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 Lettjournal_title
FEBS lettersauthors
Sigrist-Nelson K,Müller RK,Fischli AEdoi
10.1016/0014-5793(86)80324-6subject
Has Abstractpub_date
1986-03-03 00:00:00pages
187-91issue
1-2eissn
0014-5793issn
1873-3468pii
0014-5793(86)80324-6journal_volume
197pub_type
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