Novel Furin Inhibitors with Potent Anti-infectious Activity

New peptidomimetic furin inhibitors with unnatural amino acid residues in the P3 position were synthesized. The most potent compound 4‐guanidinomethyl‐phenylacteyl‐Arg‐Tle‐Arg‐4‐amidinobenzylamide (MI‐1148) inhibits furin with a Ki value of 5.5 pM. The derivatives also strongly inhibit PC1/3, wherea...

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Veröffentlicht in:	ChemMedChem 2015-07, Vol.10 (7), p.1218-1231
Hauptverfasser:	Hardes, Kornelia, Becker, Gero L., Lu, Yinghui, Dahms, Sven O., Köhler, Susanne, Beyer, Wolfgang, Sandvig, Kirsten, Yamamoto, Hiroyuki, Lindberg, Iris, Walz, Lisa, von Messling, Veronika, Than, Manuel E., Garten, Wolfgang, Steinmetzer, Torsten
Format:	Artikel
Sprache:	eng
Schlagworte:	Amino acids antiviral agents Antiviral Agents - chemistry Antiviral Agents - pharmacology Canine distemper virus crystal structure analysis Distemper Virus, Canine - drug effects Dose-Response Relationship, Drug Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology furin Furin - antagonists & inhibitors Furin - metabolism Humans Influenza Influenza A virus - drug effects inhibitors Microbial Sensitivity Tests Molecular Structure proprotein convertases Structure-Activity Relationship
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