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首页> 外文期刊>Applied radiation and isotopes: including data, instrumentation and methods for use in agriculture, industry and medicine >t-Butyloxycarbonyl: an ordinary but promising group for protecting peptides from deiodination.
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t-Butyloxycarbonyl: an ordinary but promising group for protecting peptides from deiodination.

机译：叔丁氧羰基：一个普通但有希望的基团，用于保护肽免受碘化。

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摘要

In order to protect directly radioiodinated peptides from in vivo deiodination, a novel procedure was explored. Two peptides, Try-Gly-Gly-Gly-Gly-Gly-Cys-Asn-Gly-Arg-Cys (YG5) and t-Boc-Try-Gly-Gly-Gly-Gly-Gly-Cys-Asn-Gly-Arg-Cys (t-BOC-YG5) were synthesized and radiolabeled. A paired-label biodistribution study using [131I]t-BOC-YG5 and [125I]YG5 was undertaken in normal mice. Compared to [125I]YG5, [131I]t-BOC-YG5 was quite resistant to in vivo deiodination, resulting in rapid reduction of the radioactive background and negligible radioactivity accumulation in both thyroid and stomach. [131I]t-BOC-YG5 was also stable in human serum even after 24 h. In conclusion, the t-BOC group has the potential to protect peptide from deiodination.
机译：为了保护直接放射性碘标记的肽免于体内脱碘，探索了一种新的方法。两种肽，Try-Gly-Gly-Gly-Gly-Cys-Asn-Gly-Arg-Cys（YG5）和t-Boc-Try-Gly-Gly-Gly-Gly-Gly-Cys-Asn-Gly-合成了Arg-Cys（t-BOC-YG5）并进行了放射性标记。在正常小鼠中进行了使用[131I] t-BOC-YG5和[125I] YG5的配对标记生物分布研究。与[125I] YG5相比，[131I] t-BOC-YG5对体内的碘化反应具有相当的抵抗力，从而导致放射本底的迅速降低和在甲状腺和胃中的放射性累积可忽略不计。即使在24小时后，[131I] t-BOC-YG5在人血清中也稳定。总之，t-BOC基团具有保护肽免受脱碘作用的潜力。

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