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Literature summary for 1.1.3.15 extracted from

  • Barawkar, D.; Meru, A.; Bandyopadhyay, A.; Banerjee, A.; Deshpande, A.; Athare, C.; Koduru, C.; Khose, G.; Gundu, J.; Mahajan, K.; Patil, P.; Kandalkar, S.; Niranjan, S.; Bhosale, S.; De, S.; Mukhopadhyay, S.; Chaudhary, S.; Koul, S.; Singh, U.; Chugh, A.
    Potent and selective inhibitors of long chain l-2-hydroxy acid oxidase reduced blood pressure in DOCA salt-treated rats (2011), ACS Med. Chem. Lett., 2, 919-923.
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
drug development isozyme Hao2 is a target for drug development in high blood pressure Rattus norvegicus

Inhibitors

Inhibitors Comment Organism Structure
3-methyl-4-(2-phenylethyl)-1H-pyrazole-5-carboxylic acid
-
Rattus norvegicus
4-(1-benzothiophen-2-ylmethyl)-3-methyl-1H-pyrazole-5-carboxylic acid
-
Rattus norvegicus
4-(4-fluorophenyl)-3-methyl-1H-pyrazole-5-carboxylic acid 35% inhibition at 0.010 mM Rattus norvegicus
4-(biphenyl-3-ylmethyl)-3-methyl-1H-pyrazole-5-carboxylic acid
-
Rattus norvegicus
4-[(4'-fluorobiphenyl-3-yl)methyl]-3-methyl-1H-pyrazole-5-carboxylic acid
-
Rattus norvegicus
additional information treatment with 4-[(4'-fluorobiphenyl-3-yl)methyl]-3-methyl-1H-pyrazole-5-carboxylic acid or 4-(1-benzothiophen-2-ylmethyl)-3-methyl-1H-pyrazole-5-carboxylic acid results in a significant reduction or attenuation of blood pressure in an established or developing model of hypertension, deoxycorticosterone acetate-treated rats Rattus norvegicus

Localization

Localization Comment Organism GeneOntology No. Textmining
peroxisome
-
Rattus norvegicus 5777
-

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
39000
-
x * 39000, about, sequence calculation Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
kidney
-
Rattus norvegicus
-
liver
-
Rattus norvegicus
-

Subunits

Subunits Comment Organism
? x * 39000, about, sequence calculation Rattus norvegicus
More molecular modeling studies using the rat Hao2 crystal structure, PDB ID 1TB3, overview Rattus norvegicus

Synonyms

Synonyms Comment Organism
Hao2
-
Rattus norvegicus
L-2-hydroxy acid oxidase
-
Rattus norvegicus
long chain l-2-hydroxy acid oxidase
-
Rattus norvegicus

Cofactor

Cofactor Comment Organism Structure
FMN
-
Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0003
-
pH and temperature not specified in the publication Rattus norvegicus 4-[(4'-fluorobiphenyl-3-yl)methyl]-3-methyl-1H-pyrazole-5-carboxylic acid
0.0003
-
pH and temperature not specified in the publication Rattus norvegicus 4-(1-benzothiophen-2-ylmethyl)-3-methyl-1H-pyrazole-5-carboxylic acid
0.0091
-
pH and temperature not specified in the publication Rattus norvegicus 4-(biphenyl-3-ylmethyl)-3-methyl-1H-pyrazole-5-carboxylic acid
427
-
pH and temperature not specified in the publication Rattus norvegicus 3-methyl-4-(2-phenylethyl)-1H-pyrazole-5-carboxylic acid

General Information

General Information Comment Organism
physiological function pharmacological role of the enzyme in the management of blood pressure Rattus norvegicus