| NSAID-derived γ-secretase modulation requires an acidic moiety on the carbazole scaffold. | |
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MedLine Citation:
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PMID: 21763147 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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Modulation of γ-secretase activity holds potential for the treatment of Alzheimer's disease. Most NSAID-derived γ-secretase modulators feature a carboxylic acid, which may impair blood-brain barrier permeation. The structure activity relationship of 33 carbazoles featuring diverse carboxylic acid isosteres or metabolic precursors thereof was established in a cellular amyloid secretion assay. The modulatory activity was observed for acidic moieties and metabolically labile esters only, which supports our hypothesis of an acid-lysine interaction to be relevant for this type of γ-secretase modulators. |
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Authors:
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Andrea Zall; Daniel Kieser; Nicole Höttecke; Eva C Naumann; Binia Thomaszewski; Katrin Schneider; Dirk T Steinbacher; Robert Schubenel; Stefan Masur; Karlheinz Baumann; Boris Schmidt |
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Publication Detail:
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Type: JOURNAL ARTICLE Date: 2011-6-29 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry Volume: - ISSN: 1464-3391 ISO Abbreviation: - Publication Date: 2011 Jun |
Date Detail:
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Created Date: 2011-7-18 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9413298 Medline TA: Bioorg Med Chem Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Copyright Information:
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Copyright © 2011 Elsevier Ltd. All rights reserved. |
Affiliation:
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Clemens Schöpf-Institute of Chemistry and Biochemistry, Technische Universität Darmstadt, Petersenstr. 22, Darmstadt D-64287, Germany. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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