期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 49, 期 14, 页码 4297-4304出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm060317v
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资金
- Intramural NIH HHS Funding Source: Medline
- NCI NIH HHS [R24 CA86307] Funding Source: Medline
A versatile bifunctional chelating reagent based on a preorganized cyclohexyl derivative of DTPA (CHX-A ) has been developed for the convenient N-terminal labeling of peptides with metal ion radionuclides of Bi(III), In(III), Lu(III), or Y(III). This was achieved via the synthesis of a mono-N-hydroxysuccinimidyl penta-tert-butyl ester derivative of CHX-A (trans-cyclohexyldiethylenetriaminepenta-acetic acid) featuring a glutaric acid spacer. Commercially obtained octreotide was modified at its N-terminus by this reagent in the solution phase, and its subsequent radiolabeling with In-111 (T-1/2 = 2.8 d) and Y-86 (T-1/2 = 14.7 h) demonstrated. Small animal PET/CT imaging results of Y-86-CHX-A-octreotide in a somatostatin receptor-positive tumor-bearing rat model are presented for the validation of the novel agent.
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