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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
2019
Source PublicationBIOORGANIC & MEDICINAL CHEMISTRY
ISSN0968-0896
Volume27Issue:5Pages:785—789
Subtype期刊论文
AbstractCarbonic 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.
KeywordRENAL-CELL CARCINOMA IN-VIVO CA-IX BIOLOGICAL EVALUATION TUMOR HYPOXIA POOR-PROGNOSIS BREAST-CANCER EXPRESSION MARKER INHIBITION
DOI10.1016/j.bmc.2019.01.014
Indexed BySCI
Language英语
Citation statistics
Document Type期刊论文
Identifierhttp://ir.sinap.ac.cn/handle/331007/31637
Collection中科院上海应用物理研究所2011-2020年
Affiliation1.Chinese Acad Sci, Shanghai Inst Appl Phys, Shanghai 201800, Peoples R China;
2.Changhai Hosp, Dept Nucl Med, Shanghai 200433, Peoples R China;
3.Fudan Univ, Zhongshan Hosp, Shanghai 200032, Peoples R China
Recommended Citation
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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.
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