TY - JOUR
T1 - Esterastin
T2 - A potent inhibitor of lysosomal acid lipase
AU - Imanaka, Tsuneo
AU - Moriyama, Yoshinori
AU - Ecsedi, Gnobor G.
AU - Aoyagi, Takaaki
AU - Amanuma-muto, Kimiko
AU - Ohkuma, Shoji
AU - Takano, Tatsuya
PY - 1983/7
Y1 - 1983/7
N2 - The effect of a fungal metabolite, esterastin, on lysosomal acid lipase purified from rabbit liver was studied. Esterastin inhibited the enzyme activity very strongly (IC50, about 80 nM). The inhibition of acid lipase by esterastin was competitive with respect to the substrate and the inhibition constant for esterastin was 90 nM. Esterastin was less inhibitory to other lipolytic enzymes, such as pancreatic lipase and carboxylesterase. Thus esterastin is a potent new inhibitor of lysosomal acid lipase.
AB - The effect of a fungal metabolite, esterastin, on lysosomal acid lipase purified from rabbit liver was studied. Esterastin inhibited the enzyme activity very strongly (IC50, about 80 nM). The inhibition of acid lipase by esterastin was competitive with respect to the substrate and the inhibition constant for esterastin was 90 nM. Esterastin was less inhibitory to other lipolytic enzymes, such as pancreatic lipase and carboxylesterase. Thus esterastin is a potent new inhibitor of lysosomal acid lipase.
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U2 - 10.1093/oxfordjournals.jbchem.a134399
DO - 10.1093/oxfordjournals.jbchem.a134399
M3 - Article
C2 - 6643414
AN - SCOPUS:0020544832
SN - 0021-924X
VL - 94
SP - 1017
EP - 1020
JO - Journal of Biochemistry
JF - Journal of Biochemistry
IS - 3
ER -