Recent Advances in the Development of Fatty Acid Synthase Inhibitors of Anticancer Agents.

Recent Advances in the Development of Fatty Acid Synthase Inhibitors of Anticancer Agents.
Mini Rev Med Chem. 2020 Aug 10;:
Authors: Singh S, Karthikeyan C, Moorthy NSHN
Abstract
Fatty acid synthase (FASN) is a multifunctional enzyme involved in the production of fatty acids for lipid biosynthesis. FASN is overexpressed in multiple diseases like cancer, viral, non-alcoholic fatty liver disease and metabolic disorders making it an attractive target for new drug discovery for these diseases. In cancer, FASN affects the structure and function of the cellular membrane by channelizing with signaling pathways along with the post-translational palmitoylation of proteins. There are several natural and synthetic FASN inhibitors reported in the literature, a few examples are GSK 2194069 (7.7 nM), imidazopyridine (16 nM), epigallocatechin-3-gallate (42.0 µg/ml) and platensimycin (300 nM) but except for TVB-2640, none of the aforementioned inhibitors have made into clinical trials. The present review summarizes the recent advancements made in anticancer drug discovery targeting FASN. Furthermore, the review also provides insights into the medicinal chemistry of small molecule inhibitors targeting different FASN enzyme domains, and also critically analyses the structural requirements for FASN inhibition with an objective to support rational design and development of new generation FASN inhibitors with clinical potential in diseases like cancer.
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Source: Mini Reviews in Medicinal Chemistry - August 9, 2020 Category: Chemistry Authors: Singh S, Karthikeyan C, Moorthy NSHN Tags: Mini Rev Med Chem Source Type: research