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Progress in the development of fatty acid synthase inhibitors as anticancer targets》.pdf
Bioorganic Medicinal Chemistry Letters 25 (2015) 4363–4369
Contents lists available at ScienceDirect
Bioorganic Medicinal Chemistry Letters
journal homepage: /locate/bmcl
Progress in the development of fatty acid synthase inhibitors
as anticancer targets
Genevieve E. Mullen, Larry Yet ⇑
University of South Alabama, Department of Chemistry, Mobile, AL 36688, United States
a r t i c l e i n f o a b s t r a c t
Article history: Fatty acid synthase (E.C. 5; FASN) is a multifunctional enzyme system that catalyzes the formation
Received 27 July 2015 of fatty acids from acetyl-CoA, malonyl-CoA, and NADPH and plays a central role in lipid biosynthesis.
Revised 26 August 2015 Two classes of FASN exist: FASN I in animals and fungi, and FASN II in plants and prokaryotes. Animal
Accepted 31 August 2015
FASN I is a homodimeric protein found in the cytosol of lipogenic tissues such as the liver and brain.
Available online 2 September 2015
Many human carcinomas exhibit elevated levels of FASN I, though the benefit to cancer cells is still
unclear. Inhibition of FASN I selectively effects apoptosis in cancer cells, and the role of FASN I in
Keywords:
chemotherapy is a growing area of research with the use of natural products and small molecule
Fatty acid synthase
inhibitors.
Natural produc
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