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1篇 您的检索式:作者名="Yuanyuan Houn"
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1Glycyrrhetinic acid binds to the conserved P-loop region and interferes with the interaction of RAS-effector proteins显示文摘Members of the RAS proto-oncogene superfamily are indispensable molecular switches that play critical roles in cell proliferation, differentiation, and cell survival. Recent studies have attempted to prevent the interaction of RAS/GTP with RAS guanine nucleotide exchange factors(GEFs), impair RASeffector interactions, and suppress RAS localization to prevent oncogenic signalling. The present study aimed to investigate the effect of the natural triterpenoic acid inhibitor glycyrrhetinic acid, which is isolated from the roots of Glycyrrhiza plant species, on RAS stability. We found that glycyrrhetinic acid may bind to the P-loop of RAS and alter its stability. Based on our biochemical tests and structural analysis results, glycyrrhetinic acid induced a conformational change in RAS. Meanwhile, glycyrrhetinic acid abolishes the function of RAS by interfering with the effector protein RAF kinase activation and RAS/MAPK signalling.Yuan Zhang Zhihua Wang Xiaoyao Ma Shengnan Yang Xueyan Hu Jin Tao Yuanyuan Houn Gang Bai 2019Acta Pharmaceutica Sinica B2019,9,2:7
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