AI Article Synopsis
- Noninvasive imaging of integrin expression, particularly αvβ3, using 18F-labeled cyclic RGD peptides has gained significant attention in nuclear medicine.
- Recent advancements have also focused on other integrins, like α5β1 and αvβ6, leading to the evaluation of various tracers in clinical trials.
- The review highlights developments aimed at optimizing existing compounds, such as [18F]Galacto-RGD, and explores new 18F-labeling and 68Ga-complex chemistry methods for creating radiopharmaceuticals targeting these integrins.
Article Abstract
Noninvasive determination of integrin expression has become an interesting approach in nuclear medicine. Since the discovery of the first 18F-labeled cyclic RGD peptide as radiotracer for imaging integrin αvβ3 expression in vivo, there have been carried out enormous efforts to develop RGD peptides for PET imaging. Moreover, in recent years, additional integrins, including α5β1 and αvβ6 came into the focus of pharmaceutical radiochemistry. This review will discuss the tracers already evaluated in clinical trials and summarize the preliminary outcome. It will also give an overview on recent developments to further optimize the first-generation compounds such as [18F]Galacto-RGD. This includes recently developed 18F-labeling strategies and also new approaches in 68Ga-complex chemistry. Furthermore, the approaches to develop radiopharmaceuticals targeting integrin α5β1 and αvβ6 will be summarized and discussed.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4072020 | PMC |
| http://dx.doi.org/10.1155/2014/871609 | DOI Listing |
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