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通过马来酰胺酸-半胱氨酸生物共轭实现蛋白质和抗体的高效放射性标记

Efficient Radiolabeling of Proteins and Antibodies via Maleamate-Cysteine Bioconjugation.

作者信息

Mushtaq Sajid, Lee Kyo Chul, Park Ji Ae, Kim Jung Young

机构信息

Division of Applied RI, Korea Institute of Radiological & Medical Sciences, 75 Nowon-ro, Nowon-gu, Seoul 01812, Republic of Korea.

Department of Nuclear Engineering, Pakistan Institute of Engineering and Applied Sciences, P. O. Nilore, Islamabad 45650, Pakistan.

出版信息

ACS Med Chem Lett. 2024 Apr 10;15(5):691-695. doi: 10.1021/acsmedchemlett.4c00092. eCollection 2024 May 9.

Abstract

The study introduces a novel maleamate-based prosthetic group specifically designed for efficient, site-specific radioiodination of biomolecules that contain or are modified with cysteine residues. This strategy is a compelling alternative to the conventional maleimide-based approach, demonstrating outstanding attributes such as high radiochemical yield, rapid reaction kinetics, applicability in aqueous media at neutral pH, and exceptional stability under a competitive environment.

摘要

该研究引入了一种新型的基于马来酰胺酸的 prosthetic 基团,专门设计用于对含有半胱氨酸残基或经半胱氨酸残基修饰的生物分子进行高效、位点特异性的放射性碘化。这种策略是传统基于马来酰亚胺的方法的一个极具吸引力的替代方案,展现出诸如高放射化学产率、快速反应动力学、在中性 pH 水溶液中的适用性以及在竞争环境下的卓越稳定性等突出特性。

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