Synthesis and in vitro evaluation of a novel radioligand for αvβ3 integrin receptor imaging: [(18)F]FPPA-c(RGDfK).

Details

Serval ID
serval:BIB_66572DB13977
Type
Article: article from journal or magazin.
Collection
Publications
Institution
Title
Synthesis and in vitro evaluation of a novel radioligand for αvβ3 integrin receptor imaging: [(18)F]FPPA-c(RGDfK).
Journal
Bioorganic and Medicinal Chemistry Letters
Author(s)
Monaco A., Zoete V., Alghisi G.C., Rüegg C., Michelin O., Prior J., Scapozza L., Seimbille Y.
ISSN
1464-3405 (Electronic)
ISSN-L
0960-894X
Publication state
Published
Issued date
2013
Volume
23
Number
22
Pages
6068-6072
Language
english
Notes
Publication types: Journal ArticlePublication Status: ppublish
Abstract
The development of RGD-based antagonist of αvβ3 integrin receptor has enhanced the interest in PET probes to image this receptor for the early detection of cancer, to monitor the disease progression and the response to therapy. In this work, a novel prosthetic group (N-(4-fluorophenyl)pent-4-ynamide or FPPA) for the (18)F-labeling of an αvβ3 selective RGD-peptide was successfully prepared. [(18)F]FPPA was obtained in three steps with a radiochemical yield of 44% (decay corrected). Conjugation to c(RGDfK(N3)) by the Cu(II) catalyzed Huisgen azido alkyne cycloaddition provided the [(18)F]FPPA-c(RGDfK) with a radiochemical yield of 29% (decay corrected), in an overall synthesis time of 140min.
Pubmed
Web of science
Create date
17/11/2013 19:14
Last modification date
20/08/2019 15:22
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