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发现并确定EIF2AK2作为柏柏林抗炎作用的直接关键点

Wei Wei¹, Qingxuan Zeng¹, Yan Wang¹

¹Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.

Acta pharmaceutica Sinica. B

|May 30, 2023

概括

柏柏林 (BBR) 通过向EIF2AK2,这是一种调节炎症通路的关键蛋白质,具有抗炎作用. 抑制EIF2AK2二分化为与炎症相关的疾病提供了潜在的治疗策略.

科学领域:

生物化学生物化学
分子生物学分子生物学
药理学药理学是指药理学的学科.

背景情况:

柏柏林 (BBR) 是一种具有已知的抗炎性质的天然化合物.
在BBR的抗炎作用的基础上,精确的分子标和机制需要进一步阐明.

研究的目的:

为了确定BBR的直接分子点,负责其抗炎作用.
调查EIF2AK2在调解BBR抗炎作用中的作用.
探索针对EIF2AK2二分化作为治疗策略的潜力.

主要方法:

化学蛋白质技术被用来识别BBR目标.
分析了BBR和EIF2AK2之间的结合亲和力和相互作用模式.
研究了EIF2AK2二分化抑制和下游途径调节 (JNK,NF-κB,AKT,NLRP3).研究了EIF2AK2二分化抑制和下游途径调节.
在小鼠中使用EIF2AK2基因敲除来验证该机制.

主要成果:

确定了EIF2AK2,eEF1A1,PRDX3和VPS4B作为直接的BBR目标.
BBR通过离子键对EIF2AK2表现出最强的亲和力,调节炎症途径.
BBR选择性地抑制了EIF2AK2的二分化,而不是其酶活性,调节JNK,NF-κB,AKT和NLRP3.
EIF2AK2敲击减弱了BBR对IL-1β,IL-6,IL-18和TNF-α分泌的抑制作用.

结论:

EIF2AK2是BBR抗炎作用的关键调解者.
准EIF2AK2二分化是一种有前途的治疗方法,用于管理与炎症相关的疾病.
BBR的机制涉及通过EIF2AK2.2.通过炎症途径的网络调节.

关键词:

抗炎药物抗炎药物抗炎药物柏柏林蛋白是一种柏柏林蛋白.化学蛋白质技术是化学蛋白质的技术.EIF2AK2AK2 是一个国际金融基金.照片亲和力探测器探测器目标识别目标识别

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