The lead molecule ABX-1431 is a potent selective inhibitor of the serine hydrolase monoacylglycerol lipase
(MGLL) that potentiates endocannabinoid signalling to restore homeostatic balance in the central nervous system.
JZL184 was originally developed by the Cravatt lab as an inhibitor of the mammalian enzyme monoacylglycerol lipase
(MAGL), whose normal job includes the breakdown of a molecule called 2-AG.
The final step during lipolysis is controlled by the monoacylglycerol lipase
(Mgl) and by the breaking down of MG into FA and glycerol.
There are three lipases expressed in skeletal muscle that are responsible for the breakdown of TAGs: monoacylglycerol lipase
, adipose triglyceride lipase (ATGL), and hormone-sensitive lipase (HSL) .
- US-based pharmaceutical company Abide Therapeutics has started enrollment and dosing in a Phase 1 PET occupancy study with ABX-1431, a first-in-class investigational monoacylglycerol lipase
inhibitor, and [18F] ABX-1488, a human MGLL-specific PET ligand, the company said.
2-AG is hydrolyzed into arachidonic acid and glycerol primarily by monoacylglycerol lipase (MGL), which was first cloned from mouse adipose tissue.
(2007) Presynaptic monoacylglycerol lipase activity determines basal endocannabinoid tone and terminates retrograde endocannabinoid signaling in the hippocampus.
Lipolysis in adipocytes is regulated in a step-wise fashion by adipose triglyceride lipase (ATGL), hormone-sensitive lipase (HSL), and monoacylglycerol lipase
. These lipases locate around the lipid droplet and HSL is activated by the adrenaline effect.
Lambert, "Synthesis and pharmacological evaluation of 2,4-dinitroaryldithiocarbamate derivatives as novel monoacylglycerol lipase inhibitors," Journal of Medicinal Chemistry, vol.
Lambert, "Disulfiram is an inhibitor of human purified monoacylglycerol lipase, the enzyme regulating 2-arachidonoylglycerol signaling," ChemBioChem, vol.
Washington, November 2 ( ANI ): A new study has identified an enzyme called Monoacylglycerol lipase
(MAGL) as a potential therapeutic target to treat or prevent Alzheimer's disease.
Experts at The Scripps Research Institute identified the enzyme, called monoacylglycerol lipase
(MAGL) as a key player responsible for the aggressive behaviour of cancer cells.