| 4-Substituted boro-proline dipeptides: Synthesis, characterization, and dipeptidyl peptidase IV, 8, and 9 activities. | |
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MedLine Citation:
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PMID: 22853995 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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The boroProline-based dipeptidyl boronic acids were among the first DPP-IV inhibitors identified, and remain the most potent known. We introduced various substitutions at the 4-position of the boroProline ring regioselectively and stereoselectively, and incorporated these aminoboronic acids into a series of 4-substituted boroPro-based dipeptides. Among these dipeptidyl boronic acids, Arg-(4S)-boroHyp (4q) was the most potent inhibitor of DPP-IV, DPP8 and DPP9, while (4S)-Hyp-(4R)-boroHyp (4o) exhibited the most selectivity for DPP-IV over DPP8 and DPP9. |
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Authors:
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Wengen Wu; Yuxin Liu; Lawrence J Milo; Ying Shu; Peng Zhao; Youhua Li; Iwona Woznica; Gengli Yu; David G Sanford; Yuhong Zhou; Sarah E Poplawski; Beth A Connolly; James L Sudmeier; William W Bachovchin; Jack H Lai |
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Publication Detail:
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Type: JOURNAL ARTICLE Date: 2012-7-14 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry letters Volume: - ISSN: 1464-3405 ISO Abbreviation: Bioorg. Med. Chem. Lett. Publication Date: 2012 Jul |
Date Detail:
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Created Date: 2012-8-2 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 © 2012 Elsevier Ltd. All rights reserved. |
Affiliation:
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Tufts University School of Medicine, Department of Biochemistry, 136 Harrison Ave., Boston, MA 02111, United States. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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