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首页> 外文期刊>Molecular imaging >Noninvasive Detection of Matrix Metalloproteinase Activity In Vivo using a Novel Magnetic Resonance Imaging Contrast Agent with a Solubility Switch
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Noninvasive Detection of Matrix Metalloproteinase Activity In Vivo using a Novel Magnetic Resonance Imaging Contrast Agent with a Solubility Switch

机译：使用具有溶解度开关的新型磁共振成像造影剂体内无创检测基质金属蛋白酶活性

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摘要

We have developed novel proteinase-modulated contrast agents (PCAs) to detect the activity of proteinases in vivo using magnetic resonance imaging. The PCAs are based on the concept of a solubility switch, from hydrophilic to hydrophobic, that significantly modifies the pharmacokinetic properties of the agent as revealed by the slow efflux kinetics from the activity site. Our compound PCA7-switch detects the activity of the secreted matrix-degrading proteinase matrix-metalloproteinase 7 (MMP-7) in living, tumor-bearing mice. Control experiments were performed using an agent that was not cleaved by MMP-7 (PCA7-scrambled), an agent that could be cleaved by MMP-7 but lacked the solubility switch (PCA7-B), and a standard contrast agent (gadolinium-diethylenetriaminepentaacetic acid). PCA7-switch detected a reduction in MMP-7 activity in tumor-bearing mice treated with a synthetic MMP inhibitor, demonstrating its effectiveness in noninvasive functional imaging of proteolytic activity in vivo.
机译：我们已经开发了新型蛋白酶调节的造影剂（PCA），以使用磁共振成像在体内检测蛋白酶的活性。 PCA基于从亲水性到疏水性的溶解度转换的概念，该溶解度转换显着地改变了药剂的药代动力学特性，如从活性位点流出的缓慢动力学所揭示的那样。我们的化合物PCA7开关可在活体荷瘤小鼠中检测分泌的降解基质的蛋白酶基质金属蛋白酶7（MMP-7）的活性。使用未被MMP-7裂解的试剂（PCA7扰乱），可以被MMP-7裂解但缺乏溶解度转换的试剂（PCA7-B）和标准造影剂（ga-二亚乙基三胺五乙酸）。 PCA7开关在用合成MMP抑制剂治疗的荷瘤小鼠中检测到MMP-7活性降低，证明了其在体内蛋白水解活性的非侵入性功能成像中的有效性。

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