| Discovery of BI 99179, a potent and selective inhibitor of type I fatty acid synthase with central exposure. | |
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MedLine Citation:
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PMID: 21873051 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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Based on a high-throughput screen, cyclopentanecarboxanilides were identified as a new chemotype of non-covalent inhibitors of type I fatty acid synthase (FAS). Starting from initial hits we aimed at generating a tool compound suitable for the in vivo validation of FAS as a therapeutic target. Optimisation yielded BI 99179 which is characterised by high potency, remarkably high selectivity and significant exposure (both peripheral and central) upon oral administration in rats. |
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Authors:
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Jörg T Kley; Jürgen Mack; Bradford Hamilton; Stefan Scheuerer; Norbert Redemann |
Publication Detail:
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Type: JOURNAL ARTICLE Date: 2011-8-9 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry letters Volume: - ISSN: 1464-3405 ISO Abbreviation: - Publication Date: 2011 Aug |
Date Detail:
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Created Date: 2011-8-29 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9107377 Medline TA: Bioorg Med Chem Lett 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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Medicinal Chemistry, Boehringer Ingelheim Pharma GmbH & Co. KG, Birkendorfer Strasse 65, D-88397 Biberach, Germany. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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