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Literature summary extracted from

  • Feighery, L.M.; Cochrane, S.W.; Quinn, T.; Baird, A.W.; OToole, D.; Owens, S.E.; ODonoghue, D.; Mrsny, R.J.; Brayden, D.J.
    Myosin light chain kinase inhibition: correction of increased intestinal epithelial permeability in vitro (2008), Pharm. Res., 25, 1377-1386.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
2.7.11.18 Calmodulin dependent on Mus musculus
2.7.11.18 Calmodulin dependent on Homo sapiens
2.7.11.18 Calmodulin dependent on Rattus norvegicus

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.18 ML-7 i.e. 1-(5-iodonaphthalene-1-sulfonyl)-1H-hexahydro-1,4-diazepine Homo sapiens
2.7.11.18 ML-7 i.e. 1-(5-iodonaphthalene-1-sulfonyl)-1H-hexahydro-1,4-diazepine Mus musculus
2.7.11.18 ML-7 i.e. 1-(5-iodonaphthalene-1-sulfonyl)-1H-hexahydro-1,4-diazepine Rattus norvegicus
2.7.11.18 ML-9 i.e. 1-(5-chloronaphthalene-1-sulfonyl)-1H-hexahydro-1,4-diazepine, inhibits MLCK and paracellular permeability increases in several intestinal epithelial models Homo sapiens
2.7.11.18 ML-9 i.e. 1-(5-chloronaphthalene-1-sulfonyl)-1H-hexahydro-1,4-diazepine, inhibits MLCK and paracellular permeability increases in several intestinal epithelial models Mus musculus
2.7.11.18 ML-9 i.e. 1-(5-chloronaphthalene-1-sulfonyl)-1H-hexahydro-1,4-diazepine, inhibits MLCK and paracellular permeability increases in several intestinal epithelial models Rattus norvegicus
2.7.11.18 additional information inhibitor effects on enzyme activity in intestinal tissues, overview Homo sapiens
2.7.11.18 additional information inhibitor effects on enzyme activity in intestinal tissues, overview Mus musculus
2.7.11.18 additional information inhibitor effects on enzyme activity in intestinal tissues, overview Rattus norvegicus
2.7.11.18 RKKYKYRRK-NH2 i.e. D PIK Homo sapiens
2.7.11.18 RKKYKYRRK-NH2 i.e. D PIK Mus musculus
2.7.11.18 RKKYKYRRK-NH2
-
Rattus norvegicus

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.7.11.18 Ca2+ dependent on Mus musculus
2.7.11.18 Ca2+ dependent on Homo sapiens
2.7.11.18 Ca2+ dependent on Rattus norvegicus
2.7.11.18 Mg2+
-
Mus musculus
2.7.11.18 Mg2+
-
Homo sapiens
2.7.11.18 Mg2+
-
Rattus norvegicus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.11.18 ATP + myosin light chain Mus musculus
-
ADP + myosin light chain phosphate
-
?
2.7.11.18 ATP + myosin light chain Homo sapiens
-
ADP + myosin light chain phosphate
-
?
2.7.11.18 ATP + myosin light chain Rattus norvegicus
-
ADP + myosin light chain phosphate
-
?
2.7.11.18 ATP + myosin light chain Mus musculus C57BL/6
-
ADP + myosin light chain phosphate
-
?
2.7.11.18 additional information Homo sapiens cytochalasin-induced increases in paracellular permeability are also mediated by MLC in Caco-2 monolayers ?
-
?

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.18 Homo sapiens
-
-
-
2.7.11.18 Mus musculus
-
C57BL/6 mice
-
2.7.11.18 Mus musculus C57BL/6
-
C57BL/6 mice
-
2.7.11.18 Rattus norvegicus
-
adult male Wistar rats
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.11.18 Caco-2 cell
-
Homo sapiens
-
2.7.11.18 colon
-
Mus musculus
-
2.7.11.18 colon
-
Rattus norvegicus
-
2.7.11.18 colon from patients who had not been treated with chemotherapy or radiotherapy, freshlys collected at the time of surgical resection for malignant or non-inflammatory disease Homo sapiens
-
2.7.11.18 epithelium
-
Mus musculus
-
2.7.11.18 epithelium
-
Homo sapiens
-
2.7.11.18 epithelium
-
Rattus norvegicus
-
2.7.11.18 intestine mucosa Mus musculus
-
2.7.11.18 intestine mucosa Homo sapiens
-
2.7.11.18 intestine mucosa Rattus norvegicus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.18 ATP + myosin light chain
-
Mus musculus ADP + myosin light chain phosphate
-
?
2.7.11.18 ATP + myosin light chain
-
Homo sapiens ADP + myosin light chain phosphate
-
?
2.7.11.18 ATP + myosin light chain
-
Rattus norvegicus ADP + myosin light chain phosphate
-
?
2.7.11.18 ATP + myosin light chain
-
Mus musculus C57BL/6 ADP + myosin light chain phosphate
-
?
2.7.11.18 additional information cytochalasin-induced increases in paracellular permeability are also mediated by MLC in Caco-2 monolayers Homo sapiens ?
-
?

Synonyms

EC Number Synonyms Comment Organism
2.7.11.18 MLC kinase
-
Mus musculus
2.7.11.18 MLC kinase
-
Homo sapiens
2.7.11.18 MLC kinase
-
Rattus norvegicus
2.7.11.18 MLCK
-
Mus musculus
2.7.11.18 MLCK
-
Homo sapiens
2.7.11.18 MLCK
-
Rattus norvegicus
2.7.11.18 myosin light chain kinase
-
Mus musculus
2.7.11.18 myosin light chain kinase
-
Homo sapiens
2.7.11.18 myosin light chain kinase
-
Rattus norvegicus

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.11.18 ATP
-
Mus musculus
2.7.11.18 ATP
-
Homo sapiens
2.7.11.18 ATP
-
Rattus norvegicus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.11.18 0.029
-
-
Homo sapiens RKKYKYRRK-NH2