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Literature summary 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

Application

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

Cloned(Commentary)

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

Protein Variants

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

Inhibitors

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

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.1.1.45 0.063
-
 lenampicillin recombinant CMBL, Vmax: 4 nmol/min/mg Homo sapiens
3.1.1.45 0.16
-
 olmesartan medoxomil native enzyme from liver cytosol, Vmax: 19.7 nmol/min/mg Homo sapiens
3.1.1.45 0.17
-
 olmesartan medoxomil recombinant CMBL, Vmax: 24.6 nmol/min/mg Homo sapiens
3.1.1.45 0.19
-
 olmesartan medoxomil native enzyme from intestine cytosol, Vmax: 45 nmol/min/mg Homo sapiens
3.1.1.45 0.23
-
 olmesartan medoxomil native enzyme from intestinal microsomes, Vmax: 6.76 nmol/min/mg Homo sapiens
3.1.1.45 0.28
-
 faropenem medoxomil recombinant CMBL, Vmax: 16.4 nmol/min/mg Homo sapiens
3.1.1.45 0.48
-
 olmesartan medoxomil native enzyme from liver microsomes, Vmax: 15 nmol/min/mg Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
3.1.1.45 Homo sapiens
-
-
-

Purification (Commentary)

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

Source Tissue

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

Substrates and Products (Substrate)

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

Synonyms

EC Number Synonyms Comment Organism
3.1.1.45 carboxymethylenebutenolidase
-
 Homo sapiens
3.1.1.45 CMBL
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
3.1.1.45 37
-
 assay at Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.1.1.45 7.4
-
 assay at Homo sapiens