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A model of reversible inhibitors in the gastric H+/K+-ATPase binding site determined by rotational echo double resonance NMR.

Abstract:

Several close analogues of the noncovalent H(+)/K(+)-ATPase inhibitor SCH28080 (2-methyl-3-cyanomethyl-8-(phenylmethoxy)imidazo[1,2-a]pyridine) have been screened for activity and examined in the pharmacological site of action by solid-state NMR spectroscopy. TMPIP, the 1,2,3-trimethyl analogue of SCH28080, and variants of TMPIP containing fluorine in the phenylmethoxy ring exhibited IC(50) values for porcine H(+)/K(+)-ATPase inhibition falling in the sub-10 microm range. Deuterium NMR spectr...

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Publication status:
Published

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Publisher copy:
10.1074/jbc.m104808200

Authors


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Institution:
University of Oxford
Department:
Oxford, MSD, Biochemistry
Middleton, DA More by this author
Journal:
The Journal of biological chemistry
Volume:
276
Issue:
46
Pages:
43197-43204
Publication date:
2001-11-05
DOI:
EISSN:
1083-351X
ISSN:
0021-9258
URN:
uuid:c0089a51-5539-4e5d-8603-efae9f57bb55
Source identifiers:
100334
Local pid:
pubs:100334

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