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Literature summary extracted from

  • Tinsley, J.H.; Yuan, S.Y.; Wilson, E.
    Isoform-specific knockout of endothelial myosin light chain kinase: closing the gap on inflammatory lung disease (2004), Trends Pharmacol. Sci., 25, 64-66.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.7.11.18 medicine therapeutic inhibition via specific chemical inhibitors of endothelial isozyme, i.e. 11-(3-chloro-6-immino-6H-pyridazin-1-yl)-undecanoic acid (6-phenyl-pyridazin-3-yl)-amide, represents an important new target for the treatment of inflammatory lung disease with less side effects than other therapies Mus musculus

Protein Variants

EC Number Protein Variants Comment Organism
2.7.11.18 additional information construction of eMLCK or smMLCK knockout mutant mice by genetic or chemical methods, overview Mus musculus

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.18 11-(3-chloro-6-iminopyridazin-1(6H)-yl)-N-(6-phenylpyridazin-3-yl)undecanamide highly specific inhibitor, competitive to ATP binding Mus musculus
2.7.11.18 KT5926 i.e. (8R,9S,11S)-(-)-9-hydroxy-9-methoxycarbonyl-8-methyl-14-n-propoxy-2,3,9,10-tetrahydro-8,11-epoxy,1H,8H,11H-2,7beta,11alpha-triazadeibenzo[a,g]cycloocta[cde]triden-1-one, specific inhibitor Homo sapiens
2.7.11.18 ML-7 i.e. 1-(5-iodonaphthalene-1-sulfonyl)-1H-hexahydro-1,4-diazepine HCl, specific inhibitor Homo sapiens

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
2.7.11.18 108000
-
 smooth muscle isozyme Mus musculus
2.7.11.18 130000 150000 smooth muscle isozyme Homo sapiens
2.7.11.18 210000
-
 endothelial isozyme Mus musculus
2.7.11.18 214000
-
 endothelial isozyme Homo sapiens

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 activation of the enzyme is a key regulatory step in the modulation of endothelial permeability, central to parthogenesis of inflammatory lung disease is disruption of the endothelial barrier function ADP + [myosin light chain] phosphate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.18 Homo sapiens
-
 2 isozymes encoded by a single gene and translated from 2 different splicing variants
-
2.7.11.18 Mus musculus
-
 2 isozymes encoded by a single gene and translated from 2 different splicing variants
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.11.18 endothelium specific isozyme Mus musculus
-
2.7.11.18 endothelium specific isozyme Homo sapiens
-
2.7.11.18 smooth muscle specific isozyme Mus musculus
-
2.7.11.18 smooth muscle specific isozyme Homo sapiens
-

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] activation of the enzyme is a key regulatory step in the modulation of endothelial permeability, central to parthogenesis of inflammatory lung disease is disruption of the endothelial barrier function Homo sapiens ADP + [myosin light chain] phosphate
-
 ?

Subunits

EC Number Subunits Comment Organism
2.7.11.18 More the endothelial isozyme possesses a catalytic domain including the actin-binding domain and the calmodulin binding domain, like the smooth muscle isozyme, but also a protein-protein interaction domain including SH2 and SH3 domains Mus musculus
2.7.11.18 More the endothelial isozyme possesses a catalytic domain including the actin-binding domain and the calmodulin binding domain, like the smooth muscle isozyme, but also a protein-protein interaction domain including SH2 and SH3 domains Homo sapiens

Synonyms

EC Number Synonyms Comment Organism
2.7.11.18 endothelial MLCK
-
 Mus musculus
2.7.11.18 endothelial MLCK
-
 Homo sapiens
2.7.11.18 endothelial myosin light chain kinase
-
 Mus musculus
2.7.11.18 endothelial myosin light chain kinase
-
 Homo sapiens
2.7.11.18 MLCK
-
 Mus musculus
2.7.11.18 MLCK
-
 Homo sapiens
2.7.11.18 myosine light chain kinase
-
 Mus musculus
2.7.11.18 myosine light chain kinase
-
 Homo sapiens
2.7.11.18 smMLCK
-
 Mus musculus
2.7.11.18 smMLCK
-
 Homo sapiens
2.7.11.18 smooth muscle myosin light chain kinase
-
 Mus musculus
2.7.11.18 smooth muscle myosin light chain kinase
-
 Homo sapiens

Cofactor

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