来自……的蛋白质酪氨酸磷酸酶的治疗靶向作用
Therapeutic Targeting of Protein Tyrosine Phosphatases from .
作者信息
Ruddraraju Kasi Viswanatharaju, Aggarwal Devesh, Zhang Zhong-Yin
机构信息
Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN 47907, USA.
Department of Chemistry, Purdue University, West Lafayette, IN 47907, USA.
出版信息
Microorganisms. 2020 Dec 23;9(1):14. doi: 10.3390/microorganisms9010014.
Tuberculosis (TB) is an airborne infectious disease caused by (Mtb). According to the World Health Organization, an estimated 10 million people developed TB in 2018. The occurrence of drug-resistant TB demands therapeutic agents with novel mechanisms of action. Antivirulence is an alternative strategy that targets bacterial virulence factors instead of central growth pathways to treat disease. protein tyrosine phosphatases, mPTPA and mPTPB, are secreted by Mtb into the cytoplasm of macrophages and are required for survival and growth of infection within the host. Here we present recent advances in understanding the roles of mPTPA and mPTPB in the pathogenesis of TB. We also focus on potent, selective, and well-characterized small molecule inhibitors reported in the last decade for mPTPA and mPTPB.
结核病（TB）是由结核分枝杆菌（Mtb）引起的一种空气传播的传染病。根据世界卫生组织的数据，2018年估计有1000万人患上了结核病。耐药结核病的出现需要具有新型作用机制的治疗药物。抗毒力是一种替代策略，它针对细菌毒力因子而非核心生长途径来治疗疾病。结核分枝杆菌分泌的蛋白酪氨酸磷酸酶mPTPA和mPTPB进入巨噬细胞的细胞质，是宿主内感染存活和生长所必需的。在这里，我们介绍了在理解mPTPA和mPTPB在结核病发病机制中的作用方面的最新进展。我们还重点关注了过去十年中报道的针对mPTPA和mPTPB的强效、选择性且特征明确的小分子抑制剂。
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