Liu Hailan, Liu Jing-Yuan, Wu Xi, Zhang Jian-Ting
Department of Pharmacology and Toxicology and IU Simon Cancer Center, Indiana University School of Medicine, Indianapolis, IN 46202.
Int J Biochem Mol Biol. 2010 Jul 18;1(1):69-89.
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.
人类脂肪酸合酶（FASN）是一种分子量为270 kDa的胞质二聚体酶，负责棕榈酸酯的合成。FASN正逐渐作为人类癌症诊断和预后的标志物重新被发现。最近的研究表明，FASN是一种癌基因，抑制FASN可有效且选择性地杀死癌细胞。随着FASN晶体结构的最新发表以及FASN抑制剂的新进展，靶向FASN为代谢性对抗癌症打开了一扇新的机遇之窗。在本文中，我们将批判性地综述在理解FASN的结构、功能及其在癌症中的作用，以及将FASN作为人类癌症治疗的药理学靶点方面的最新进展。
