Literature summary for 3.4.21.21 extracted from

Olivero, A.G.; Eigenbrot, C.; Goldsmith, R.; Robarge, K.; Artis, D.R.; Flygare, J.; Rawson, T.; Sutherlin, D.P.; Kadkhodayan, S.; Beresini, M.; Elliott, L.O.; DeGuzman, G.G.; Banner, D.W.; Ultsch, M.; Marzec, U.; Hanson, S.R.; Refino, C.; Bunting, S.; Kirchhofer, D.
A selective, slow binding inhibitor of factor VIIa binds to a nonstandard active site conformation and attenuates thrombus formation in vivo (2005), J. Biol. Chem., 280, 9160-9169.

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Crystallization (Commentary)

Crystallization (Comment)	Organism
hanging drop vapour diffusion method	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
R-4-[2-(3-aminobenzenesulfonylamino)-1-(3,5-diethoxy-2-fluorophenyl)-2-oxoethylamino]-2-hydroxy-benzamidine	incubation with enzyme in 100 mM Hepes, pH 7.8, 140 mM NaCl, 0.1% (v/v) polyethylene glycol 8000, 0.02% (v/v) Tween 80, 5 mM CaCl2 for 40 min at room temperature	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	P08709	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
factor X + H2O	-	Homo sapiens	factor Xa	-	?
N-methylsulfonyl-D-phenyl-D-glycyl-D-arginyl-4-nitroanilide + H2O	-	Homo sapiens	N-methylsulfonyl-D-phenyl-D-glycyl-D-arginine + 4-nitroaniline	-	?

Synonyms

Synonyms	Comment	Organism
FVIIa	-	Homo sapiens
serine protease factor VIIa	-	Homo sapiens
TF-FVIIa	factor VIIa in complex with tissue factor	Homo sapiens

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
0.00000035	-	R-4-[2-(3-aminobenzenesulfonylamino)-1-(3,5-diethoxy-2-fluorophenyl)-2-oxoethylamino]-2-hydroxy-benzamidine	-	Homo sapiens

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Release 2023.1 (January 2023)