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Literature summary extracted from

  • Tropak, M.B.; Zhang, J.; Yonekawa, S.; Rigat, B.A.; Aulakh, V.S.; Smith, M.R.; Hwang, H.J.; Ciufolini, M.A.; Mahuran, D.J.
    Pyrimethamine derivatives insight into binding mechanism and improved enhancement of mutant beta-N-acetylhexosaminidase activity (2015), J. Med. Chem., 58, 4483-4493 .
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.2.1.52 2-amino-4-ethyl-5-(4-(trifluoromethyl)phenyl)pyrimidine
-
 Homo sapiens
3.2.1.52 2-amino-4-ethyl-5-(4-chlorophenyl)pyrimidine
-
 Homo sapiens
3.2.1.52 2-amino-6-ethyl-5-(4-chlorophenyl)pyrimidin-4(3H)-one
-
 Homo sapiens
3.2.1.52 4-ethyl-5-[4-(trifluoromethyl)phenyl]pyrimidine
-
 Homo sapiens
3.2.1.52 5-(3,5-dimethylphenyl)-6-ethylpyrimidine-2,4-diamine
-
 Homo sapiens
3.2.1.52 5-(4-chlorophenyl)-6-butylpyrimidine-2,4-diamine
-
 Homo sapiens
3.2.1.52 5-(4-chlorophenyl)-6-isopropylpyrimidine-2,4-diamine
-
 Homo sapiens
3.2.1.52 5-(4-chlorophenyl)-6-methylpyrimidine-2,4-diamine
-
 Homo sapiens
3.2.1.52 5-(4-chlorophenyl)-6-propylpyrimidine-2,4-diamine
-
 Homo sapiens
3.2.1.52 6-(aminomethyl)-5-(4-chlorophenyl)pyrimidine-2,4-diamine
-
 Homo sapiens
3.2.1.52 6-ethyl-5-(4-(trifluoromethyl)phenyl)pyrimidine-2,4-diamine
-
 Homo sapiens
3.2.1.52 6-ethyl-5-(4-methoxyphenyl)pyrimidine-2,4-diamine
-
 Homo sapiens
3.2.1.52 6-ethyl-5-(m-tolyl)pyrimidine-2,4-diamine
-
 Homo sapiens
3.2.1.52 6-ethyl-5-(o-tolyl)pyrimidine-2,4-diamine
-
 Homo sapiens
3.2.1.52 6-ethyl-5-(p-tolyl)pyrimidine-2,4-diamine
-
 Homo sapiens
3.2.1.52 6-ethyl-5-phenylpyrimidine-2,4-diamine
-
 Homo sapiens
3.2.1.52 pyrimethamine i.e. 5-(4-chlorophenyl)-6-ethylpyrimidine-2,4-diamine Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
3.2.1.52 lysosome
-
 Homo sapiens 5764
-

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.2.1.52 ganglioside GM2 + H2O Homo sapiens
-
 ganglioside GM3 + N-acetyl-beta-D-galactosamine
-
 ?

Organism

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

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.2.1.52 fibroblast
-
 Homo sapiens
-
3.2.1.52 placenta
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.2.1.52 4-methylumbelliferyl 2-acetamido-2-deoxy-beta-D-glucopyranoside 6-sulfate + H2O
-
 Homo sapiens 4-methylumbelliferone + 2-acetamido-2-deoxy-beta-D-glucopyranoside 6-sulfate
-
 ?
3.2.1.52 4-nitrophenyl N-acetyl-beta-D-glucosaminide + H2O
-
 Homo sapiens 4-nitrophenol + N-acetyl-beta-D-glucosamine
-
 ?
3.2.1.52 ganglioside GM2 + H2O
-
 Homo sapiens ganglioside GM3 + N-acetyl-beta-D-galactosamine
-
 ?

Subunits

EC Number Subunits Comment Organism
3.2.1.52 heterodimer
-
 Homo sapiens

Synonyms

EC Number Synonyms Comment Organism
3.2.1.52 beta-N-acetylhexosaminidase A
-
 Homo sapiens
3.2.1.52 beta-N-acetylhexosaminidase B
-
 Homo sapiens
3.2.1.52 Hex A
-
 Homo sapiens
3.2.1.52 Hex B
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.2.1.52 0.0031
-
 wild type enzyme isoform Hex A from placenta, at pH 7.0 and 37°C Homo sapiens pyrimethamine
3.2.1.52 0.0045
-
 wild type enzyme isoform Hex B from placenta, at pH 7.0 and 37°C Homo sapiens pyrimethamine
3.2.1.52 0.0085
-
 mutant enzyme G269S of isoform Hex A from fibroblasts, at pH 4.5 and 37°C Homo sapiens pyrimethamine
3.2.1.52 0.0089
-
 wild type enzyme isoform Hex A from placenta, at pH 4.5 and 37°C Homo sapiens pyrimethamine
3.2.1.52 0.0091
-
 wild type enzyme isoform Hex B from placenta, at pH 4.5 and 37°C Homo sapiens pyrimethamine
3.2.1.52 0.014
-
 wild type enzyme isoform Hex A from fibroblasts, at pH 4.5 and 37°C Homo sapiens pyrimethamine