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Literature summary for 3.4.21.75 extracted from

  • Dahms, S.O.; Jiao, G.S.; Than, M.E.
    Structural studies revealed active site distortions of human furin by a small molecule inhibitor (2017), ACS Chem. Biol., 12, 1211-1216 .
    View publication on PubMed

Crystallization (Commentary)

Crystallization (Comment) Organism
purified furin in complex with a non-substrate-like small molecule inhibitor N,N'-[[(1S,3R,4R,6S)-4-carbamimidamido-6-(4-carbamimidamidoanilino)cyclohexane-1,3-diyl]bis(oxy-4,1-phenylene)]diguanidine, hexagonal crystals of unliganded furin are soaked in a 5 mM solution of inhibitor in 100 mM MES, pH 5.5, 200 mM K/NaH2PO4, 1 mM CaCl2, 10% DMSO, and 3.4 mM NaCl for 16 h, X-ray diffraction structure determination and analysis at 1.9 A resolution Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1,1'-((1R,3S,4S,6R)-4,6-bis(4-guanidinophenoxy)cyclohexane-1,3-diyl)diguanidine meso compound Homo sapiens
1,1'-((1R,3S,4S,6R)-4-((4-guanidinonaphthalen-1-yl)oxy)-6-(4-guanidinophenoxy)cyclohexane-1,3-diyl)diguanidine racemate, blocks the S2 pocket Homo sapiens
1,1'-((1S,3R,4R,6S)-4-((4-guanidinonaphthalen-1-yl)oxy)-6-(4-guanidinophenoxy)cyclohexane-1,3-diyl)diguanidine blocks the S2 pocket Homo sapiens
additional information active site distortions of human furin by a small molecule inhibitor N,N'-[[(1S,3R,4R,6S)-4-carbamimidamido-6-(4-carbamimidamidoanilino)cyclohexane-1,3-diyl]bis(oxy-4,1-phenylene)]diguanidine, analysis of binding structures of noncovalent 2,5-dideoxystreptamine-derived furin inhibitors, overview Homo sapiens
N,N'-[[(1R,3S,4S,6R)-4-carbamimidamido-6-(4-carbamimidamidoanilino)cyclohexane-1,3-diyl]bis(oxy-4,1-phenylene)]diguanidine racemate, interferes directly with the catalytic competent conformation of the catalytic triad. Inhibition mechanism, overview Homo sapiens
N,N'-[[(1S,3R,4R,6S)-4-carbamimidamido-6-(4-carbamimidamidoanilino)cyclohexane-1,3-diyl]bis(oxy-4,1-phenylene)]diguanidine interferes directly with the catalytic competent conformation of the catalytic triad. Inhibition mechanism, overview Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Ca2+ required Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens proprotein convertases represent highly selective serine proteases that activate their substrates upon proteolytic cleavage ?
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?

Organism

Organism UniProt Comment Textmining
Homo sapiens P09958
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-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information proprotein convertases represent highly selective serine proteases that activate their substrates upon proteolytic cleavage Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
Proprotein convertase
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Homo sapiens