| Nicotinic acids: Liver-targeted SCD inhibitors with preclinical anti-diabetic efficacy. | |
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MedLine Citation:
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PMID: 22047692 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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An in vitro screening protocol was used to transform a systemically-distributed SCD inhibitor into a liver-targeted compound. Incorporation of a key nicotinic acid moiety enables molecular recognition by OATP transporters, as demonstrated by uptake studies in transfected cell lines, and likely serves as a critical component of the observed liver-targeted tissue distribution profile. Preclinical anti-diabetic oGTT efficacy is demonstrated with nicotinic acid-based, liver-targeting SCD inhibitor 10, and studies with a close-structural analog devoid of SCD1 activity, suggest this efficacy is a result of on-target activity. |
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Authors:
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David A Powell; W Cameron Black; Kelly Bleasby; Chi-Chung Chan; Denis Deschenes; Marc Gagnon; Rob Gordon; Jocelyne Guay; Sebastien Guiral; Michael J Hafey; Zheng Huang; Elise Isabel; Yves Leblanc; Angela Styhler; Li-Jing Xu; Lei Zhang; Renata M Oballa |
Publication Detail:
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Type: JOURNAL ARTICLE Date: 2011-10-18 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry letters Volume: - ISSN: 1464-3405 ISO Abbreviation: - Publication Date: 2011 Oct |
Date Detail:
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Created Date: 2011-11-3 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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Merck Frosst Centre for Therapeutic Research, 16711 Trans Canada Highway, Kirkland, Québec, Canada H9H 3L1. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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