| High-Throughput Screening of Potassium-Competitive Acid Blockers. | |
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MedLine Citation:
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PMID: 21940711 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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H(+),K(+)-ATPase is a key enzyme in the process of gastric acid secretion, and proton pump inhibitors (PPIs) have been accepted as one of the most effective treatments for peptic ulcer and gastroesophageal reflux disease. To discover a novel class of PPIs, the authors screened a low-molecular-weight compound library and identified two prospective acid blockers that were pyrrole derivatives. Both compounds inhibited H(+),K(+)-ATPase in a reversible and potassium-competitive manner. These compounds led to the development of TAK-438 (1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine monofumarate), which is currently undergoing clinical trials as a novel potassium-competitive acid blocker for the treatment of acid-related diseases. |
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Authors:
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Mitsuyo Kondo; Makiko Kawamoto; Atsushi Hasuoka; Masahiro Kajino; Nobuhiro Inatomi; Naoki Tarui |
Publication Detail:
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Type: JOURNAL ARTICLE Date: 2011-9-22 |
Journal Detail:
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Title: Journal of biomolecular screening Volume: - ISSN: 1552-454X ISO Abbreviation: - Publication Date: 2011 Sep |
Date Detail:
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Created Date: 2011-9-23 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9612112 Medline TA: J Biomol Screen Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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