Red fluorescent scaffold for highly sensitive protease activity probes

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• 作者：Yu Kushida ; Kenjiro Hanaoka ; Toru Komatsu ; Takuya Terai ; Tasuku Ueno ; Kengo Yoshida ; Masanobu Uchiyama ; Tetsuo Nagano ; ^{tlong@mol.f.u-tokyo.ac.jp}
• 关键词：Fluorescent probes ; Enzymes ; Proteases
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 June, 2012
• 卷：22
• 期：12
• 页码：3908-3911
• 文件大小：539 K

摘要

We have developed a novel red fluorescent dye, 2Me SiR600 (位_em = 613 nm), in which the O atom of Rhodamine Green at the 10 position of the xanthene moiety is replaced with a Si atom, as a scaffold for probes to detect protease activity with extremely high S/N ratio. As proof of concept, we designed and synthesized probes for caspase-3 activity (Z-DEVD-SiR600) and leucine aminopeptidase activity (Leu-SiR600). Caspase-3-mediated cleavage of Z-DEVD-SiR600 resulted in a large bathochromic shift (93 nm) of the absorption maximum and a 432-fold fluorescence enhancement.