Förster resonance energy transfer reveals phillygenin and swertiamarin concurrently target AKT on different binding domains to increase the anti-inflammatory effect
作者机构：State Key Laboratory of Medicinal Chemical BiologyCollege of Pharmacy and Tianjin Key Laboratory of Molecular Drug ResearchNankai UniversityTianjin 300000China College of Life HealthDalian UniversityDalian 116622China Dalian Fusheng Pharmaceutical Co.Ltd.Dalian 116000China
出 版 物：《Chinese Chemical Letters》 (中国化学快报（英文版）)
年 卷 期：2024年第35卷第5期
页 面：207-212页
核心收录：
学科分类：1007[医学-药学(可授医学、理学学位)] 0703[理学-化学] 10[医学]
基 金：supported by the National Natural Science Foundation of China(No.81973449)
主 题：FRET Swertiamarin Phillygenin AKT Anti-inflammation Combinatorial drug
摘 要：The clinical benefit of combination therapy is significant,but it is not easy to define the mechanism of complexity and *** studies illustrate that phillygenin(Phi)binds in the allosteric inhibit pocket of protein kinase B(AKT),and swertiamarin(Swe)acts on the pleckstrin homology(PH)domain of ***,the combined synergistic effect of relieving the inflammatory response has yet to be *** on high sensitivity,specificity and fast-responsibility fluorescent sensors,the Förster resonance energy transfer(FRET)technique offers a route to provide clear insights into physiological and pathological *** the study,molecular docking,the fluorescent probes of Phi and Swe for FRET were designed and *** analysis shown that Swe and Phi concurrently acted on the PH domain and allosterically inhibited pocket of AKT,*** combination of Swe and Phi significantly increased the heat stability of AKT and decreased protease-induced *** lipopolysaccharides(LPS)-induced mice and cells,the combination arrested AKT activation,nuclear factor kappa-B(NF-κB)phosphorylation,and the expression of tumor necrosis factor-α(TNF-α),interleukin(IL)-6 and *** conclusion,FRET revealed Phi and Swe concurrently targeted AKT on different domains and the combination of Phi and Swe enhanced the anti-inflammatory effect.
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