Fatty acid synthase as a potential therapeutic target in cancer.
Fatty acid synthase as a potential therapeutic target in cancer.
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DOI：
10.2217/fon.10.11
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发表时间：
2010-04
期刊：
影响因子：
--
通讯作者：
Loda M
中科院分区：
文献类型：
--
作者：
Flavin R;Peluso S;Nguyen PL;Loda M
脂肪酸合成酶（FASN）是参与肿瘤脂肪生成的关键酶。FASN的过表达在许多癌症中都很常见，越来越多的证据表明它是一种代谢性癌基因，在肿瘤生长和生存中起着重要作用，使其成为癌症治疗的一个有吸引力的靶点。早期的小分子FASN抑制剂如cerulenin、C75和奥利司他已被证明在几种癌细胞系中诱导细胞凋亡，并在几种癌症异种移植模型中诱导肿瘤生长延迟，但其机制仍不清楚。这些分子受到药理学限制和体重减轻的副作用，阻碍了它们作为全身药物的发展。最近报道了几种有效的抑制剂，可能有助于揭示和利用FASN的全部潜力，在不久的将来作为癌症治疗的靶点。此外，FASN抑制剂的新来源，如绿茶和膳食大豆，使饮食控制和化学预防成为未来治疗的潜在替代模式。
Fatty acid synthase (FASN) is a key enzyme involved in neoplastic lipogenesis. Overexpression of FASN is common in many cancers, and accumulating evidence suggests that it is a metabolic oncogene with an important role in tumor growth and survival, making it an attractive target for cancer therapy. Early small-molecule FASN inhibitors such as cerulenin, C75 and orlistat have been shown to induce apoptosis in several cancer cell lines and to induce tumor growth delay in several cancer xenograft models but their mechanism is still not well understood. These molecules suffer from pharmacological limitations and weight loss as a side effect that prevent their development as systemic drugs. Several potent inhibitors have recently been reported that may help to unravel and exploit the full potential of FASN as a target for cancer therapy in the near future. Furthermore, novel sources of FASN inhibitors, such as green tea and dietary soy, make both dietary manipulation and chemoprevention potential alternative modes of therapy in the future.
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DOI：
10.1038/labinvest.2008.97
发表时间：
2008-12
期刊：
Laboratory investigation; a journal of technical methods and pathology
影响因子：
--
作者：
通讯作者：
--
影响因子：
16.8
作者：
Asturias, FJ;Chadick, JZ;Smith, S
通讯作者：
Smith, S
影响因子：
8
作者：
Bandyopadhyay, S;Pai, SK;Watabe, K
通讯作者：
Watabe, K
影响因子：
4.8
作者：
Knowles, LM;Axelrod, F;Smith, JW
通讯作者：
Smith, JW
影响因子：
6.4
作者：
Brusselmans, K;De Schrijver, E;Swinnen, JV
通讯作者：
Swinnen, JV