一种来源于海绵真菌 581F1 的新型脯氨酰内肽酶（GLP-1R）和真核延伸因子 2 激酶（eEF2K）亲和性的新型索马菌素衍生物。
New sorbicillinoid derivatives with GLP-1R and eEF2K affinities from a sponge-derived fungus 581F1.
机构信息
Research Center for Marine Drugs, State Key Laboratory of Oncogenes and Related Genes, Department of Pharmacy, Renji Hospital, School of Medicine, Shanghai Jiao Tong University, Shanghai, China.
State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, and Collaborative Innovation Center of Biotherapy, Sichuan University, Chengdu, China.
出版信息
Nat Prod Res. 2020 Oct;34(20):2880-2886. doi: 10.1080/14786419.2019.1596099. Epub 2019 Apr 16.
Two new sorbicillinoids, 13-hydroxy-dihydrotrichodermolide () and 10,11,27,28-tetrahydrotrisorbicillinone C (), were isolated from the sponge-derived fungus 581F1. Their structures were determined on the basis of spectroscopic analysis. Compounds and displayed high affinities to target proteins GLP-1R (diabetes) and eEF2K (cancer) with K values of 0.0285 μM, 0.0162 μM for GLP-1R and 0.118 μM, 0.0746 μM for eEF2K, respectively.
两种新的索比菌素，13-羟基二氢曲霉菌内酯（）和 10,11,27,28-四氢三索比菌素 C（），从海绵来源的真菌 581F1 中分离得到。基于光谱分析确定了它们的结构。化合物和对 GLP-1R（糖尿病）和 eEF2K（癌症）靶蛋白具有高亲和力，K 值分别为 0.0285μM 和 0.0162μM，0.118μM 和 0.0746μM。
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