RESEARCH ARTICLE
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F-FP-PEG -β-Glu-RGD : A Symmetric
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Integrin α β -Targeting Radiotracer for
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Tumor PET Imaging
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Kongzhen Hu , Xiaolan Tang , Ganghua Tang *, Shaobo Yao , Baoguo Yao ,
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Hongliang Wang , Dahong Nie *, Xiang Liang , Caihua Tang , Shanzhen He
1 Department of Nuclear Medicine, the First Affiliated Hospital, Sun Yat-Sen University, Guangzhou,
510080, China, 2 College of Materials and Energy, Southern China Agricultural University, Guangzhou,
510642, China
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These authors contributed equally to this work.
¤ Current address: Department of Chemistry, Stony Brook University, New York, 11794, United Stated of
America
*
Abstract
OPEN ACCESS
Radiolabeled cyclic arginine-glycine-aspartic (RGD) peptides can be used for noninvasive
determination of integrin α β expression in tumors. In this study, we performed radiosynth-
Citation: Hu K, Tang X, Tang G, Yao S, Yao B, Wang
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H, et al. (2015) F-FP-PEG -β-Glu-RGD : A
esis and biological evaluation of a new F-labeled RGD homodimeric peptide with one 8-
Symmetric Integrin α -Targeting Radiotracer for
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β
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amino-3,6-dioxaoctanoic acid (PEG ) linker on the glutamate β-amino group ( F-FP-
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Tumor PET Imaging. PLoS ONE 10(9): e0138675.
doi:10.1371/journal.pone.0138675
PEG -β-Glu-RGD ) as a symmetric PET tracer for tumor imaging. Biodistribution studies
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showed that radioactivity of F-FP-PEG -β-Glu-RGD was rapidly cleared from blood by
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Editor: Effie C Tsilibary, National Center for Scientific
Research Demokritos, GREECE
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predominately renal excretion. MicroPET-CT imaging with F-FP-PEG -β-Glu-RGD2
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revealed high tumor contrast and low background in A549 human lung adenocarcinoma-
bearing mouse models, PC-3 prostate cancer-bearing mouse models, and orthotopic trans-
Received: July 5, 2015
Accepted: September 2, 2015
Published: September 23, 2015
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planted C6 brain glioma models. F-FP-PEG -β-Glu-RGD exhibited good stability in vitro
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and in vivo. The results suggest that this tracer is a potential PET tracer for tumor imaging.
Copyright: © 2015 Hu et al. This is an open access
unrestricted use, distribution, and reproduction in any
medium, provided the original author and source are
credited.
Introduction
Data Availability Statement: All relevant data are
within the paper.
Angiogenesis is the process of formation of new vessels in avascular tissue. It plays a key role in a
variety of processes such as rheumatoid arthritis [1], psoriasis [2], cardiovascular diseases [3],
diabetic retinopathy [4], and tumor growth, as well as tumor metastasis [5]. The angiogenic pro-
cess depends on vascular endothelial cells (ECs) migration and invasion [6]. Integrin αvβ3
involves in the migration of ECs during formation of new blood vessels and is highly expressed
only in activated ECs of tumor neovasculature, not in normal cells or quiescent ECs [7]. Mono-
meric cyclic arginine-glycine-aspartic (RGD) peptides and analogs showed high affinity and
Funding: This work was funded by the National
Natural Science Foundation (No. 81571704, No.
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1371584, No.81201116), the Science Technology
Foundation of Guangdong Province (No.
014A020210008, No.2013B021800264), Science
and Technology Planning Project of Guangzhou (No.
011J5200025, No. 201510010145), the Wu Jieping
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selectivity for the integrin α β [8]. Thus, several radiolabeled monomeric RGD peptides and
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analogs have been developed for monitoring and quantifying integrin α β expression noninva-
sively in tumors with positron emission tomography (PET) [9–16]. For example, F-galacto-
Medical Foundation (320675013203), and Sun Yat-
Sen University (No. 80000-3126132).
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PLOS ONE | DOI:10.1371/journal.pone.0138675 September 23, 2015
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