Esterastin: A potent inhibitor of lysosomal acid lipase

Tsuneo Imanaka, Yoshinori Moriyama, Gnobor G. Ecsedi, Takaaki Aoyagi, Kimiko Amanuma-muto, Shoji Ohkuma, Tatsuya Takano

Research output: Contribution to journalArticle

18 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)1017-1020
Number of pages4
JournalJournal of Biochemistry
Volume94
Issue number3
Publication statusPublished - Jul 1983
Externally publishedYes

Fingerprint

Sterol Esterase
Lipases
Inhibitor
Enzymes
Acids
Rabbit
Liver
Substrate
Lipase
Enzyme inhibition
Enzyme activity
Metabolites
Carboxylesterase
Inhibitory Concentration 50
esterastin
Substrates
Rabbits

ASJC Scopus subject areas

  • Statistics, Probability and Uncertainty
  • Applied Mathematics
  • Physiology (medical)
  • Radiology Nuclear Medicine and imaging
  • Molecular Biology
  • Biochemistry

Cite this

Imanaka, T., Moriyama, Y., Ecsedi, G. G., Aoyagi, T., Amanuma-muto, K., Ohkuma, S., & Takano, T. (1983). Esterastin: A potent inhibitor of lysosomal acid lipase. Journal of Biochemistry, 94(3), 1017-1020.

Esterastin : A potent inhibitor of lysosomal acid lipase. / Imanaka, Tsuneo; Moriyama, Yoshinori; Ecsedi, Gnobor G.; Aoyagi, Takaaki; Amanuma-muto, Kimiko; Ohkuma, Shoji; Takano, Tatsuya.

In: Journal of Biochemistry, Vol. 94, No. 3, 07.1983, p. 1017-1020.

Research output: Contribution to journalArticle

Imanaka, T, Moriyama, Y, Ecsedi, GG, Aoyagi, T, Amanuma-muto, K, Ohkuma, S & Takano, T 1983, 'Esterastin: A potent inhibitor of lysosomal acid lipase', Journal of Biochemistry, vol. 94, no. 3, pp. 1017-1020.
Imanaka T, Moriyama Y, Ecsedi GG, Aoyagi T, Amanuma-muto K, Ohkuma S et al. Esterastin: A potent inhibitor of lysosomal acid lipase. Journal of Biochemistry. 1983 Jul;94(3):1017-1020.
Imanaka, Tsuneo ; Moriyama, Yoshinori ; Ecsedi, Gnobor G. ; Aoyagi, Takaaki ; Amanuma-muto, Kimiko ; Ohkuma, Shoji ; Takano, Tatsuya. / Esterastin : A potent inhibitor of lysosomal acid lipase. In: Journal of Biochemistry. 1983 ; Vol. 94, No. 3. pp. 1017-1020.
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