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Natural Product Albiziabioside A Conjugated with Pyruvate Dehydrogenase Kinase Inhibitor Dichloroacetate To Induce Apoptosis-Ferroptosis-M2-TAMs Polarization for Combined Cancer Therapy

文献类型：期刊论文

作者Wei, Gaofei3,4; Sung, Jiahong2; Luan, Weijing1,3; Hou, Zhuang3; Wang, Shuai3; Cui, Shanshan3; Cheng, Maosheng3; Liu, Yang3
刊名JOURNAL OF MEDICINAL CHEMISTRY
出版日期2019-10-10
卷号62期号:19页码:8760-8772
ISSN号0022-2623
DOI10.1021/acs.jmedchem.9b00644
通讯作者Wei, Gaofei(weigf0605@163.com) ; Cheng, Maosheng(mscheng@syphu.edu.cn) ; Liu, Yang(y.liu@syphu.edu.cn)
英文摘要The reprogramming of energy metabolism is considered to be one of the main characteristics of cancer. The development of therapeutic agents targeting glycolysis to alter aberrant glucose metabolism and restore oxidative phosphorylation has emerged as an effective approach for cancer therapy. In this way, we have developed a conjugate AlbA-DCA, which can induce a marked increase in intracellular ROS and alleviate the accumulation of lactic acid in TME. Meanwhile, AlbA-DCA selectively kills cancer cells and exhibits an excellent synergistic effect. Mechanism studies confirm that AlbA-DCA can induce apoptosis and ferroptosis. We also confirm that AlbA-DCA can remold the tumor immunosuppression microenvironment via eliminating M2-TAMs to inhibit both primary and distal tumor progression in a dual-4T1 tumor model in female BALB/c mice. As a result, rational design of natural saponin and PDK inhibitor to induce apoptosis-ferroptosis-M2-TAMs polarization for enhanced cancer therapy is a promising strategy, thus providing a new idea for cancer therapy.
WOS关键词TUMOR-ASSOCIATED MACROPHAGES ; LACTIC-ACID ; FERROPTOSIS ; APOPTOSIS ; DERIVATIVES ; DYSFUNCTION ; METABOLISM ; REVERSAL ; CELLS ; IRON
资助项目National Natural Science Foundation of China[81703335] ; National Natural Science Foundation of China[81703599] ; National Natural Science Foundation of China[81473087] ; Natural Science Foundation of Guangdong[2017A030313069] ; Medical Research Foundation of Guangdong[A2017114] ; Program for Liaoning Innovative Talents in University[LR2017043] ; Career Development Support Plan for Young and Middleaged Teachers in Shenyang Pharmaceutical University[ZQN2016005]
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000490355000006
出版者AMER CHEMICAL SOC
源URL[http://119.78.100.183/handle/2S10ELR8/282590]  
专题中国科学院上海药物研究所
通讯作者Wei, Gaofei; Cheng, Maosheng; Liu, Yang
作者单位1.Chinese Acad Sci, Shanghai Inst Materia Med, Yantai Branch, Yantai 264000, Peoples R China
2.Keck Grad Inst, Sch Pharm & Hlth Sci, Dept Biopharmaceut Sci, Claremont, CA 91711 USA
3.Shenyang Pharmaceut Univ, Minist Educ, Key Lab Struct Based Drug Design & Discovery, Shenyang 110016, Liaoning, Peoples R China
4.Northwestern Polytech Univ, Inst Med Res, Xian 710072, Shaanxi, Peoples R China
推荐引用方式
GB/T 7714		 Wei, Gaofei,Sung, Jiahong,Luan, Weijing,et al. Natural Product Albiziabioside A Conjugated with Pyruvate Dehydrogenase Kinase Inhibitor Dichloroacetate To Induce Apoptosis-Ferroptosis-M2-TAMs Polarization for Combined Cancer Therapy[J]. JOURNAL OF MEDICINAL CHEMISTRY,2019,62(19):8760-8772.
APA Wei, Gaofei.,Sung, Jiahong.,Luan, Weijing.,Hou, Zhuang.,Wang, Shuai.,...&Liu, Yang.(2019).Natural Product Albiziabioside A Conjugated with Pyruvate Dehydrogenase Kinase Inhibitor Dichloroacetate To Induce Apoptosis-Ferroptosis-M2-TAMs Polarization for Combined Cancer Therapy.JOURNAL OF MEDICINAL CHEMISTRY,62(19),8760-8772.
MLA Wei, Gaofei,et al."Natural Product Albiziabioside A Conjugated with Pyruvate Dehydrogenase Kinase Inhibitor Dichloroacetate To Induce Apoptosis-Ferroptosis-M2-TAMs Polarization for Combined Cancer Therapy".JOURNAL OF MEDICINAL CHEMISTRY 62.19(2019):8760-8772.

入库方式： OAI收割

来源：上海药物研究所

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