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Literature summary extracted from

  • Bijvelds, M.J.; Bot, A.G.; Escher, J.C.; de Jonge, H.R.
    Activation of intestinal Cl- secretion by lubiprostone requires the cystic fibrosis transmembrane conductance regulator (2009), Gastroenterology, 137, 976-985.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
5.6.1.6 forskolin lubiprostone and forskolin activate the same pool of apical Cl- channels Homo sapiens
5.6.1.6 lubiprostone lubiprostone and forskolin activate the same pool of apical Cl- channels, lubiprostone induces the secretory response in intestinal epithelium involving the enzyme. Lubiprostone enhances intestinal Cl- and fluid secretion via prostanoid receptor signaling, triggering activation of CFTR. The EP4-type prostanoid receptor antagonist L-161982 blocks the lubiprostone response. Lubiprostone enhances Cl- secretion across human large and mall intestinal epithelium through a CFTR-dependent pathway Homo sapiens
5.6.1.6 lubiprostone lubiprostone enhances Cl- secretion across mouse ileum through a CFTR-dependent pathway and induces the secretory response in intestinal epithelium involving the enzyme. Lubiprostone enhances intestinal Cl- and fluid secretion via prostanoid receptor signaling, triggering activation of CFTR. The EP4-type prostanoid receptor antagonist L-161982 blocks the lubiprostone response Mus musculus

Inhibitors

EC Number Inhibitors Comment Organism Structure
5.6.1.6 bumetanide blocks CFTR Homo sapiens
5.6.1.6 CFTRinh172 blocks CFTR Homo sapiens
5.6.1.6 additional information no inhibition of CFTR by CdCl2 Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
5.6.1.6 membrane
-
Mus musculus 16020
-
5.6.1.6 membrane
-
Homo sapiens 16020
-

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
5.6.1.6 ATP + H2O + closed Cl- channel Mus musculus CFTR is a Cl- channel ADP + phosphate + open Cl- channel
-
?
5.6.1.6 ATP + H2O + closed Cl- channel Homo sapiens CFTR is a Cl- channel ADP + phosphate + open Cl- channel
-
?
5.6.1.6 additional information Mus musculus enzyme defects or inhibition lead to cystic fibrosis ?
-
?
5.6.1.6 additional information Homo sapiens enzyme defects or inhibition lead to cystic fibrosis ?
-
?

Organism

EC Number Organism UniProt Comment Textmining
5.6.1.6 Homo sapiens
-
-
-
5.6.1.6 Mus musculus
-
wild-type mice, Cftr-null mice, homozygous F508del mice, and Cftr-/- littermates
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
5.6.1.6 ileum
-
Mus musculus
-
5.6.1.6 intestinal epithelium
-
Mus musculus
-
5.6.1.6 intestinal epithelium
-
Homo sapiens
-
5.6.1.6 intestine
-
Mus musculus
-
5.6.1.6 large intestine
-
Homo sapiens
-
5.6.1.6 small intestine
-
Homo sapiens
-
5.6.1.6 T-84 cell derived from a human colon carcinoma Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5.6.1.6 ATP + H2O + closed Cl- channel CFTR is a Cl- channel Mus musculus ADP + phosphate + open Cl- channel
-
?
5.6.1.6 ATP + H2O + closed Cl- channel CFTR is a Cl- channel Homo sapiens ADP + phosphate + open Cl- channel
-
?
5.6.1.6 additional information enzyme defects or inhibition lead to cystic fibrosis Mus musculus ?
-
?
5.6.1.6 additional information enzyme defects or inhibition lead to cystic fibrosis Homo sapiens ?
-
?

Synonyms

EC Number Synonyms Comment Organism
5.6.1.6 CFTR
-
Mus musculus
5.6.1.6 CFTR
-
Homo sapiens
5.6.1.6 cystic fibrosis transmembrane conductance regulator
-
Mus musculus
5.6.1.6 cystic fibrosis transmembrane conductance regulator
-
Homo sapiens