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Literature summary for 2.7.11.18 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

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

Inhibitors

Inhibitors Comment Organism Structure
ML-7 i.e. 1-(5-iodonaphthalene-1-sulfonyl)-1H-hexahydro-1,4-diazepine Homo sapiens
ML-7 i.e. 1-(5-iodonaphthalene-1-sulfonyl)-1H-hexahydro-1,4-diazepine Mus musculus
ML-7 i.e. 1-(5-iodonaphthalene-1-sulfonyl)-1H-hexahydro-1,4-diazepine Rattus norvegicus
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
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
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
additional information inhibitor effects on enzyme activity in intestinal tissues, overview Homo sapiens
additional information inhibitor effects on enzyme activity in intestinal tissues, overview Mus musculus
additional information inhibitor effects on enzyme activity in intestinal tissues, overview Rattus norvegicus
RKKYKYRRK-NH2 i.e. D PIK Homo sapiens
RKKYKYRRK-NH2 i.e. D PIK Mus musculus
RKKYKYRRK-NH2
-
Rattus norvegicus

Metals/Ions

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

Natural Substrates/ Products (Substrates)

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

Organism

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

Source Tissue

Source Tissue Comment Organism Textmining
Caco-2 cell
-
Homo sapiens
-
colon
-
Mus musculus
-
colon
-
Rattus norvegicus
-
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
-
epithelium
-
Mus musculus
-
epithelium
-
Homo sapiens
-
epithelium
-
Rattus norvegicus
-
intestine mucosa Mus musculus
-
intestine mucosa Homo sapiens
-
intestine mucosa Rattus norvegicus
-

Substrates and Products (Substrate)

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

Synonyms

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

Cofactor

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

IC50 Value

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