HRASLS
H-RAS-like suppressor
HRASLS is a family of proteins that are involved in the metabolism of phospholipids, particularly lysophospholipids. HRASLS proteins can act as phospholipases, catalyzing the hydrolysis of lysophospholipids like LPA and LPC. This hydrolysis plays a crucial role in regulating the levels of these bioactive lipids in the cell. For example, HRASLS3 has phospholipase D activity and can influence the production of signaling molecules derived from lysophospholipids. HRASLS6, on the other hand, has LPCAT activity and can modify the acyl composition of LPC. Dysregulation of HRASLS functions has been associated with various physiological and pathological processes, including inflammation, cancer, and lipid metabolism disorders[1][2].
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LEI110
0 ImagesLEI110 is a pan-inhibitor of the HRASLS family and an inhibitor of AP-2α, with a Ki of 20 nM against PLA2G16. LEI110 exhibits inhibitory activity against PLA2G16, HRASLS2, RARRES3 and iNAT, with pIC50 values of 7.0, 6.8, 6.8 and 7.6, respectively. LEI110 binds to the active site of PLA2G16, reduces intracellular arachidonic acid levels, and attenuates oleic acid-induced lipolysis. LEI110 stabilizes AP-2α, impairs its DNA-binding ability, inhibits the transcription of DNA damage repair genes, induces the accumulation of oxidative DNA damage, suppresses cell proliferation and clonogenicity, and sensitizes HCC cells to DNA-damaging agents. LEI110 can be used in research related to obesity, fatty liver disease, the common cold and hepatocellular carcinoma. -
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