Gastric (H+ + K+)-ATPase: modulation of the inhibitory properties of the novel potent antisecretagogue Ro 18-5364 by sulfhydryl reagents and nucleotides.

Abstract:

:The sulfoxide Ro 18-5364, a potential metabolite of the IND Ro 18-5362, is a powerful inhibitor of gastric mucosal (H+ + K+)-ATPase, decreasing enzymatic activity with an apparent Ki of 0.1 microM. Exposure of Ro 18-5364-treated gastric membranes to dithiothreitol fully restored (H+ + K+)-ATPase activity. ATP protected the enzyme against Ro 18-5364-induced inactivation of enzymatic activity. In addition, Ro 18-5364 inhibited vesicular proton uptake. In proton translocation experiments reduced lipoic acid methyl ester partially restored transport properties. Dithiothreitol and mercaptoethanol were without effect. The results are discussed with respect to the possible location of essential sulfhydryl groups for enzyme activity and proton transport.

journal_name

FEBS Lett

journal_title

FEBS letters

authors

Sigrist-Nelson K,Müller RK,Fischli AE

doi

10.1016/0014-5793(86)80324-6

subject

Has Abstract

pub_date

1986-03-03 00:00:00

pages

187-91

issue

1-2

eissn

0014-5793

issn

1873-3468

pii

0014-5793(86)80324-6

journal_volume

197

pub_type

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