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The importance of the hydroxyl moieties for inhibition of the Ca(2+)-ATPase by trilobolide and 2,5-di(tert-butyl)-1,4-benzohydroquinone.

Abstract：

:Trilobolide and 2,5-di(tert-butyl)-1,4-benzohydroquinone (BHQ) are potent inhibitors of the Ca(2+)-ATPase of skeletal muscle sarcoplasmic reticulum. Desoxytrilobolide and 2,5-di(tert-butyl)-1,4-diacetylphenol (acetyl-BHQ) have much lower potencies than their parent compounds and 2,5-di(tert-butyl)-1,4-benzoquinone (BQ) has no effect on ATPase activity. Studies using the ATPase labelled with 4-nitrobenzo-2-oxa-1,3-diazole (NBD) suggest that both trilobolide and BHQ bind more strongly to the E2 conformation of the ATPase than to the E1 conformation. Desoxytrilobolide, acetyl-BHQ and BQ have little effect on the E1/E2 equilibrium. Studies with mixtures of trilobolide and desoxytrilobolide suggest that the inactive derivatives are unable to bind to the ATPase.

journal_name

Biochem Biophys Res Commun

journal_title

Biochemical and biophysical research communications

authors

Wictome M,Holub M,East JM,Lee AG

doi

10.1006/bbrc.1994.1316

subject

Has Abstract

pub_date

1994-03-15 00:00:00

pages

916-21

issue

2

eissn

0006-291X

issn

1090-2104

pii

S0006-291X(84)71316-7

journal_volume

199

pub_type

杂志文章

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