| Amides of xanthurenic acid as zinc-dependent inhibitors of Lp-PLA(2). | |
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MedLine Citation:
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PMID: 22217870 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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AX10185, the phenyl amide of xanthurenic acid, was found to be a sub-100nM inhibitor of Lp-PLA(2). However, in the presence of EDTA the inhibitory activity of AX10185 was extinguished while the enzymatic activity of Lp-PLA(2) did not change. Subsequent metal screening experiments determined the inhibition to be Zn(2+) dependent. Structure-activity relationship studies indicated the presence of the 4-hydroxy group to be critical and selected substituted phenyl, polycyclic, and cycloaliphatic amides of xanthurenic acid to be well tolerated. |
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Authors:
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Emme C K Lin; Yi Hu; Christopher M Amantea; Lan M Pham; Julia Cajica; Eric Okerberg; Heidi E Brown; Allister Fraser; Lingling Du; Yasushi Kohno; Junichi Ishiyama; John W Kozarich; Kevin R Shreder |
Publication Detail:
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Type: JOURNAL ARTICLE Date: 2011-12-13 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry letters Volume: - ISSN: 1464-3405 ISO Abbreviation: - Publication Date: 2011 Dec |
Date Detail:
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Created Date: 2012-1-5 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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ActivX Biosciences, Inc., 11025 N. Torrey Pines Road, La Jolla, CA 92037, USA. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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