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Molecular Imaging of Proteases in Cancer

机译:癌症中蛋白酶的分子成像

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Proteases play important roles during tumor angiogenesis, invasion, and metastasis. Various molecular imaging techniques have been employed for protease imaging: optical (both fluorescence and bioluminescence), magnetic resonance imaging (MRI), single-photon emission computed tomography (SPECT), and positron emission tomography (PET). In this review, we will summarize the current status of imaging proteases in cancer with these techniques. Optical imaging of proteases, in particular with fluorescence, is the most intensively validated and many of the imaging probes are already commercially available. It is generally agreed that the use of activatable probes is the most accurate and appropriate means for measuring protease activity. Molecular imaging of proteases with other techniques (i.e. MRI, SPECT, and PET) has not been well-documented in the literature which certainly deserves much future effort. Optical imaging and molecular MRI of protease activity has very limited potential for clinical investigation. PET/SPECT imaging is suitable for clinical investigation; however the optimal probes for PET/SPECT imaging of proteases in cancer have yet to be developed. Successful development of protease imaging probes with optimal in vivo stability, tumor targeting efficacy, and desirable pharmacokinetics for clinical translation will eventually improve cancer patient management. Not limited to cancer, these protease-targeted imaging probes will also have broad applications in other diseases such as arthritis, atherosclerosis, and myocardial infarction.
机译:蛋白酶在肿瘤血管生成,侵袭和转移中起重要作用。各种分子成像技术已用于蛋白酶成像:光学(荧光和生物发光),磁共振成像(MRI),单光子发射计算机断层扫描(SPECT)和正电子发射断层扫描(PET)。在这篇综述中,我们将总结使用这些技术的成像蛋白酶在癌症中的现状。蛋白酶的光学成像,尤其是荧光成像,得到了最深入的验证,许多成像探针已经可以在市场上买到。一般认为,使用可活化探针是测量蛋白酶活性的最准确和最合适的方法。使用其他技术(例如MRI,SPECT和PET)对蛋白酶进行的分子成像尚未在文献中得到充分记录,这无疑值得未来的努力。蛋白酶活性的光学成像和分子MRI在临床研究中的潜力非常有限。 PET / SPECT成像适合临床研究;然而,尚未开发出用于癌症中蛋白酶的PET / SPECT成像的最佳探针。具有最佳体内稳定性,肿瘤靶向功效和临床翻译所需药代动力学的蛋白酶成像探针的成功开发将最终改善癌症患者的管理。这些靶向蛋白酶的成像探针不仅限于癌症,还将在其他疾病(例如关节炎,动脉粥样硬化和心肌梗塞)中具有广泛的应用。

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