Literature summary for 3.4.21.5 extracted from

Nogami, K.; Zhou, Q.; Myles, T.; Leung, L.L.; Wakabayashi, H.; Fay, P.J.
Exosite-interactive regions in the A1 and A2 domains of factor VIII facilitate thrombin-catalyzed cleavage of heavy chain (2005), J. Biol. Chem., 280, 18476-18487.

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Inhibitors

Inhibitors	Comment	Organism	Structure
heparin	blocks enzyme interaction with A2 subunit of substrate factor VIII	Homo sapiens
Hirudin	blocks interaction of enzyme with A1 subunit of substrate factor VIII	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
factor VIII + H2O	high affinity site in A1 subunit of substrate, dependent on Na+-bound form of enzyme. Moderate affinity site in A2 subunit, independent of Na+-state of enzyme	Homo sapiens	factor VIIIa + propeptide	-	?
factor VIII mutant D392A/D394A + H2O	reduction in specific activity similar to a severe hemophilia phenotype. No cleavage at R740, while cleavage at R372 is not affected	Homo sapiens	?	-	?

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Release 2023.1 (January 2023)