Radioiodination of Pimonidazole as a Novel Theranostic Hypoxia Probe

Makaleler > Tam Makale · 2020

Yazarlar: Ilknur Demir Inci, Volkan Tekin, Ayfer YURT KILÇAR, Özge KOZGUŞ GÜLDÜ, Emin İlker MEDİNE, Kadriye Busra Karatay, Emine Dervis, Fazilet Zümrüt BİBER MÜFTÜLER

Current Radiopharmaceuticals, SCI Expanded İndekslerine Giren Dergi, Uluslararası, Scopus, 2020, cilt 14, ss 46-50

DOI: 10.2174/1874471013666200331114908

Özet

BACKGROUND: Tumors are defined as abnormal tissue masses, and one of the most important factors leading to the growth of these abnormal tissue masses is Vascular Endothelial Growth Factor, which stimulates angiogenesis by releasing cells under hypoxic conditions. Hypoxia has a vital role in cancer therapy, thus it is important to monitor hypoxia. The hypoxia marker Pimonidazole (PIM) is a candidate biomarker of cancer aggressiveness. OBJECTIVE: I) to join a theranostic approach. For this purpose, PIM was derived as PIM-TOS to be able to be radioiodinated. METHODS: PIM was derived via a tosylation reaction. Derivatization product (PIM-TOS) was radioiodinated by using iodogen method and was analyzed by High-Performance Liquid Chromatography and Liquid chromatography-mass spectrometry. Thin layer radiochromatography was utilized for its quality control studies. RESULTS: PIM was derived successfully after the tosylation reaction. The radioiodination yield of PIM-TOS was over 85%. CONCLUSION: I, as a potential theranostic hypoxia agent was investigated. Further experimental studies should be performed for developing a novel hypoxia probe including theranostics approaches.

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