Abstract

Psoriasis therapy remains an extremely relevant area of modern drug design, due to necessity of adverse reaction reduction, inherent for actual methods of therapy. It was established that two serine proteases—neutrophil elastase 1 (HNE1) and cathepsin G (CatG)—are the key agents in psoriasis development. The collected molecular data for the presented targets form the basis for the molecular modeling strategy for the search for and identification of new target-specific inhibitors. The result of this work is a group of high-priority small-molecule compounds with double-targeted affinity, which are able to suppress the pro-psoriatic processes induced by the considered serine proteases at the initial stage of the disease.

中文翻译：

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嗜中性粒细胞弹性蛋白酶和组织蛋白酶G的抑制作为治疗牛皮癣的一种新方法：从基础生物学到开发新的针对特定目标的药物。

摘要

由于减少实际治疗方法固有的不良反应，牛皮癣治疗仍然是现代药物设计中极为重要的领域。已确定两种丝氨酸蛋白酶-中性粒细胞弹性蛋白酶1（HNE1）和组织蛋白酶G（CatG）-是牛皮癣发展的关键因素。为提出的靶标收集的分子数据构成了分子建模策略的基础，该策略用于寻找和鉴定新的靶标特异性抑制剂。这项工作的结果是一组具有双重目标亲和力的高优先级小分子化合物，它们能够在疾病初期抑制由考虑的丝氨酸蛋白酶诱导的促银屑病过程。