The p38 MAPK Inhibitors and Their Role in Inflammatory Diseases

被引：28
作者：
Machado, Thamires R. [1 ]
Machado, Thayna R. [2 ]
Pascutti, Pedro G. [1 ]
机构：
[1] Fed Univ Rio De Janeiro UFRJ, Carlos Chagas Filho Inst Biophys, Lab Mol Modeling & Dynam, CCS, Cidade Univ, BR-21941590 Rio De Janeiro, RJ, Brazil
[2] Fed Univ Rio De Janeiro UFRJ, Fac Pharm, Lab Mol Modeling & QSAR ModMolQSAR, Rio De Janeiro, Brazil
来源：
CHEMISTRYSELECT | 2021年 / 6卷 / 23期
关键词：
drug design; inflammation; mitogen-activated protein kinase; p38 MAPK inhibition; protein structures; KINASE INHIBITORS; CARDIOVASCULAR OUTCOMES; BIOLOGICAL EVALUATION; P38-ALPHA; BINDING; DESIGN; SELECTIVITY;
D O I：
10.1002/slct.202100406
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
The p38 family is a highly evolutionarily conserved group of mitogen-activated protein kinases (MAPKs) that is involved in and helps co-ordinate cellular responses to nearly all stressful stimuli. Four isoforms of the p38 MAPK family (alpha, beta, gamma, delta) have been identified. p38 alpha is activated by many inflammatory stimuli, and it plays a key role in regulating the biosynthesis of proinflammatory cytokines like interleukin 1 beta (IL-1 beta) and tumor necrosis factor alpha (TNF alpha). For this reason, p38 MAPK is an important target to be studied for the treatment of chronic airway inflammatory diseases, rheumatoid arthritis, inflammatory bowel disease, Alzheimer's disease, atherosclerosis, COVID-19 and acute coronary syndrome. The characteristics of p38 MAPK, the different modes of inhibition, and its involvement in inflammatory diseases are summarized in this review. We then discuss the p38 MAPK inhibitors that have been used in the in vitro systems as well as in the clinical trials.
引用
收藏
页码：5729 / 5742
页数：14
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