期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 48, 期 1, 页码 100-110出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm049437y
关键词
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Four open chain tetraamine-functionalized bombesin (BB) analogues were synthesized [parent tetradecapeptide-based Demobesin 3 and 4 and BB(7-14)-based Demobesin 5 and 6]. Labeling with Tc-99m afforded high-purity and high specific activity radiotracers. Peptides showed high affinity for the human GRP-R (GRP-R = gastrin releasing peptide receptor) expressed in PC-3 cells. In human tumors preferentially expressing single bombesin receptor subtypes, they showed high affinity for the GRP-R, less affinity for the NMB-R (NMB-R = neuromedin B receptor) and no affinity for the orphan BB3-R (bombesin subtype 3 receptor). [Tc-99m]Demobesin 3-6 efficiently internalized in a time- and dose-dependent manner in PC-3 cells and showed a high and specific uptake in human PC-3 xenografts and the pancreas of nude mice. [Tc-99m]-Demobesin 3 and 4 were rapidly excreted via the kidneys while the truncated analogues were predominantly processed by the hepatobiliary system. Patient studies are scheduled for validating the suitability of [Tc-99m]Demobesin 3 and 4 in the GRP-R-targeted imaging of tumors.
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