首页|初探氨来咕诺抑制TBK1活性与其临床副作用的关系

初探氨来咕诺抑制TBK1活性与其临床副作用的关系

扫码查看
目的 以消炎药氨来呫诺为例,对该类海洋盐单胞菌代谢产物的结构类似物抑制TBK1活性对天然免疫的影响及与临床副作用的潜在关联进行研究.方法 运用分子生物学和病毒学手段,在细胞和动物模型中,评估氨来呫诺对病原体感染及相关炎症通路的影响.结果 氨来呫诺及其类似物是潜在的TBK1抑制剂;氨来呫诺不显著抑制机体对病原体刺激的应答以氨来呫诺为代表的三环胺类结构化合物抑制TBK1(TANK-binding kinase 1)活性可能不直接导致感染概率上升.
Preliminary exploring of the relationship between the inhibition of TBK1 by amelexanox and its clinical side impact
Objective Taking the anti-inflammatory drug amlexanox as an example,the effect of the structural analog of this kind of marine halomonas metabolites inhibiting TBK1 activity on natural immunity and the potential relationship with clinical side effects were studied.Methods The effects of amlexanox on pathogenic infections and associated inflammatory pathways were evaluated in cell and animal models utilizing molecular biology and virology.Results Amlexanox and its analogues marine Halomonas sp.metabolites were potent inhibitors of TBK1.Amlexanox did not significantly inhibit the immune responses to pathogen stimuli.Tricyclic amine structural compounds represented by amlexanox inhibited TBK1(TANK-binding kinase 1)activity and probably did not directly increase infection probability.

amlexanoxmarine compoundmarine Halomonas sp.TBK1safety pharmacology

翟晓晨、张梅芳、武娟、杜凯欣、王鑫

展开 >

中国海洋大学海洋药物教育部重点实验室,医药学院,山东青岛 266003

青岛海洋生物医药研究院海洋创新药物药筛选与评价中心,山东青岛 266100

氨来呫诺 海洋化合物 海洋Halomonas sp. TBK1 安全药理学研究

2024

中国海洋药物
中国药学会

中国海洋药物

CSTPCD
影响因子:0.539
ISSN:1002-3461
年,卷(期):2024.43(4)