Improved quenched fluorescent probe for imaging of cysteine cathepsin activity.
Improved quenched fluorescent probe for imaging of cysteine cathepsin activity.
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DOI：
10.1021/ja4056068
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发表时间：
2013-10-02
影响因子：
15
通讯作者：
Bogyo M
中科院分区：
文献类型：
--
作者：
Verdoes M;Oresic Bender K;Segal E;van der Linden WA;Syed S;Withana NP;Sanman LE;Bogyo M
半胱氨酸组织蛋白酶是一个蛋白酶家族，在正常细胞生理学和许多人类疾病中发挥重要作用。在癌症中，许多半胱氨酸组织蛋白酶的活性上调，可用于肿瘤成像。在这里，我们展示了一类新型基于猝灭荧光活性的探针（qABP）的设计和合成，其中含有苯氧基甲基酮（PMK）亲电子试剂。与之前报道的 ABP 相比，这些试剂显示出增强的体内特性和广泛的反应性，从而显着改善了标记和肿瘤成像特性。
The cysteine cathepsins are a family of proteases that play important roles in both normal cellular physiology and many human diseases. In cancer, the activity of many of the cysteine cathepsins is upregulated and can be exploited for tumor imaging. Here we present the design and synthesis of a new class of quenched fluorescent activity-based probes (qABPs) containing a phenoxymethyl ketone (PMK) electrophile. These reagents show enhanced in vivo properties and broad reactivity resulting in dramatically improved labeling and tumor imaging properties compared to previously reported ABPs.