Please use this identifier to cite or link to this item: https://doi.org/10.21256/zhaw-1689
Publication type: Article in scientific journal
Type of review: Peer review (publication)
Title: Cover picture : targeted fluoro positioning for the discovery of a potent and highly selective matrix metalloproteinase inhibitor (ChemistryOpen 2/2017)
Authors: Fischer, Thomas
Riedl, Rainer
DOI: 10.1002/open.201700043
10.21256/zhaw-1689
Published in: ChemistryOpen
Volume(Issue): 6
Issue: 2
Page(s): 165
Issue Date: 2017
Publisher / Ed. Institution: Wiley
ISSN: 2191-1363
Language: English
Subjects: Medicinal chemistry; Drug discovery; Drug design
Subject (DDC): 572: Biochemistry
615: Pharmacology and therapeutics
Abstract: The Front Cover picture shows the design of the highly potent and selective inhibitor ZHAWOC5684 bound to its target protein matrix metalloproteinase-13 (MMP-13). The key design principle involves the structure-based positioning of a single fluorine atom to probe water-mediated interactions within the allosteric binding site. In combination with a zinc-binding carboxylic acid fragment blocking the active site this approach delivers a drug-like small molecule inhibitor of MMP-13 with excellent microsomal and plasma stability.
Further description: Zugehöriger Artikel: https://digitalcollection.zhaw.ch/handle/11475/2857
URI: https://digitalcollection.zhaw.ch/handle/11475/2859
Fulltext version: Published version
License (according to publishing contract): CC BY-NC-ND 4.0: Attribution - Non commercial - No derivatives 4.0 International
Departement: Life Sciences and Facility Management
Organisational Unit: Institute of Chemistry and Biotechnology (ICBT)
Appears in collections:Publikationen Life Sciences und Facility Management

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Fischer, T., & Riedl, R. (2017). Cover picture : targeted fluoro positioning for the discovery of a potent and highly selective matrix metalloproteinase inhibitor (ChemistryOpen 2/2017). ChemistryOpen, 6(2), 165. https://doi.org/10.1002/open.201700043
Fischer, T. and Riedl, R. (2017) ‘Cover picture : targeted fluoro positioning for the discovery of a potent and highly selective matrix metalloproteinase inhibitor (ChemistryOpen 2/2017)’, ChemistryOpen, 6(2), p. 165. Available at: https://doi.org/10.1002/open.201700043.
T. Fischer and R. Riedl, “Cover picture : targeted fluoro positioning for the discovery of a potent and highly selective matrix metalloproteinase inhibitor (ChemistryOpen 2/2017),” ChemistryOpen, vol. 6, no. 2, p. 165, 2017, doi: 10.1002/open.201700043.
FISCHER, Thomas und Rainer RIEDL, 2017. Cover picture : targeted fluoro positioning for the discovery of a potent and highly selective matrix metalloproteinase inhibitor (ChemistryOpen 2/2017). ChemistryOpen. 2017. Bd. 6, Nr. 2, S. 165. DOI 10.1002/open.201700043
Fischer, Thomas, and Rainer Riedl. 2017. “Cover Picture : Targeted Fluoro Positioning for the Discovery of a Potent and Highly Selective Matrix Metalloproteinase Inhibitor (ChemistryOpen 2/2017).” ChemistryOpen 6 (2): 165. https://doi.org/10.1002/open.201700043.
Fischer, Thomas, and Rainer Riedl. “Cover Picture : Targeted Fluoro Positioning for the Discovery of a Potent and Highly Selective Matrix Metalloproteinase Inhibitor (ChemistryOpen 2/2017).” ChemistryOpen, vol. 6, no. 2, 2017, p. 165, https://doi.org/10.1002/open.201700043.


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