Fluorine-18 click radiosynthesis and microPET/CT evaluation of a small peptide-a potential PET probe for carbonic anhydrase IX

doi:10.1016/j.bmc.2019.01.014

CORC > 上海应用物理研究所 > 中国科学院上海应用物理研究所 > 中科院上海应用物理研究所2011-2017年

	Fluorine-18 click radiosynthesis and microPET/CT evaluation of a small peptide-a potential PET probe for carbonic anhydrase IX
	Jia, LN ; Li, X ; Cheng, DF ; Zhang, L
刊名	BIOORGANIC & MEDICINAL CHEMISTRY
	2019
卷号	27 期号:5 页码:785—789
关键词	RENAL-CELL CARCINOMA IN-VIVO CA-IX BIOLOGICAL EVALUATION TUMOR HYPOXIA POOR-PROGNOSIS BREAST-CANCER EXPRESSION MARKER INHIBITION
ISSN号	0968-0896
DOI	10.1016/j.bmc.2019.01.014
文献子类	期刊论文
英文摘要	Carbonic anhydrase IX (CA IX) is the first carbonic anhydrase found to be associated with cancer that is over expressed in a variety of human solid tumors. As a surrogate marker for hypoxia, the expression of CA IX is strongly upregulated in hypoxic tumors by hypoxia and hypoxia-inducible factor 1a (HIF-1a). In our pursuit of a CA IX-specific PET probe, we designed and synthesized a peptide-based CA IX imaging probe by the efficient click reaction of 1,3-dipolar cycloaddition of terminal alkynes and organic azides. The probe F-18-CA IX-P1-4-10 was obtained with a radiochemical yield of 35-45% (n=5) and radiochemical purity of > 99% in 70-80 min (HPLC purification time included). F-18-CA IX-P1-4-10 had good stability in phosphate buffered saline (PBS), but about 51% peptide degradation was detected in new-born calf serum (NBCS) after incubation. Preliminary microPET/CT experiments demonstrated a specific uptake of F-18-CA IX-P1-4-10 in HT29 tumor and the uptake of F-18-CA IX-P1-4-10 was blocked by peptide CA IX-P1-4-10-Yne pretreatment. Immunohistochemical staining and western blotting studies confirmed the HT29 tumor was CA IX-positive which further proved tumor accumulation of F-18-CA IX-P1-4-10 was correlated with CA IX expression. The results suggest that F-18-CA IX-P1-4-10 is a promising PET tracer for the specific imaging of CA IX-expressing tumors at the molecular level.
语种	英语
内容类型	期刊论文
源URL	[http://ir.sinap.ac.cn/handle/331007/31637]
专题	上海应用物理研究所_中科院上海应用物理研究所2011-2017年
作者单位	1.Chinese Acad Sci, Shanghai Inst Appl Phys, Shanghai 201800, Peoples R China; 2.Fudan Univ, Zhongshan Hosp, Shanghai 200032, Peoples R China 3.Changhai Hosp, Dept Nucl Med, Shanghai 200433, Peoples R China;
推荐引用方式 GB/T 7714	Jia, LN,Li, X,Cheng, DF,et al. Fluorine-18 click radiosynthesis and microPET/CT evaluation of a small peptide-a potential PET probe for carbonic anhydrase IX[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2019,27(5):785—789.
APA	Jia, LN,Li, X,Cheng, DF,&Zhang, L.(2019).Fluorine-18 click radiosynthesis and microPET/CT evaluation of a small peptide-a potential PET probe for carbonic anhydrase IX.BIOORGANIC & MEDICINAL CHEMISTRY,27(5),785—789.
MLA	Jia, LN,et al."Fluorine-18 click radiosynthesis and microPET/CT evaluation of a small peptide-a potential PET probe for carbonic anhydrase IX".BIOORGANIC & MEDICINAL CHEMISTRY 27.5(2019):785—789.