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furin 抑制剂治疗应用的开发与前景。

Development and Prospects of Furin Inhibitors for Therapeutic Applications.

机构信息

ChemDiv Inc., San Diego, CA 92130, USA.

出版信息

Int J Mol Sci. 2024 Aug 24;25(17):9199. doi: 10.3390/ijms25179199.

DOI:10.3390/ijms25179199
PMID:39273149
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11394684/
Abstract

Furin, a serine protease enzyme located in the Golgi apparatus of animal cells, plays a crucial role in cleaving precursor proteins into their mature, active forms. It is ubiquitously expressed across various tissues, including the brain, lungs, gastrointestinal tract, liver, pancreas, and reproductive organs. Since its discovery in 1990, furin has been recognized as a significant therapeutic target, leading to the active development of furin inhibitors for potential use in antiviral, antibacterial, anticancer, and other therapeutic applications. This review provides a comprehensive overview of the progress in the development and characterization of furin inhibitors, encompassing peptides, linear and macrocyclic peptidomimetics, and non-peptide compounds, highlighting their potential in the treatment of both infectious and non-infectious diseases.

摘要

弗林蛋白酶，一种位于动物细胞高尔基体中的丝氨酸蛋白酶，在将前体蛋白切割成成熟、有活性的形式方面起着关键作用。它在各种组织中广泛表达，包括脑、肺、胃肠道、肝、胰腺和生殖器官。自 1990 年发现以来，弗林蛋白酶已被认为是一个重要的治疗靶点，导致弗林蛋白酶抑制剂的积极开发，潜在用于抗病毒、抗菌、抗癌和其他治疗应用。本综述全面概述了弗林蛋白酶抑制剂的开发和表征方面的进展，包括肽、线性和大环肽模拟物以及非肽化合物，强调了它们在治疗感染性和非传染性疾病方面的潜力。

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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4cce/11394684/c75947235993/ijms-25-09199-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4cce/11394684/e5dfaf692bd2/ijms-25-09199-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4cce/11394684/4d7da1f24cc1/ijms-25-09199-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4cce/11394684/d7f0823b3c41/ijms-25-09199-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4cce/11394684/ff3fa4b81295/ijms-25-09199-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4cce/11394684/5b27e20c861c/ijms-25-09199-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4cce/11394684/21abea44d4c9/ijms-25-09199-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4cce/11394684/2816578c7bc5/ijms-25-09199-g012.jpg

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