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Optimization of Substrate‐Analogue Furin Inhibitors
ChemMedChem, 2017AbstractThe proprotein convertase furin is a potential target for drug design, especially for the inhibition of furin‐dependent virus replication. All effective synthetic furin inhibitors identified thus far are multibasic compounds; the highest potency was found for our previously developed inhibitor 4‐(guanidinomethyl)phenylacetyl‐Arg‐Tle‐Arg‐4 ...
Teodora Ivanova +10 more
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Precursor Processing by Kex2/Furin Proteases
ChemInform, 2002AbstractFor Abstract see ChemInform Abstract in Full Text.
Nathan C, Rockwell +3 more
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Internally Quenched Fluorogenic Substrate for Furin
Analytical Biochemistry, 1995A new substrate for furin, Abz-Arg-Val-Lys-Arg-Gly-Leu-Ala-Tyr(NO2)-Asp-OH, has been synthesized and characterized. The peptide is an internally quenched fluorogenic substrate. The kinetic parameters are Km = 3.8 microM, kcat = 29.3 s-1, and kcat/KM = 7,710,000 M-1 s-1.
H, Angliker +3 more
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Journal of Medicinal Chemistry, 2021
Analysis of the SARS-CoV-2 sequence revealed a multibasic furin cleavage site at the S1/S2 boundary of the spike protein distinguishing this virus from SARS-CoV. Furin, the best-characterized member of the mammalian proprotein convertases, is an ubiquitously expressed single pass type 1 transmembrane protein.
Essam Eldin A. Osman +2 more
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Analysis of the SARS-CoV-2 sequence revealed a multibasic furin cleavage site at the S1/S2 boundary of the spike protein distinguishing this virus from SARS-CoV. Furin, the best-characterized member of the mammalian proprotein convertases, is an ubiquitously expressed single pass type 1 transmembrane protein.
Essam Eldin A. Osman +2 more
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Colloquium Series on Protein Activation and Cancer, 2012
Abstract The proprotein convertase Furin is a serine endoprotease which cleaves protein precursors carboxyterminal of basic residues in motifs such as Arg–X–X–Arg and Lys/Arg–Arg. Cleavage usually results in activation of the proprotein but can also inactivate or modify the activity.
Jeroen Declercq, J.W.M. Creemers
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Abstract The proprotein convertase Furin is a serine endoprotease which cleaves protein precursors carboxyterminal of basic residues in motifs such as Arg–X–X–Arg and Lys/Arg–Arg. Cleavage usually results in activation of the proprotein but can also inactivate or modify the activity.
Jeroen Declercq, J.W.M. Creemers
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1994
Abstract Furin is the translation product encoded by the fur locus, which was initially identified by its proximity to the fes/fps proto-oncogene (fes/fps JJ.pstream region)3. Furin cDNAs have been isolated from several species including human, mouse, rat and Xenopus4-8.
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Abstract Furin is the translation product encoded by the fur locus, which was initially identified by its proximity to the fes/fps proto-oncogene (fes/fps JJ.pstream region)3. Furin cDNAs have been isolated from several species including human, mouse, rat and Xenopus4-8.
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[Furin and its biological role].
Ukrains'kyi biokhimichnyi zhurnal (1999 ), 2008The survey deals with structure, properties and biological role of furin, the calcium-dependent serine endoprotease, which is expressed in all tissues and cell lines examined. It is the best-characterized representative of the mammalian subtilisin-like family of proprotein convertases, which is capable to cleave precursors of a wide variety of proteins,
V K, Kibirev +2 more
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[New non-peptide inhibitors of furin].
Ukrains'kyi biokhimichnyi zhurnal (1999 ), 2010Furin, a human subtilisin-related proprotein convertase, is the most important pharmaceutical target because it plays a vital role in development of numerous disease processes. To identify a new class of small non-peptide inhibitors of furin we performed a study of several flavonoids and some natural products.
V K, Kibirev +3 more
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