Zhou, Juan; Mock, Elliot D.; Al Ayed, Karol; Di, Xinyu; Kantae, Vasudev; Burggraaff, Lindsey; Stevens, Anna F.; Martella, Andrea; Mohr, Florian; Jiang, Ming; van der Wel, Tom; Wendel, Tiemen J.; Ofman, Tim P.; Tran, Yvonne; de Koster, Nicky; van Westen, Gerard J. P.; Hankemeier, Thomas; van der Stelt, Mario published the artcile< Structure-Activity Relationship Studies of α-Ketoamides as Inhibitors of the Phospholipase A and Acyltransferase Enzyme Family>, HPLC of Formula: 16799-05-6, the main research area is PLAAT inhibitor NAPEs NAEs anandamide alpha ketoamides SAR.
The phospholipase A and acyltransferase (PLAAT) family of cysteine hydrolases consists of five members, which are involved in the Ca2+-independent production of N-acylphosphatidylethanolamines (NAPEs). NAPEs are lipid precursors for bioactive N-acylethanolamines (NAEs) that are involved in various physiol. processes such as food intake, pain, inflammation, stress, and anxiety. Recently, we identified α-ketoamides as the first pan-active PLAAT inhibitor scaffold that reduced arachidonic acid levels in PLAAT3-overexpressing U2OS cells and in HepG2 cells. Here, we report the structure-activity relationships of the α-ketoamide series using activity-based protein profiling. This led to the identification of LEI-301(I), a nanomolar potent inhibitor for the PLAAT family members. LEI-301 reduced the NAE levels, including anandamide, in cells overexpressing PLAAT2 or PLAAT5. Collectively, LEI-301 may help to dissect the physiol. role of the PLAATs.
Journal of Medicinal Chemistry published new progress about N-Acylethanolamines Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 16799-05-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H8BrCl, HPLC of Formula: 16799-05-6.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics