Aminopeptidase N as a potential drug target

O. Farsa, Veronika Ballayová, Radka Žáčková, P. Zubáč
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Abstract

Aminopeptidase N (APN) is a broad specificity zinc metallopeptidase with many functions that do not always depend on its enzymatic activity. Among others, it is involved in tumor angiogenesis and metastasizing and also serves as a cellular receptor of some coronaviruses. Some APN inhibitors, such as bestatin or tosedostat, were used or tested as anticancer drugs in the past. Within the past two decades, we have prepared several series of potential APN inhibitors. Some of them reached interesting values of inhibitory activity and were also successfully tested for antiproliferation activity in cancer cell lines. We also performed some QSAR studies with APN inhibitors prepared by us and other authors.
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作为潜在药物靶点的氨基肽酶 N
氨基肽酶 N(APN)是一种特异性很强的锌金属肽酶,具有许多并不总是取决于其酶活性的功能。除其他外,它参与肿瘤血管生成和转移,也是某些冠状病毒的细胞受体。过去,一些 APN 抑制剂,如 bestatin 或 tosedostat,曾被用作或测试用作抗癌药物。在过去二十年中,我们制备了多个潜在的 APN 抑制剂系列。其中一些抑制剂的抑制活性达到了令人感兴趣的数值,并成功地在癌细胞系中进行了抗增殖活性测试。我们还对自己和其他作者制备的 APN 抑制剂进行了一些 QSAR 研究。
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来源期刊
European Pharmaceutical Journal
European Pharmaceutical Journal Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (all)
CiteScore
0.60
自引率
0.00%
发文量
16
期刊介绍: European Pharmaceutical Journal publishes only original articles not previously published and articles that are not being considered or have not been submitted for publication elsewhere. If parts of the results have been published as conference abstract or elsewhere, it should be stated in references. The ethical standards of the Helsinki-Tokio Declaration should be kept. This should be mentioned in the Methods of manuscript. Reviews are published only on request. Authors, whose submitted research work was performed with the support of a company, should indicate this in Conflict of Interest.
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