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Lipase inhibitors act on enzymes that hydrolyze ester bonds in triglycerides, diglycerides and monoglycerides. In adipose tissue, adipose triglyceride lipase (ATGL) starts lipolysis, a role reported in 2004. Hormone-sensitive lipase (HSL) and monoacylglycerol lipase (MAGL) then complete the release of fatty acids. Atglistatin, described in 2013, inhibits ATGL, and HSL-IN-1 targets HSL. JZL184 blocks MAGL, which hydrolyzes the endocannabinoid 2-arachidonoylglycerol, and its 2009 report linked this to cannabinoid behavioral effects in mice. JZL195 inhibits MAGL together with fatty acid amide hydrolase (FAAH), covered in the FAAH category. KT109 targets diacylglycerol lipase beta (DAGLβ), and XEN445 inhibits endothelial lipase.
SR-4559 is a selective ligand for α/β hydrolase domain-containing protein 5 (ABHD5). It activates adipose triglyceride lipase (ATGL) and promotes lipolysis by disrupting the interactions between ABHD5 and perilipin (PLIN) in adipocytes and muscle cells. This compound is applicable in research related to metabolic disorders, including Chanarin-Dorfman syndrome.
