脂肪酸合酶——抑制肿瘤的新靶点
作者：张嘉穗;陈惠;魏国清;雷洁萍;蒋合众;
Author：
收稿日期： 年卷（期）页码：2014,29(05):-599-601
期刊名称：华西药学杂志
Journal Name：WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字：脂肪酸合酶;脂肪酸合酶抑制剂;肿瘤
Key words：
基金项目：国家自然科学基金资助项目(批准号:31200256);;
四川省科技支撑计划项目(No.2014SZ0071);;
成都市科技局高校院所应用成果转化项目(No.12DXYB228JH-002);;
中央高校基本科研业务费科技创新项目(No.2682014CX045)
中文摘要
脂肪酸合酶是生物体内催化合成内源性脂肪酸的关键酶,其在正常细胞和组织中的含量很低,但在肿瘤细胞中,脂肪酸合酶有较高的表达。对脂肪酸合酶过表达的肿瘤细胞使用脂肪酸合酶抑制剂,可诱导肿瘤细胞凋亡,而对正常细胞无影响,这对肿瘤的治疗和预防提供了新的作用靶点。文中综述了脂肪酸合酶抑制剂的研究进展。
参考文献
[1]卢辰,羊惠君,史恺.脂肪酸合成酶基因表达调控[J].四川解剖学杂志,2009,17(2):31-35.
[2]Flavin R,Peluso S,Nguyen PL,et al.Fatty acid synthase as a potential therapeutic target in cancer[J].Future Oncol,2010,6(4):551-562.
[3]Esalimani-Sahla M,Thezenas S,Simony-Lafontaine J,et al.Increased expression of fatty acid synthase and progesterone receptor in early steps of human mammary carcinogenesis[J].Int J Cancer,2007,120(2):224-229.
[4]Murata S,Yanagisawa K,Oda T,et al.Fatty acid synthase inhibitor cerulenin suppresses liver metastasis of colon cancer in mice[J].Cancer Sci,2010,101(8):1861-1865.
[5]Pandey PR,Liu W,Xing F,et al.Anti-cancer drugs targeting fatty acid synthase(FAS)[J].Recent Pat Anticancer Drug Discov,2012,7(2):185-197.
[6]Zeng XF,Li WW,Fan HJ,et al.Discovery of novel fatty acid synthase(FAS)inhibitors based on the structure of ketoaceyl synthase(KS) domain[J].Bioorg Med Chem Lett,2011,21(16):4742-4744.
[7]费翔,宋永胜.脂肪酸合成酶在上尿路移行细胞癌组织表达的临床意义及预后相关性分析[J].山西医药杂志,2012,41(1):20-22.
[8]Yoshii Y,Furukawa T,Oyama N,et al.Fatty acid synthase is a key target in multiple essential tumor functions of prostate cancer:Uptake of radiolabeled acetate as a predictor of the targeted therapy outcome[J].PLoS One,2013,8(5):e64570.
[9]Kwan HY,Yang Z,Fong WF,et al.The anti-cancer effect of oridonin is mediated by fatty acid synthase suppression in human colorectal cancer cells[J].J Gastroenterol,2013,48:182-192.
[10]Lu S,Archer MC.Fatty acid synthase is a potential molecular target for the chemoprevention of breast cancer[J].Carcinogenesis,2005,26(1):153-157.
[11]Lee JS,Sul JY,Park JB,et al.Fatty acid synthase inhibition by amentoflavone suppresses HER2/neu(erbB2)oncogene in SKBR3 human breast cancer cells[J].Phytother Res,2012,27(5):713-720.
[12]樊慧锦,田维熙,马晓丰.熊果酸抑制脂肪酸合酶及诱导HepG2细胞凋亡机制研究[J].北京师范大学学报:自然科学版,2012,48(3):266-269.
[13]Thupari JN,Pinn ML,Kuhajda FP.Fatty acid synthase inhibition in human breast cancer cells leads to malonyl-CoA-induced inhibition of fatty acid oxidation and cytotoxicity[J].Biochem Biophys Res Commun,2001,285:217-223.
[14]Bandyopadhyay S,Zhan R,Wang Y,et al.Mechanism of apoptosis induced by the inhibition of fatty acid synthase in breast cancer cells[J].Cancer Res,2006,66(11):5934-5940.
[15]Knowles LM,Yang C,Osterman A,et al.Inhibition of fatty acid synthase induces caspase-8-mediated tumor cell apoptosis by up-regulating DDIT4[J].J Biol Chem,2008,283(46):31378-31384.
[16]许乐乐,许春芳.浅蓝菌素对人胰腺癌细胞株BXPC-3的影响及机制[J].中华临床医师杂志(电子版),2013,7(19):8739-8744.
[17]Little JL,Wheeler FB,Fels DR,et al.Inhibition of fatty acid synthase induces endoplasmic reticulum stress in tumor cells[J].Cancer Res,2007,67(3):1262-1269.
[18]Chajès V,Cambot M,Moreau K,et al.Acetyl-CoA carboxylase alpha is essential to breast cancer cell survival[J].Cancer Res,2006,66(10):5287-5294.
[19]徐晓伟,王晓奎,李松.脂肪酸合成酶抑制剂的研究进展[J].国际药学研究杂志,2009,36(2):105-120.
[20]Fuentes PP,Salvesen GS.The protein structures that shape caspase activity,specificity,activation and inhibition[J].Biochem J,2004,384(2):201-232.
[21]张晔.脂肪酸合酶抑制剂的抗癌研究[J].国外医学:肿瘤学分册,2002,29(4):258-261.
[22]Loftus TM,Jawomky DE,Frehywot GL,et al.Reduced food intake and body weight in mice treated with fatty acid synthase inhibitors[J].Science,2000,28(5475):2379-2381.
[23]Zhou W,Simpson PJ,McFadden JM,et al.Fatty acid synthase inhibition triggers apoptosis during S phase in human cancer cells[J].Cancer Res,2003,63:7330-7337.
[24]Mc Fadden JM,Medg halchi SM,Thupari JN,et al.Application of a flexible synthesis of(5R)-thiolactomycin to develop new inhibitors of type I fatty acid synthase[J].J Med Chem,2005,48(4):946-961.
[25]Tian WX,Ma XF,Zhang SY,et al.Fatty acid synthase inhibitors from plants and their potential application in the prevention of metabolic syndrome[J].Clin Oncol Cancer Res,2011,8(1):1-9.
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