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Literature summary for 3.4.21.75 extracted from

  • Basak, A.; Khatib, A.M.; Mohottalage, D.; Basak, S.; Kolajova, M.; Bag, S.S.; Basak, A.
    A novel enediynyl peptide inhibitor of furin that blocks processing of proPDGF-A, B and proVEGF-C (2009), PLoS ONE, 4, e7700.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.21.75

Application

Application Comment Organism
drug development furin is considered a major target for intervention of cancer, tumorgenesis, viral and bacterial pathogenesis Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1,2,12,13-tetradehydro-3,4,10,11-tetrahydro-5,9-(azeno)-4,10-benzodiazacyclopentadecine 12% inhibition at 0.1 mM Homo sapiens
1,2,12,13-tetradehydro-3,4,10,11-tetrahydro-5,9-(metheno)-4,10-benzodiazacyclopentadecine 10% inhibition at 0.1 mM Homo sapiens
4,10-bis[(4-methylphenyl)sulfonyl]-1,2,12,13-tetradehydro-3,4,10,11-tetrahydro-5,9-(metheno)-4,10-benzodiazacyclopentadecine
-
 Homo sapiens
4,7-dibenzyl-1,2,9,10-tetradehydro-3,4,5,6,7,8-hexahydro-4,7-benzodiazacyclododecine
-
 Homo sapiens
8,11,22,25-tetrabenzyl-5,6,13,14,19,20,27,28-octadehydro-7,8,9,10,11,12,21,22,23,24,25,26-dodecahydrodibenzo[h,t][1,4,13,16]tetraazacyclotetracosine
-
 Homo sapiens
furin-Eda peptide acyclic synthesis, overview. Designed a potent furin inhibitor that contains a highly reactive beta-turn inducing and radical generating enediynyl amino acid moiety, which is inserted between P1 and P19 residues of hfurin98-112 peptide, derived from the primary cleavage site of furin's own prodomain. The inhibitor displays a predominantly beta-turn structure. The inhibitor protects furin protein from self degradation Homo sapiens
furin-Eda peptide cyclic synthesis, overview Homo sapiens
additional information synthetic aromatic enediyne derivatives and their effects on protease activity of proprotein convertases furin, overview Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Ca2+ dependent on Homo sapiens

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
55000
-
 x * 55000, soluble furin, SDS-PAGE Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2-amino benzoyl-AEQDRNTREVFAQ-T(3-nitro-tyrosine)-A + H2O furin-mediated cleavage of a fluorogenic peptide derived from hSARS-CoV spike protein Homo sapiens 2-amino benzoyl-AEQDRNTR + EVFAQ-T(3-nitro-tyrosine)-A
-
 ?
Boc-RVRR-4-methylcoumarin 7-amide + H2O
-
 Homo sapiens Boc-RVRR + 7-amino-4-methylcoumarin
-
 ?
additional information furin performs autocleaqvage to its soluble form Homo sapiens ?
-
 ?
proPDGF-A + H2O a growth factor proform Homo sapiens PDGF-A + PGDF-A propeptide
-
 ?
proPDGF-B + H2O a growth factor proform of 31 kDa Homo sapiens PDGF-B + PGDF-B propeptide mature form of 17 kDa ?
proVEGF-C + H2O a growth factor proform Homo sapiens VEGF-C + VEGF-C propeptide
-
 ?

Subunits

Subunits Comment Organism
? x * 55000, soluble furin, SDS-PAGE Homo sapiens

Synonyms

Synonyms Comment Organism
More furin is a crucial member of secretory mammalian subtilase, the proprotein convertase or proprotein convertase subtilisin/kexin, PCSK, superfamily Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000105
-
-
 Homo sapiens 4,7-dibenzyl-1,2,9,10-tetradehydro-3,4,5,6,7,8-hexahydro-4,7-benzodiazacyclododecine
0.0000142
-
-
 Homo sapiens 4,10-bis[(4-methylphenyl)sulfonyl]-1,2,12,13-tetradehydro-3,4,10,11-tetrahydro-5,9-(metheno)-4,10-benzodiazacyclopentadecine
0.00004
-
 versus substrate N-benzyloxy-RVRR-4-methylcoumarin 7-amide Homo sapiens furin-Eda peptide acyclic
0.00004
-
 versus substrate N-benzyloxy-RVRR-4-methylcoumarin 7-amide, pH not specified in the publication, temperature not specified in the publication Homo sapiens furin-Eda peptide acyclic
0.00016
-
-
 Homo sapiens 8,11,22,25-tetrabenzyl-5,6,13,14,19,20,27,28-octadehydro-7,8,9,10,11,12,21,22,23,24,25,26-dodecahydrodibenzo[h,t][1,4,13,16]tetraazacyclotetracosine
0.000192
-
-
 Homo sapiens 8,11,22,25-tetrabenzyl-5,6,13,14,19,20,27,28-octadehydro-7,8,9,10,11,12,21,22,23,24,25,26-dodecahydrodibenzo[h,t][1,4,13,16]tetraazacyclotetracosine
0.000193
-
 versus substrate fluorogenic peptide derived from hSARS-CoV spike protein Homo sapiens furin-Eda peptide cyclic
0.000193
-
 versus substrate fluorogenic peptide derived from hSARS-CoV spike protein, pH not specified in the publication, temperature not specified in the publication Homo sapiens furin-Eda peptide acyclic

General Information

General Information Comment Organism
malfunction furin is linked to cancer, tumorgenesis, and viral and bacterial pathogenesis Homo sapiens