LCAT activator compound A is an activator of Lecithin:cholesterol acyltransferase (LCAT) including some mutant LCATs found in Familial LCAT Deficiency (FLD). LCAT activator compound A forms a covalent hydrophobic adduct with LCAT Cys 31. The chronic treatment with LCAT activator compound A results in a significant increase in HDLc, HDL particle, size, plasma apolipoprotein A-I level, plasma cholesteryl ester to free cholesterol ratio, and a significant reduction in very low-density lipoprotein cholesterol in hamsters.
Lecithin:cholesterol acyltransferase (LCAT) including some FLD mutant LCATs
Metabolism: clinical and experimental, 61(4), 470-481 (2011-10-18)
The objective was to assess whether pharmacological activation of lecithin cholesterol acyltransferase (LCAT) could exert beneficial effects on lipoprotein metabolism. A putative small molecule activator (compound A) was used as a tool compound in in vitro and in vivo studies.
The Journal of pharmacology and experimental therapeutics, 362(2), 306-318 (2017-06-04)
Lecithin:cholesterol acyltransferase (LCAT) catalyzes plasma cholesteryl ester formation and is defective in familial lecithin:cholesterol acyltransferase deficiency (FLD), an autosomal recessive disorder characterized by low high-density lipoprotein, anemia, and renal disease. This study aimed to investigate the mechanism by which compound
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