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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
Published in : ChemistryOpen
Volume(Issue) : 6
Issue : 2
Pages : 165
Publisher / Ed. Institution : Wiley
Issue Date: 2017
License (according to publishing contract) : CC BY-NC-ND 4.0: Namensnennung - Nicht kommerziell - Keine Bearbeitungen 4.0 International
Type of review: Peer review (Publication)
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. More information can be found in the Communication by R. Riedl and T. Fischer on page 192 in Issue 2, 2017 (DOI: 10.1002/open.201600158).
Further description : Zugehöriger Artikel:
Departement: Life Sciences und Facility Management
Organisational Unit: Institute of Chemistry and Biotechnology (ICBT)
Publication type: Article in scientific Journal
DOI : 10.1002/open.201700043
ISSN: 2191-1363
Appears in Collections:Publikationen Life Sciences und Facility Management

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