Design of a Hyperpolarized Molecular Probe for Detection of Aminopeptidase N Activity
Design of a Hyperpolarized Molecular Probe for Detection of Aminopeptidase N Activity
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DOI：
10.1002/anie.201509457
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发表时间：
2016-01-26
影响因子：
16.6
通讯作者：
Sando, Shinsuke
中科院分区：
文献类型：
--
作者：
Hata, Ryunosuke;Nonaka, Hiroshi;Sando, Shinsuke
氨肽酶N（APN）是参与肿瘤血管生成的重要酶。因此，APN活性的检测可以导致肿瘤发展的早期诊断和阐明。虽然已经开发了一些APN的分子探针，但在不透明的生物样品中检测APN活性仍然是一个挑战。为此，我们设计了一种超极化NMR探针[1-C-13] Ala-NH 2，其满足APN检测的先决条件，即，足够的超极化状态的保留，对APN的高反应性，以及APN诱导的化学位移变化。[1-C-13] Ala-NH 2探针允许使用C-13 NMR光谱法灵敏地检测APN活性。
Aminopeptidase N (APN) is an important enzyme that is involved in tumor angiogenesis. Detection of APN activity can thus lead to early diagnosis and elucidation of tumor development. Although some molecular probes for APN have been developed, the detection of APN activity in opaque biological samples remains a challenge. To this end, we designed a hyperpolarized NMR probe [1-C-13]Ala-NH2 which satisfies the prerequisites for APN detection, namely, sufficient retention of the hyperpolarized state, a high reactivity to APN, and an APN-induced chemical shift change. The [1-C-13]Ala-NH2 probe allowed sensitive detection of APN activity using C-13 NMR spectroscopy.