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组织蛋白酶 C 抑制剂作为抗炎药物研发:挑战与机遇。

Cathepsin C inhibitors as anti-inflammatory drug discovery: Challenges and opportunities.

机构信息

Engineering Research Center of Biomass Conversion and Pollution Prevention of Anhui Educational Institutions, Fuyang Normal University, Fuyang, 236037, PR China.

School of Pharmacy, Anhui Medical University, Hefei, 230032, China.

出版信息

Eur J Med Chem. 2021 Dec 5;225:113818. doi: 10.1016/j.ejmech.2021.113818. Epub 2021 Sep 3.

Abstract

Cathepsin C, an important lysosomal cysteine protease, mediates the maturation process of neutrophil serine proteases, and participates in the inflammation and immune regulation process associated with polymorphonuclear neutrophils. Therefore, cathepsin C is considered to be an attractive target for treating inflammatory diseases. With INS1007 (trade name: brensocatib) being granted a breakthrough drug designation by FDA for the treatment of Adult Non-cystic Fibrosis Bronchiectasis and Coronavirus Disease 2019, the development of cathepsin C inhibitor will attract attentions from medicinal chemists in the future soon. Here, we summarized the research results of cathepsin C as a therapeutic target, focusing on the development of cathepsin C inhibitor, and provided guidance and reference opinions for the upcoming development boom of cathepsin C inhibitor.

摘要

组织蛋白酶 C 是一种重要的溶酶体半胱氨酸蛋白酶,介导中性粒细胞丝氨酸蛋白酶的成熟过程,并参与与多形核白细胞相关的炎症和免疫调节过程。因此,组织蛋白酶 C 被认为是治疗炎症性疾病的一个有吸引力的靶点。随着 INS1007(商品名:brensocatib)被 FDA 授予突破性药物指定用于治疗成人非囊性纤维化支气管扩张症和 2019 年冠状病毒病,组织蛋白酶 C 抑制剂的开发将很快引起药物化学家的关注。在这里,我们总结了组织蛋白酶 C 作为治疗靶点的研究结果,重点介绍了组织蛋白酶 C 抑制剂的开发,并为即将到来的组织蛋白酶 C 抑制剂开发热潮提供了指导和参考意见。

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