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Literature summary for 3.1.1.1 extracted from

  • Thomsen, R.; Rasmussen, H.B.; Linnet, K.; Linnet, K.
    In vitro drug metabolism by human carboxylesterase 1: focus on angiotensin-converting enzyme inhibitors (2014), Drug Metab. Dispos., 42, 126-133.
    View publication on PubMed
Search for more literature for 3.1.1.1

Inhibitors

Inhibitors Comment Organism Structure
(2R)-2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile about 30% residual activity at 0.1 mM Homo sapiens
amlodipine about 40% residual activity at 0.1 mM Homo sapiens
atorvastatin about 45% residual activity at 0.1 mM Homo sapiens
bendroflumethiazide about 70% residual activity at 0.1 mM Homo sapiens
bisoprolol about 90% residual activity at 0.1 mM Homo sapiens
carvedilol about 17% residual activity at 0.1 mM Homo sapiens
clopidogrel about 15% residual activity at 0.1 mM Homo sapiens
diltiazem about 23% residual activity at 0.1 mM Homo sapiens
eplerenone about 80% residual activity at 0.1 mM Homo sapiens
Furosemide about 78% residual activity at 0.1 mM Homo sapiens
irbesartan about 75% residual activity at 0.1 mM Homo sapiens
isradipine about 18% residual activity at 0.1 mM Homo sapiens
lercanidipine about 78% residual activity at 0.1 mM Homo sapiens
additional information not inhibited by 0.1 mM dabigatran exilate, dabigatran, pindolol, labetalol, propranolol, metoprolol, sotalol, and azathioprine Homo sapiens
nimodipine about 70% residual activity at 0.1 mM Homo sapiens
simvastatin complete inhibition at 0.1 mM Homo sapiens
sirolimus about 90% residual activity at 0.1 mM Homo sapiens
spironolactone about 70% residual activity at 0.1 mM Homo sapiens
tacrolimus about 28% residual activity at 0.1 mM Homo sapiens
valsartan about 90% residual activity at 0.1 mM Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.901
-
 ramipril in 100 mM phosphate buffer at 37°C, pH not specified in the publication Homo sapiens
1.721
-
 trandolapril in 100 mM phosphate buffer at 37°C, pH not specified in the publication Homo sapiens
1.734
-
 enalapril in 100 mM phosphate buffer at 37°C, pH not specified in the publication Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
microsome
-
 Homo sapiens
-
-

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4-nitrophenyl acetate + H2O
-
 Homo sapiens 4-nitrophenol + acetate
-
 ?
enalapril + H2O
-
 Homo sapiens ?
-
 ?
ramipril + H2O
-
 Homo sapiens ?
-
 ?
trandolapril + H2O
-
 Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
carboxylesterase 1
-
 Homo sapiens
CES1
-
 Homo sapiens

General Information

General Information Comment Organism
metabolism carboxylesterase 1 plays a role in the metabolism of several drugs used in the treatment of common conditions, including hypertension, congestive heart failure, and diabetes mellitus Homo sapiens