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Literature summary for 3.4.21.7 extracted from

  • Swedberg, J.E.; Harris, J.M.
    Plasmin substrate binding site cooperativity guides the design of potent peptide aldehyde inhibitors (2011), Biochemistry, 50, 8454-8462.
    View publication on PubMed

Application

Application Comment Organism
medicine antifibrinolytic inhibitors, e.g. aprotinin, of the serine protease plasmin are commonly used to reduce bleeding during surgery Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
Aprotinin
-
Homo sapiens
Lys-Met(sulfone)-Tyr-Arg shows 25fold selectivity for plasmin over plasma kallikrein Homo sapiens
additional information development and evaluation of alternative potent and selective serine lysine analogues to inhibit plasmin, usage of a noncombinatorial peptide library to define plasmin's extended substrate specificity and guide the design of potent transition state analogue inhibitors, molecular modeling, overview Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
additional information plasmin shows substrate binding site cooperativity, Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
commercial preparation
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Ac-FM(O2)YK-4-nitroanilide + H2O peptide substrate, M(O2) i.e. L-methionine sulfone Homo sapiens Ac-FM(O2)YK + 4-nitroaniline M(O2) i.e. L-methionine sulfone ?
Ac-KM(O2)FR-4-nitroanilide + H2O peptide substrate, M(O2) i.e. L-methionine sulfone Homo sapiens Ac-KM(O2)FR + 4-nitroaniline M(O2) i.e. L-methionine sulfone ?
Ac-KM(O2)YR-4-nitroanilide + H2O peptide substrate, M(O2) i.e. L-methionine sulfone Homo sapiens Ac-KM(O2)YR + 4-nitroaniline M(O2) i.e. L-methionine sulfone ?
Ac-RM(O2)WR-4-nitroanilide + H2O peptide substrate, M(O2) i.e. L-methionine sulfone Homo sapiens Ac-RM(O2)WR + 4-nitroaniline M(O2) i.e. L-methionine sulfone ?
Ac-RM(O2)YR-4-nitroanilide + H2O peptide substrate, M(O2) i.e. L-methionine sulfone Homo sapiens Ac-RM(O2)YR + 4-nitroaniline M(O2) i.e. L-methionine sulfone ?
Fibrin + H2O fibrin is formed from fibrinogen by thrombin, EC 3.4.21.5 Homo sapiens ?
-
?
KQWK-4-nitroanilide + H2O peptide substrate Homo sapiens KQWK + 4-nitroaniline
-
?
KTFK-4-nitroanilide + H2O peptide substrate Homo sapiens KTFK + 4-nitroaniline
-
?
additional information plasmin, possessing various substrate binding sites, shows substrate binding site cooperativity, molecular modeling of the plasmin-Ac-RM(O2)YR-H complex Homo sapiens ?
-
?
RQFR-4-nitroanilide + H2O peptide substrate Homo sapiens RQFR + 4-nitroaniline
-
?
RQWK-4-nitroanilide + H2O peptide substrate Homo sapiens RQWK + 4-nitroaniline
-
?
VQYK-4-nitroanilide + H2O peptide substrate Homo sapiens VQYK + 4-nitroaniline
-
?
VQYR-4-nitroanilide + H2O peptide substrate Homo sapiens VQYR + 4-nitroaniline
-
?

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
22 37 assay at 37°C or at room temperature Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4 8 assay at Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000031
-
Lys-Met(sulfone)-Tyr-Arg pH 8.0, 22°C Homo sapiens