摘要
Hepsin是一种在细胞生长发育中发挥关键作用的II型跨膜丝氨酸蛋白酶(TTSP)。 Hepin在前列腺癌(PCa)中高度表达,与其进展和转移相关。因此,它被认为是PCa的有吸引力的生物标志物。近来,已经开发了针对hepsin的低分子量抑制剂。基于关键的化学支架,它们可以分为四类:吲哚甲酰胺,苯甲酰胺,基于肽的类似物和2,3-二氢-1H-伴侣二胺。在这次审查中,我们讨论了四种类型的蛋白酶抑制剂的设计策略,结构 - 活性关系(SAR)和结合模式
关键词: Hepsin,前列腺癌,II型跨膜丝氨酸蛋白酶,结构活性关系(SAR),脒,肽。
Current Medicinal Chemistry
Title:Recent Advances of Hepsin-Targeted Inhibitors
Volume: 24 Issue: 21
关键词: Hepsin,前列腺癌,II型跨膜丝氨酸蛋白酶,结构活性关系(SAR),脒,肽。
摘要: Hepsin is a type II transmembrane serine protease (TTSP) that plays a crucial role in cell growth and development. Hepsin is highly expressed in prostate cancer (PCa) and associated with its progression and metastasis. Therefore, it has been considered as an attractive biomarker of PCa. Recently, low molecular weight inhibitors targeting hepsin have been developed. Based on the key chemical scaffold, they can be classified into four classes: Indolecarboxamidines, benzamidines, peptide-based analogs, and 2,3-dihydro- 1H-perimidines. In this review, we discuss design strategy, structure-activity relationship (SAR), and binding mode of the four classes of hepsin inhibitors.
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Recent Advances of Hepsin-Targeted Inhibitors, Current Medicinal Chemistry 2017; 24 (21) . https://dx.doi.org/10.2174/0929867324666170227115835
DOI https://dx.doi.org/10.2174/0929867324666170227115835 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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