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KMID : 1145520190050010036
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Journal of Radiopharmaceuticals and Molecular Probes
2019 Volume.5 No. 1 p.36 ~ p.47
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1-Benzyl indazole derivative-based 18F-labeled PET radiotracer: Radiosynthesis and cell uptake study in cancer cells
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More Kunal N.
Lee Jun-Young
Park Jeong-Hoon
Chang Dong-Jo
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Abstract
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Hypoxia-inducible factor-1 (HIF-1α) is a transcription factor activated in response to low oxygen level, and is highly expressed in many solid tumors. Moreover, HIF-1α is a representative biomarker of hypoxia and also helps to maintain cell homeostasis under hypoxic condition. Most solid tumors show hypoxia, which induces poor prognosis and resistance to conventional cancer therapies. Thus, early diagnosis of hypoxia with positron emission tomography (PET) radiotracer would be highly beneficial for management of malignant solid tumors with effective cancer therapy. YC-1 is a most promising candidate among several HIF-1α inhibitors. As an effort to develop a hypoxia imaging tool as a PET radiotracer, we designed and synthesized [18F]DFYC based on potent derivative of YC-1 and performed preliminary in vitro cell uptake study. [18F]DFYC showed a significant accumulation in SKBR-3 cells among other cancer cells, proving as a good lead to develop a hypoxic solid tumor such as breast cancer.
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KEYWORD
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Hypoxia, HIF-1α inhibitors, YC-1, Positron emission tomography, [18F]DFYC
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