• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

硬脂酰辅酶 A 去饱和酶抑制对表现出高水平从头脂肪酸生物合成和去饱和的急性髓系白血病具有毒性。

Stearoyl-CoA desaturase inhibition is toxic to acute myeloid leukemia displaying high levels of the de novo fatty acid biosynthesis and desaturation.

机构信息

Centre for Haemato-Oncology, Barts Cancer Institute, Queen Mary University of London, London, UK.

Department of Physiology and Croatian Institute for Brain Research, University of Zagreb School of Medicine, Zagreb, Croatia.

出版信息

Leukemia. 2024 Nov;38(11):2395-2409. doi: 10.1038/s41375-024-02390-9. Epub 2024 Aug 26.

DOI:10.1038/s41375-024-02390-9
PMID:39187579
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11518998/
Abstract

Identification of specific and therapeutically actionable vulnerabilities, ideally present across multiple mutational backgrounds, is needed to improve acute myeloid leukemia (AML) patients' outcomes. We identify stearoyl-CoA desaturase (SCD), the key enzyme in fatty acid (FA) desaturation, as prognostic of patients' outcomes and, using the clinical-grade inhibitor SSI-4, show that SCD inhibition (SCDi) is a therapeutic vulnerability across multiple AML models in vitro and in vivo. Multiomic analysis demonstrates that SCDi causes lipotoxicity, which induces AML cell death via pleiotropic effects. Sensitivity to SCDi correlates with AML dependency on FA desaturation regardless of mutational profile and is modulated by FA biosynthesis activity. Finally, we show that lipotoxicity increases chemotherapy-induced DNA damage and standard chemotherapy further sensitizes AML cells to SCDi. Our work supports developing FA desaturase inhibitors in AML while stressing the importance of identifying predictive biomarkers of response and biologically validated combination therapies to realize their full therapeutic potential.

摘要

需要鉴定具有特异性和治疗作用的弱点,理想情况下这些弱点应存在于多种突变背景中,以改善急性髓系白血病(AML)患者的预后。我们确定硬脂酰辅酶 A 去饱和酶(SCD)是脂肪酸(FA)去饱和的关键酶,它可以预测患者的预后,并且使用临床级抑制剂 SSI-4 表明,SCD 抑制(SCDi)是体外和体内多种 AML 模型的治疗弱点。多组学分析表明,SCDi 导致脂肪毒性,通过多效性作用诱导 AML 细胞死亡。对 SCDi 的敏感性与 AML 对 FA 去饱和的依赖性相关,而与突变特征无关,并受 FA 生物合成活性的调节。最后,我们表明脂肪毒性会增加化疗引起的 DNA 损伤,并且标准化疗会进一步使 AML 细胞对 SCDi 敏感。我们的工作支持在 AML 中开发 FA 去饱和酶抑制剂,同时强调确定反应预测性生物标志物和经过生物学验证的联合治疗方案的重要性,以充分发挥其治疗潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f605/11518998/43a421fe1b62/41375_2024_2390_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f605/11518998/94edc0b2251d/41375_2024_2390_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f605/11518998/33e28b240dcc/41375_2024_2390_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f605/11518998/cb7d633005b3/41375_2024_2390_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f605/11518998/873cf37abdb8/41375_2024_2390_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f605/11518998/30b8366420b9/41375_2024_2390_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f605/11518998/5abf2360ee53/41375_2024_2390_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f605/11518998/43a421fe1b62/41375_2024_2390_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f605/11518998/94edc0b2251d/41375_2024_2390_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f605/11518998/33e28b240dcc/41375_2024_2390_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f605/11518998/cb7d633005b3/41375_2024_2390_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f605/11518998/873cf37abdb8/41375_2024_2390_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f605/11518998/30b8366420b9/41375_2024_2390_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f605/11518998/5abf2360ee53/41375_2024_2390_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f605/11518998/43a421fe1b62/41375_2024_2390_Fig7_HTML.jpg

相似文献

1
Stearoyl-CoA desaturase inhibition is toxic to acute myeloid leukemia displaying high levels of the de novo fatty acid biosynthesis and desaturation.硬脂酰辅酶 A 去饱和酶抑制对表现出高水平从头脂肪酸生物合成和去饱和的急性髓系白血病具有毒性。
Leukemia. 2024 Nov;38(11):2395-2409. doi: 10.1038/s41375-024-02390-9. Epub 2024 Aug 26.
2
In vitro and in vivo antitumor activities of T-3764518, a novel and orally available small molecule stearoyl-CoA desaturase 1 inhibitor.新型口服小分子硬脂酰辅酶 A 去饱和酶 1 抑制剂 T-3764518 的体内外抗肿瘤活性。
Eur J Pharmacol. 2017 Jul 15;807:21-31. doi: 10.1016/j.ejphar.2017.03.064. Epub 2017 Apr 22.
3
FGFR3 stimulates stearoyl CoA desaturase 1 activity to promote bladder tumor growth.成纤维细胞生长因子受体 3 可激活硬脂酰辅酶 A 去饱和酶 1 活性,促进膀胱癌生长。
Cancer Res. 2012 Nov 15;72(22):5843-55. doi: 10.1158/0008-5472.CAN-12-1329. Epub 2012 Sep 26.
4
The importance of the stearoyl-CoA desaturase system in octadecenoate metabolism in the Morris hepatoma 7288C.硬脂酰辅酶A去饱和酶系统在莫里斯肝癌7288C中十八碳烯酸代谢中的重要性。
Biochim Biophys Acta. 1985 Jun 30;845(3):380-8. doi: 10.1016/0167-4889(85)90202-2.
5
C/EBPα Confers Dependence to Fatty Acid Anabolic Pathways and Vulnerability to Lipid Oxidative Stress-Induced Ferroptosis in FLT3-Mutant Leukemia.C/EBPα赋予FLT3突变型白血病对脂肪酸合成途径的依赖性以及对脂质氧化应激诱导的铁死亡的易感性。
Cancer Discov. 2023 Jul 7;13(7):1720-1747. doi: 10.1158/2159-8290.CD-22-0411.
6
Stearoyl-CoA Desaturase-1 Protects Cells against Lipotoxicity-Mediated Apoptosis in Proximal Tubular Cells.硬脂酰辅酶A去饱和酶-1保护细胞免受近端肾小管细胞中脂毒性介导的细胞凋亡。
Int J Mol Sci. 2016 Nov 9;17(11):1868. doi: 10.3390/ijms17111868.
7
Short communication: heritability of milk fatty acid composition and stearoyl-CoA desaturase indices in dairy cows.短讯:奶牛乳脂肪酸组成和硬脂酰辅酶 A 去饱和酶指数的遗传力。
J Dairy Sci. 2010 Apr;93(4):1743-8. doi: 10.3168/jds.2009-2695.
8
Metabolic reprogramming of the heart through stearoyl-CoA desaturase.通过硬脂酰辅酶 A 去饱和酶对心脏进行代谢重编程。
Prog Lipid Res. 2015 Jan;57:1-12. doi: 10.1016/j.plipres.2014.11.003. Epub 2014 Dec 5.
9
Biochemical and physiological function of stearoyl-CoA desaturase.硬脂酰辅酶A去饱和酶的生化及生理功能
Am J Physiol Endocrinol Metab. 2009 Jul;297(1):E28-37. doi: 10.1152/ajpendo.90897.2008. Epub 2008 Dec 9.
10
Abrogation of de novo lipogenesis by stearoyl-CoA desaturase 1 inhibition interferes with oncogenic signaling and blocks prostate cancer progression in mice.通过硬脂酰辅酶 A 去饱和酶 1 抑制作用废除从头脂肪生成会干扰致癌信号转导并阻止小鼠前列腺癌的进展。
Mol Cancer Ther. 2010 Jun;9(6):1740-54. doi: 10.1158/1535-7163.MCT-09-1064. Epub 2010 Jun 8.

引用本文的文献

1
WNK1 signalling regulates amino acid transport and mTORC1 activity to sustain acute myeloid leukaemia growth.WNK1信号传导调节氨基酸转运和mTORC1活性以维持急性髓系白血病的生长。
Nat Commun. 2025 May 27;16(1):4920. doi: 10.1038/s41467-025-59969-8.
2
Targeting lipid metabolism in acute myeloid leukemia: biological insights and therapeutic opportunities.靶向急性髓系白血病中的脂质代谢:生物学见解与治疗机遇
Leukemia. 2025 May 22. doi: 10.1038/s41375-025-02645-z.
3
Identification of a novel unfolded protein response related signature for predicting the prognosis of acute myeloid leukemia.

本文引用的文献

1
A 4-gene prognostic index for enhancing acute myeloid leukaemia survival prediction.用于增强急性髓系白血病生存预测的 4 基因预后指数。
Br J Haematol. 2024 Jun;204(6):2287-2300. doi: 10.1111/bjh.19472. Epub 2024 Apr 23.
2
Acute myeloid leukaemia.急性髓细胞白血病。
Lancet. 2023 Jun 17;401(10393):2073-2086. doi: 10.1016/S0140-6736(23)00108-3. Epub 2023 Apr 15.
3
Mannose metabolism inhibition sensitizes acute myeloid leukaemia cells to therapy by driving ferroptotic cell death.甘露糖代谢抑制通过驱动铁死亡细胞死亡使急性髓系白血病细胞对治疗敏感。
鉴定一种用于预测急性髓系白血病预后的新型未折叠蛋白反应相关特征。
Sci Rep. 2025 Feb 25;15(1):6705. doi: 10.1038/s41598-025-91524-9.
4
CAMKIIδ Reinforces Lipid Metabolism and Promotes the Development of B Cell Lymphoma.钙/钙调蛋白依赖性蛋白激酶IIδ增强脂质代谢并促进B细胞淋巴瘤的发展。
Adv Sci (Weinh). 2025 Mar;12(10):e2409513. doi: 10.1002/advs.202409513. Epub 2025 Jan 22.
Nat Commun. 2023 Apr 14;14(1):2132. doi: 10.1038/s41467-023-37652-0.
4
C/EBPα Confers Dependence to Fatty Acid Anabolic Pathways and Vulnerability to Lipid Oxidative Stress-Induced Ferroptosis in FLT3-Mutant Leukemia.C/EBPα赋予FLT3突变型白血病对脂肪酸合成途径的依赖性以及对脂质氧化应激诱导的铁死亡的易感性。
Cancer Discov. 2023 Jul 7;13(7):1720-1747. doi: 10.1158/2159-8290.CD-22-0411.
5
Integrative phosphoproteomics defines two biologically distinct groups of KMT2A rearranged acute myeloid leukaemia with different drug response phenotypes.整合磷酸化蛋白质组学定义了具有不同药物反应表型的 KMT2A 重排急性髓系白血病的两种生物学上不同的群体。
Signal Transduct Target Ther. 2023 Feb 27;8(1):80. doi: 10.1038/s41392-022-01288-1.
6
Complex I inhibitor of oxidative phosphorylation in advanced solid tumors and acute myeloid leukemia: phase I trials.晚期实体瘤和急性髓系白血病中氧化磷酸化复合物 I 抑制剂的 I 期临床试验。
Nat Med. 2023 Jan;29(1):115-126. doi: 10.1038/s41591-022-02103-8. Epub 2023 Jan 19.
7
Targeting de novo lipid synthesis induces lipotoxicity and impairs DNA damage repair in glioblastoma mouse models.靶向从头合成脂质会导致神经胶质瘤小鼠模型中的脂毒性,并损害 DNA 损伤修复。
Sci Transl Med. 2023 Jan 18;15(679):eabq6288. doi: 10.1126/scitranslmed.abq6288.
8
A tale of two lipids: Lipid unsaturation commands ferroptosis sensitivity.两种脂质的故事:脂质不饱和度决定铁死亡敏感性。
Proteomics. 2023 Mar;23(6):e2100308. doi: 10.1002/pmic.202100308. Epub 2023 Jan 13.
9
An oncogenic enhancer encodes selective selenium dependency in AML.致癌增强子赋予 AML 对硒的选择性依赖性。
Cell Stem Cell. 2022 Mar 3;29(3):386-399.e7. doi: 10.1016/j.stem.2022.01.003. Epub 2022 Feb 1.
10
Low glycaemic diets alter lipid metabolism to influence tumour growth.低血糖生成饮食通过改变脂代谢影响肿瘤生长。
Nature. 2021 Nov;599(7884):302-307. doi: 10.1038/s41586-021-04049-2. Epub 2021 Oct 20.