Tumor diagnosis with new In-radioligands based on truncated human gastrin releasing peptide sequences: Synthesis and preclinical comparison
Journal of Medicinal Chemistry, ISSN: 0022-2623, Vol: 56, Issue: 21, Page: 8579-8587
2013
- 13Citations
- 10Captures
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Example: if you select the 1-year option for an article published in 2019 and a metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019. If you select the 3-year option for the same article published in 2019 and the metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019, 2018 and 2017.
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Metrics Details
- Citations13
- Citation Indexes13
- 13
- CrossRef11
- Captures10
- Readers10
- 10
Article Description
Radiolabeled analogs of the frog tetradecapeptide bombesin (BBN) have been proposed for diagnosis and therapy of gastrin releasing peptide receptor (GRPR)-expressing tumors. Following a different and yet unexplored approach, we have developed four novel In-labeled truncated analogs of the human 27-mer GRP after conjugation of 1,4,7,10-tetraazacyclododecane-1,4,7,10- tetraacetic acid (DOTA) at the N-terminus of GRP(13/14/17/18-27) fragments. Analog affinities for the human GRPR determined against [I- Tyr]BBN were at the nanomolar level and dependent on truncation site. The respective In radioligands specifically internalized in GRPR-expressing PC-3 cells. The shorter chain [In-DOTA]GRP(17/18- 27) analogs showed higher metabolic stability in mice. Radioligands specifically localized in human PC-3 xenografts in SCID mice, with [In-DOTA] GRP(17-27) exhibiting the most favorable pharmacokinetic profile. This study has demonstrated the efficacy of human GRP-based radiopeptides to target GRPR-positive lesions in vivo and has revealed the impact of GRP chain length on key biological parameters of resulting radiotracers. © 2013 American Chemical Society.
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