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Literature summary extracted from

  • Wu, K.; Marks, D.L.; Watanabe, R.; Paul, P.; Rajan, N.; Pagano, R.E.
    Histidine-193 of rat glucosylceramide synthase resides in a UDP-glucose-and inhibitor (D-threo-1-phenyl-2-decanoylamino-3-morpholinopropan-1-ol)-binding region: a biochemical and mutational study (1999), Biochem. J., 341, 395-400.
No PubMed abstract available

Application

EC Number Application Comment Organism
2.4.1.80 medicine
-
 Homo sapiens
2.4.1.80 medicine enzyme inhibition is a possible target for chemotherapeutic agents for a number of diseases, including cancer Rattus norvegicus

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.4.1.80 cloning from rat brain genetic library and expression in Escherichia coli BL21(DE3) Rattus norvegicus

Protein Variants

EC Number Protein Variants Comment Organism
2.4.1.80 H169A 26.4% activity compared to wild-type, reduced inhibition by diethyldicarbonate and increased protection by UDP-glucose Rattus norvegicus
2.4.1.80 H193A 33.0% activity compared to wild-type, reduced inhibition by diethyldicarbonate and reduced protection by UDP-glucose Rattus norvegicus
2.4.1.80 H193D no activity Rattus norvegicus
2.4.1.80 H193N 23.0% activity compared to wild-type, reduced inhibition by diethyldicarbonate and reduced protection by UDP-glucose Rattus norvegicus
2.4.1.80 H193R no activity Rattus norvegicus
2.4.1.80 H26A 5.2% activity compared to wild-type Rattus norvegicus
2.4.1.80 H26D 10.5% activity compared to wild-type Rattus norvegicus
2.4.1.80 H26N 44.5% activity compared to wild-type Rattus norvegicus
2.4.1.80 H26R 118.5% activity compared to wild-type, slightly enhanced inhibition by diethyldicarbonate and slightly reduced protection by UDP-glucose Rattus norvegicus
2.4.1.80 H308A 35.2% activity compared to wild-type, slightly reduced inhibition by diethyldicarbonate and slightly reduced protection by UDP-glucose Rattus norvegicus
2.4.1.80 H308A/H309A 10.8% activity compared to wild-type Rattus norvegicus
2.4.1.80 H309A 69.1% activity compared to wild-type Rattus norvegicus
2.4.1.80 H322A 3.8% activity compared to wild-type Rattus norvegicus
2.4.1.80 H322D 2.6% activity compared to wild-type Rattus norvegicus
2.4.1.80 H322N 49.8% activity compared to wild-type, slightly enhanced inhibition by diethyldicarbonate and slightly reduced protection by UDP-glucose Rattus norvegicus
2.4.1.80 H322R no activity Rattus norvegicus
2.4.1.80 H36A 103.2% activity compared to wild-type, slightly enhanced inhibition by diethyldicarbonate and slightly reduced protection by UDP-glucose Rattus norvegicus
2.4.1.80 H90A 119.3% activity compared to wild-type Rattus norvegicus

General Stability

EC Number General Stability Organism
2.4.1.80 glycerol stabilizes Rattus norvegicus

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.1.80 D-threo-1-phenyl-2-(decanoylamino)-3-morpholino-1-propanol-HCl
-
 Homo sapiens
2.4.1.80 D-threo-1-phenyl-2-(decanoylamino)-3-morpholino-1-propanol-HCl His193 mutants are not inhibited; i.e. PDMP Rattus norvegicus
2.4.1.80 diethyl dicarbonate i.e. DEPC; reversible by hydroxylamine, UDP-glucose protects, inhibitor acts on histidine residues, including His193, within or near UDP-glucose binding site Rattus norvegicus

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
2.4.1.80 additional information
-
 partial amino acid sequence alignment Homo sapiens
2.4.1.80 additional information
-
 partial amino acid sequence alignment Rattus norvegicus

Organism

EC Number Organism UniProt Comment Textmining
2.4.1.80 Homo sapiens Q16739
-
-
2.4.1.80 Rattus norvegicus Q9R0E0
-
-

Reaction

EC Number Reaction Comment Organism Reaction ID
2.4.1.80 UDP-alpha-D-glucose + an N-acylsphingosine = UDP + a beta-D-glucosyl-N-acylsphingosine UDP-glucose and inhibitor D-PDMP binding region overlap and contain His193 Rattus norvegicus
a

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.4.1.80 brain
-
 Homo sapiens
-
2.4.1.80 brain
-
 Rattus norvegicus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.1.80 UDP-glucose + N-acylsphingosine i.e. ceramide Homo sapiens UDP + D-glucosyl-N-acylsphingosine i.e. glucosylceramide ?
2.4.1.80 UDP-glucose + N-acylsphingosine i.e. ceramide Rattus norvegicus UDP + D-glucosyl-N-acylsphingosine i.e. glucosylceramide ?
2.4.1.80 UDP-glucose + N-[7-(4-nitrobenzo-2-oxa-1,3-diazole)]-6-aminocaproyl-D-erythro-sphingosine synthetic fluorescent ceramide substrate analogue for fluorescence enzyme assay Rattus norvegicus UDP + D-glucosyl-N-[7-(4-nitrobenzo-2-oxa-1,3-diazole)]-6-aminocaproyl-D-erythro-sphingosine
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.4.1.80 GCS
-
 Homo sapiens
2.4.1.80 GCS
-
 Rattus norvegicus

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.4.1.80 37
-
 assay at Homo sapiens
2.4.1.80 37
-
 assay at Rattus norvegicus

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.4.1.80 7.4
-
-
 Homo sapiens
2.4.1.80 7.4
-
 assay at Rattus norvegicus