V)β(3) on these cell lines and tumor xenografts were analyzed by flow cytometry and sodium dodecyl sulfate-polyacrylamide gel electrophoresis/autoradiography, respectively. RESULTS:(64)Cu-cyclam-RAFT-c(-RGDfK-)(4) demonstrated the in vitro and in vivo specificity for the α(V)β(3) integrin and displayed rapid blood clearance, predominantly renal excretion and low uptake in nontumor tissues. Tumor uptake of (64)Cu-cyclam-RAFT-c(-RGDfK-)(4) (3 h postinjection) in HEK293(β(3)) (high levels of α(V)β(3)), U87MG (moderate levels of α(V)β(3)) and HEK293(β(1)) (undetectable levels of α(V)β(3)) tumors was 9.35%±1.19%, 3.46%±0.45% and 1.18%±0.30% injected dose per gram, respectively, with a strong and positive correlation with the tumor α(V)β(3) expression levels (correlation coefficient=0.967; P<.0001). Positron emission tomographic images showed that α(V)β(3)-positive tumors were clearly visualized with high tumor-to-background contrast, and agreed well with the biodistribution results. CONCLUSION:(64)Cu-cyclam-RAFT-c(-RGDfK-)(4) exhibits potential for noninvasively quantifying α(V)β(3) expression.
journal_name
Nucl Med Bioljournal_title
Nuclear medicine and biologyauthors
Jin ZH,Furukawa T,Galibert M,Boturyn D,Coll JL,Fukumura T,Saga T,Dumy P,Fujibayashi Ydoi
10.1016/j.nucmedbio.2010.11.008subject
Has Abstractpub_date
2011-05-01 00:00:00pages
529-40issue
4eissn
0969-8051issn
1872-9614pii
S0969-8051(10)00487-7journal_volume
38pub_type
杂志文章abstract:UNLABELLED:The evaluation of oxygenation status of solid tumors is an important field of radiopharmaceutical research. With the aim to develop new potential 99mTc-radiopharmaceuticals for imaging hypoxia, we have synthesized two novel isocyanide derivatives of metronidazole, which has demonstrated high affinity for hyp...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/j.nucmedbio.2011.12.012
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journal_title:Nuclear medicine and biology
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doi:10.1016/j.nucmedbio.2013.12.014
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journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/s0969-8051(00)00125-6
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journal_title:Nuclear medicine and biology
pub_type: 杂志文章
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journal_title:Nuclear medicine and biology
pub_type: 临床试验,杂志文章
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abstract::Sixteen patients with colorectal cancer were administered 37-74 MBq (1 mg) of radioiodinated B72.3 monoclonal antibody. Pharmacokinetic analysis was carried out on plasma and urine samples. Elimination from the plasma was biexponential with a mean T1/2 alpha of 3.7 h and T1/2 beta of 62.4 h. The plasma clearance was f...
journal_title:Nuclear medicine and biology
pub_type: 杂志文章
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journal_title:Nuclear medicine and biology
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journal_title:Nuclear medicine and biology
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journal_title:Nuclear medicine and biology
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pub_type: 杂志文章
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pub_type: 杂志文章
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更新日期:2013-01-01 00:00:00
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pub_type: 杂志文章
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更新日期:2014-05-01 00:00:00
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journal_title:Nuclear medicine and biology
pub_type: 杂志文章
doi:10.1016/s0969-8051(97)00222-9
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journal_title:Nuclear medicine and biology
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更新日期:2000-01-01 00:00:00
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journal_title:Nuclear medicine and biology
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更新日期:1995-11-01 00:00:00
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pub_type: 杂志文章
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更新日期:1995-08-01 00:00:00
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journal_title:Nuclear medicine and biology
pub_type: 杂志文章,评审
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更新日期:2001-07-01 00:00:00
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journal_title:Nuclear medicine and biology
pub_type: 杂志文章
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更新日期:1998-10-01 00:00:00
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更新日期:2012-07-01 00:00:00
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更新日期:2000-11-01 00:00:00
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pub_type: 杂志文章
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更新日期:2018-01-01 00:00:00