Journal
THERANOSTICS
Volume 6, Issue 1, Pages 78-92Publisher
IVYSPRING INT PUBL
DOI: 10.7150/thno.13242
Keywords
Angiogenesis; RGD; PET; clinical translation
Categories
Funding
- National Natural Science Foundation of China [81471684, 81371596]
- Intramural Research Program, National Institute of Biomedical Imaging and Bioengineering, National Institutes of Health
- China Scholarship Council (CSC)
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Molecular imaging for non-invasive assessment of angiogenesisis is of great interest for clinicians because of the wide-spread application of anti-angiogenic cancer therapeutics. Besides, many other interventions that involve the change of blood vessel/tumor microenvironment would also benefit from such imaging strategies. Of the imaging techniques that target angiogenesis, radiolabeled Arg-Gly-Asp (RGD) peptides have been a major focus because of their high affinity and selectivity for integrin alpha(v)beta(3)-one of the most extensively examined target of angiogenesis. Since the level of integrin alpha(v)beta(3) expression has been established as a surrogate marker of angiogenic activity, imaging alpha(v)beta(3) expression can potentially be used as an early indicator of effectiveness of antiangiogenic therapy at the molecular level. In this review, we summarize RGD-based PET tracers that have already been used in clinical trials and intercompared them in terms of radiosynthesis, dosimetry, pharmacokinetics and clinical applications. A perspective of their future use in the clinic is also provided.
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