Direct radio-iodination of folic acid for targeting folate receptor-positive tumors
Huynh Phuong Tu, 이웅희, 하영수, 유정수,
소속 상세정보
( Huynh Phuong Tu )
Kyungpook National University School of Medicine Department of Molecular Medicine
이웅희 ( Lee Woong-Hee )
Kyungpook National University School of Medicine Department of Molecular Medicine
하영수 ( Ha Yeong-Su )
Kyungpook National University School of Medicine Department of Molecular Medicine
유정수 ( Yoo Jeong-Soo )
Kyungpook National University School of Medicine Department of Molecular Medicine
Abstract
The folate receptor (FR) is a promising cell membrane-associated target for nuclear imaging of various cancers (via imaging FR-α) and potentially also inflammatory diseases (via imaging FR-β), through the use of folic acid-based radioconjugates. However, there have been several drawbacks of previously reported radioconjugates, such as a short half-life of the radiolabel (68Ga t1/2 68 min), a complex and time-consuming multistep radiosynthesis, and a high renal uptake of radiolabeled folate derivatives. The goal of this study was to develop an imaging probe by directly labeling folate with radioactive iodine without using an extra prosthetic group. The radiolabeling of folate was optimized using various labeling conditions and the labeled tracers were isolated by high-performance liquid chromatography. The in vitro stability of labeled folate was checked in phosphate-buffered saline and serum. The tumor-targeting efficacy of the probe was also evaluated by biodistribution studies using a murine 4T1 tumor model.
키워드
Folic acid; radioiodination; tumor targeting
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