自交轴蛋白
医学
体内
小分子
药物发现
计算生物学
临床试验
药理学
生物信息学
生物
内科学
受体
溶血磷脂酸
生物化学
生物技术
作者
Zehui Tan,Hongrui Lei,Ming Guo,Yuxiang Chen,Xin Zhai
标识
DOI:10.1080/13543776.2021.1867106
摘要
The ATX-LPA axis is an attractive target for therapeutic intervention in a variety of diseases, such as tumor metastasis, fibrosis, pruritus, multiple sclerosis, inflammation, autoimmune conditions, metabolic syndrome, and so on. Accordingly, considerable efforts have been devoted to the development of new chemical entities capable of modulating the ATX-LPA axis.This review aims to provide an overview of novel ATX inhibitors reported in patents from September 2016 to August 2020, discussing their structural characteristics and inhibitory potency in vitro and in vivo.In the past four years, the classification of ATX inhibitors based on binding modes has brought great benefits to the discovery of more efficacious inhibitors. In addition to GLPG1690 currently in phase III clinical studies for IPF, BBT-877, and BLD-0409 as potent ATX inhibitors have been enrolled in phase I clinical evaluation; meanwhile, many effective molecules were also reported successively. However, most emerging ATX inhibitors in the last four years are closely analogs of previous entities, such as GLPG1690 and PF-8380, which translate into the urgently identification of ATX inhibitors with diverse structural features and promising properties in the near future.
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