Journal
CURRENT MOLECULAR MEDICINE
Volume 13, Issue 10, Pages 1487-1505Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1566524013666131111115347
Keywords
Arg-Gly-Asp (RGD); integrin alpha(v)beta(3); molecular imaging; radionuclide therapy; radiotracer; tumor
Categories
Funding
- National Natural Science Foundation of China (NSFC) [81222019, 30930030, 81000625, 30870728, 30900373, 81028009]
- Outstanding Youth Fund [81125011]
- 973 projects [2011CB707703, 2013CB733802]
- Ministry of Science and Technology of China [2011 YQ030114, 2012BAK25B03-16, 2012ZX091023 01-018]
- Innovation Team Project of Ministry of Education of China [BMU20110263]
- Beijing Natural Science Foundation [7132131, 7132123]
- Beijing Nova Program [Z121107002512010]
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The cell adhesion molecule integrin alpha(v)beta(3) is an important player in the process of angiogenesis. In the last decades, a series of radiolabeled Arg-Gly-Asp (RGD) peptides targeting integrin alpha(v)beta(3) has been prepared and optimized for positron emission tomography (PET) and single-photon-emission computed tomography (SPECT) imaging of integrin alpha(v)beta(3) expression. Several promising radiotracers have been tested in clinical trials. In this review, we will introduce strategies that have been used to optimize and accelerate RGD radiotracers towards clinical translation; illustrate RGD-based radiotracers that have been investigated in clinical trials; and discuss the other applications of RGD radiotracers aside from tumor detection.
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