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Literature summary for 3.1.1.45 extracted from

  • Ishizuka, T.; Fujimori, I.; Kato, M.; Noji-Sakikawa, C.; Saito, M.; Yoshigae, Y.; Kubota, K.; Kurihara, A.; Izumi, T.; Ikeda, T.; Okazaki, O.
    Human carboxymethylenebutenolidase as a bioactivating hydrolase of olmesartan medoxomil in liver and intestine (2010), J. Biol. Chem., 285, 11892-11902.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.1.1.45

Application

Application Comment Organism
medicine enzyme serves as a bioactivating hydrolase of olmesartan medoxomil, hydrolyzing the ester bond of the pro-drug type xenobiotics Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
recombinantly expressed in mammalian cells and in Escherichia coli Homo sapiens

Protein Variants

Protein Variants Comment Organism
C132A mutant shows a drastic reduction of the olmesartan medoxomil-hydrolyzing activity Homo sapiens
C132A mutant shows a low activity, 30% of wild-type Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
bis-p-nitrophenylphosphate weak inhibitor Homo sapiens
p-chloromercuribenzoate strong inhibitor Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.063
-
 lenampicillin recombinant CMBL, Vmax: 4 nmol/min/mg Homo sapiens
0.16
-
 olmesartan medoxomil native enzyme from liver cytosol, Vmax: 19.7 nmol/min/mg Homo sapiens
0.17
-
 olmesartan medoxomil recombinant CMBL, Vmax: 24.6 nmol/min/mg Homo sapiens
0.19
-
 olmesartan medoxomil native enzyme from intestine cytosol, Vmax: 45 nmol/min/mg Homo sapiens
0.23
-
 olmesartan medoxomil native enzyme from intestinal microsomes, Vmax: 6.76 nmol/min/mg Homo sapiens
0.28
-
 faropenem medoxomil recombinant CMBL, Vmax: 16.4 nmol/min/mg Homo sapiens
0.48
-
 olmesartan medoxomil native enzyme from liver microsomes, Vmax: 15 nmol/min/mg Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
purified from human liver and intestinal cytosol using successive column chromatography Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
brain transcript detected by RT-PCR Homo sapiens
-
colon transcript detected by RT-PCR, high expression Homo sapiens
-
heart transcript detected by RT-PCR Homo sapiens
-
intestine detected by Western blot analysis Homo sapiens
-
kidney transcript detected by RT-PCR, very high expression Homo sapiens
-
liver detected by Western blot analysis Homo sapiens
-
lung transcript detected by RT-PCR Homo sapiens
-
placenta transcript detected by RT-PCR Homo sapiens
-
prostate transcript detected by RT-PCR Homo sapiens
-
skeletal muscle transcript detected by RT-PCR Homo sapiens
-
spinal cord transcript detected by RT-PCR Homo sapiens
-
spleen transcript detected by RT-PCR Homo sapiens
-
stomach transcript detected by RT-PCR Homo sapiens
-
testis transcript detected by RT-PCR Homo sapiens
-
thymus transcript detected by RT-PCR Homo sapiens
-
trachea transcript detected by RT-PCR Homo sapiens
-
uterus transcript detected by RT-PCR Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
faropenem medoxomil + H2O
-
 Homo sapiens ?
-
 ?
lenampicillin + H2O
-
 Homo sapiens ?
-
 ?
olmesartan medoxomil + H2O
-
 Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
carboxymethylenebutenolidase
-
 Homo sapiens
CMBL
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
 assay at Homo sapiens