Biochemistry, molecular biology, and pharmacology of fatty acid synthase, an emerging therapeutic target and diagnosis/prognosis marker.
Biochemistry, molecular biology, and pharmacology of fatty acid synthase, an emerging therapeutic target and diagnosis/prognosis marker.
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发表时间：
2010-07
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通讯作者：
Hailan Liu;Jing-Yuan Liu;Xi Wu;Jian-Ting Zhang
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作者：
Hailan Liu;Jing-Yuan Liu;Xi Wu;Jian-Ting Zhang
人脂肪酸合成酶（FATCH）是一种270-kDa的胞质二聚体酶，负责棕榈酸酯的合成。作为人类癌症的诊断和预后的标志物，FXR正在慢慢出现并被重新发现。近年来的研究表明，FXR是一种癌基因，抑制FXR能有效地选择性杀伤癌细胞。随着最近发表的Festival晶体结构和Festival抑制剂的新发展，靶向Festival为代谢抗癌打开了一扇新的机会之窗。本文就近年来有关FXR的结构、功能、在肿瘤中的作用以及FXR靶向治疗肿瘤的研究进展作一综述。
Human fatty acid synthase (FASN) is a 270-kDa cytosolic dimeric enzyme that is responsible for palmitate synthesis. FASN is slowly emerging and rediscovered as a marker for diagnosis and prognosis of human cancers. Recent studies showed that FASN is an oncogene and inhibition of FASN effectively and selectively kill cancer cells. With recent publications of the FASN crystal structure and the new development of FASN inhibitors, targeting FASN opens a new window of opportunity for metabolically combating cancers. In this article, we will review critically the recent progresses in understanding the structure, function, and the role of FASN in cancers and pharmacologically targeting FASN for human cancer treatment.