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Literature summary for 3.4.21.34 extracted from

  • Stoop, A.A.; Joshi, R.V.; Eggers, C.T.; Craik, C.S.
    Analysis of an engineered plasma kallikrein inhibitor and its effect on contact activation (2010), Biol. Chem., 391, 425-433.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
ecotin ecotin with mutation H53P in the 50s loop, mutations S82W/T83N/M84R/M85R/A86S in the 80s loop and mutations R108S/N110S in the 100s loop is a high-affinity and highly specific plasma kallikrein inhibitor. Specifically inhibits contact activation of human plasma at the level mediated by plasma kallikrein. Discriminates between enzyme and zymogen. Partial thromboplastin time inhibition can be rescued by addition of PKal Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Pro-Phe-Arg-7-amido-4-methylcoumarin + H2O
-
Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
PKal
-
Homo sapiens
plasma kallikrein
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000000011
-
ecotin ecotin with mutation H53P in the 50s loop, mutations S82W/T83N/M84R/M85R/A86S in the 80s loop and mutations R108S/N110S in the 100s loop, at room temperature Homo sapiens
0.000000014
-
ecotin ecotin with mutation H53P in the 50s loop and mutations S82W/T83N/M84R/M85R/A86S in the 80s loop, at room temperature Homo sapiens
0.000000025
-
ecotin ecotin with mutations S82W/T83N/M84R/M85R/A86S in the 80s loop and mutations R108S/N110S in the 100s loop, at room temperature Homo sapiens
0.000000037
-
ecotin ecotin with mutations S82W/T83N/M84R/M85R/A86S in the 80s loop, at room temperature Homo sapiens
0.000000066
-
ecotin wild-type ecotin, at room temperature Homo sapiens
0.000000097
-
ecotin ecotin with mutation H53P in the 50s loop, at room temperature Homo sapiens
0.000000118
-
ecotin ecotin with mutations R108S/N110S in the 100s loop, at room temperature Homo sapiens
0.000000186
-
ecotin ecotin with mutation H53P in the 50s loop and mutations R108S/N110S in the 100s loop, at room temperature Homo sapiens