Recent progress in the discovery and development of stearoyl CoA desaturase inhibitors.
Stearoyl-CoA desaturase 1 (SCD1) is a rate-limiting enzyme in the biosynthesis of monounsaturated fatty acids from their saturated fatty acid precursors. SCD1 introduces a cis-double bond at the Δ9 position (between carbons 9 and 10) of stearoyl (C18:0) and palmitoyl-CoA (C16:0). SCD1 has been shown to be a crucial factor in lipid metabolism and body weight control. In addition, SCD1 inhibitors are claimed to be new treatments for various diseases, such as skin disorders, nonalcoholic steatohepatitis (NASH), hepatitis C virus (HCV), Alzheimer's disease, or cancer. This review aims to summarize the examples of the recently reported novel SCD1 inhibitors and to highlight the emerging areas of target indications that may hold promise for the development of SCD1 inhibitors.
Venture Science Laboratories, Daiichi Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan. Electronic address: uto.yoshikazu.pw@daiichisankyo.co.jp.
Yoshikazu
Y
Uto
D000818:Animals; D055808:Drug Discovery; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D008099:Liver / Q000187:drug effects; D009369:Neoplasms / Q000201:enzymology / Q000473:pathology; D012867:Skin / Q000201:enzymology; D013230:Stearoyl-CoA Desaturase / Q000037:antagonists & inhibitors*
D004791:Enzyme Inhibitors; D013230:Stearoyl-CoA Desaturase
Acne; Cancer; Nonalcoholic steatohepatitis (NASH); Skin disorders; Stearoyl-CoA desaturase 1 (SCD1)