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Small-Molecule Targeting of Oncogenic FTO Demethylase in Acute Myeloid Leukemia

文献类型：期刊论文

作者Huang, Yue3,4; Su, Rui5,6,7; Sheng, Yue8,9; Dong, Lei5,6,7; Dong, Ze3; Xu, Hongjiao3,4; Ni, Tengfeng3; Zhang, Zijie Scott1,2; Zhang, Tao3; Li, Chenying5,6,10
刊名CANCER CELL
出版日期2019-04-15
卷号35期号:4页码:677-+
ISSN号1535-6108
DOI10.1016/j.ccell.2019.03.006
通讯作者Qian, Zhijian(zhijian.qian@medicine.ufl.edu) ; Chen, Jianjun(jianchen@coh.org) ; Yang, Cai-Guang(yangcg@simm.ac.cn)
英文摘要FTO, an mRNA N-6-methyladenosine (m(6)A) demethylase, was reported to promote leukemogenesis. Using structure-based rational design, we have developed two promising FTO inhibitors, namely FB23 and FB23-2, which directly bind to FTO and selectively inhibit FTO's m(6)A demethylase activity. Mimicking FTO depletion, FB23-2 dramatically suppresses proliferation and promotes the differentiation/apoptosis of human acute myeloid leukemia (AML) cell line cells and primary blast AML cells in vitro. Moreover, FB23-2 significantly inhibits the progression of human AML cell lines and primary cells in xeno-transplanted mice. Collectively, our data suggest that FTO is a druggable target and that targeting FTO by small-molecule inhibitors holds potential to treat AML.
WOS关键词MESSENGER-RNA ; FAT MASS ; M(6)A ; METHYLATION ; N-6-METHYLADENOSINE ; PROTEIN ; BINDING ; TRANSLATION ; CELLS ; DNA
资助项目National Natural Science Foundation of China[21725801] ; National Natural Science Foundation of China[21807103] ; National Natural Science Foundation of China[91753000] ; National Key R&D Program of China[2016YFA0501500] ; Science and Technology Commission of Shanghai Municipality[18YF1428500] ; Science and Technology Commission of Shanghai Municipality[18431907100] ; China Postdoctoral Science Foundation[2018M640434] ; China Postdoctoral Science Foundation[2017M621570] ; China Postdoctoral Science Foundation[2018M632187] ; Chinese Academy of Sciences[XDA12020359] ; NIH RO1[CA214965] ; NIH RO1[CA211614] ; NIH RO1[CA178454] ; NIH RO1[HL131444] ; NIH RO1[DK107615]
WOS研究方向Oncology ; Cell Biology
语种英语
WOS记录号WOS:000464931000014
出版者CELL PRESS
源URL[http://119.78.100.183/handle/2S10ELR8/290083]  
专题新药研究国家重点实验室
通讯作者Qian, Zhijian; Chen, Jianjun; Yang, Cai-Guang
作者单位1.Univ Chicago, Dept Chem, Chicago, IL 60637 USA
2.Univ Chicago, Inst Biophys Dynam, Chicago, IL 60637 USA
3.Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China
4.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
5.City Hope Natl Med Ctr, Dept Syst Biol, Duarte, CA 91010 USA
6.City Hope Natl Med Ctr, Gehr Family Ctr Leukemia Res, Duarte, CA 91010 USA
7.Univ Cincinnati, Coll Med, Dept Canc Biol, Cincinnati, OH 45219 USA
8.Univ Florida, Dept Med, Hlth Canc Ctr, Gainesville, FL 32610 USA
9.Univ Illinois, Dept Med, Chicago, IL 60612 USA
10.Zhejiang Univ, Key Lab Hematopoiet Malignancies, Dept Hematol, Affiliated Hosp 1, Hangzhou 310003, Zhejiang, Peoples R China
推荐引用方式
GB/T 7714		 Huang, Yue,Su, Rui,Sheng, Yue,et al. Small-Molecule Targeting of Oncogenic FTO Demethylase in Acute Myeloid Leukemia[J]. CANCER CELL,2019,35(4):677-+.
APA Huang, Yue.,Su, Rui.,Sheng, Yue.,Dong, Lei.,Dong, Ze.,...&Yang, Cai-Guang.(2019).Small-Molecule Targeting of Oncogenic FTO Demethylase in Acute Myeloid Leukemia.CANCER CELL,35(4),677-+.
MLA Huang, Yue,et al."Small-Molecule Targeting of Oncogenic FTO Demethylase in Acute Myeloid Leukemia".CANCER CELL 35.4(2019):677-+.

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来源：上海药物研究所

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