期刊
BIOCONJUGATE CHEMISTRY
卷 27, 期 2, 页码 309-318出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.bioconjchem.5b00335
关键词
-
类别
资金
- European Union [299009]
- Royal Society of Chemistry through a Researcher Mobility Fellowship
- Leukaemia and Lymphoma Research
- Alzheimer's Society
- Centre of Excellence in Medical Engineering - Wellcome Trust
- Centre of Excellence in Medical Engineering - EPSRC [WT088641/Z/09/Z]
- KCL and UCL Comprehensive Cancer Imaging Centre - CRUK
- KCL and UCL Comprehensive Cancer Imaging Centre - EPSRC
- MRC
- DoH (England)
- NIHR Biomedical Research Centre at Guy's and St Thomas' NHS Foundation Trust
- King's College London
- Cancer Research UK [16463] Funding Source: researchfish
Two new bifunctional tris(hydroxypyridinone) (THP) chelators designed specifically for rapid labeling with Ga-68 have been synthesized, each with pendant isothiocyanate groups and three 1,6-dimethyl-3-hydroxypyridin-4-one groups. Both compounds have been conjugated with the primary amine group of a cyclic integrin targeting peptide, RGD. Each conjugate can be radiolabeled and formulated by treatment with generator-produced Ga-68(3+) in over 95% radiochemical yield under ambient conditions in less than 5 min, with specific activities of 60-80 MBq nmol(-1). Competitive binding assays and in vivo biodistribution in mice bearing U87MG tumors demonstrate that the new Ga-68(3+)-labeled THP peptide conjugates retain affinity for the alpha(v)beta(3) integrin receptor, clear within 1-2 h from circulation, and undergo receptor mediated tumor uptake in vivo. We conclude that bifunctional THP chelators can be used for simple, efficient labeling of 68Ga biomolecules under mild conditions suitable for peptides and proteins.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据