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Literature summary for 2.4.1.80 extracted from
- 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
| Application | Comment | Organism |
|---|---|---|
| medicine | - |
Homo sapiens |
| medicine | enzyme inhibition is a possible target for chemotherapeutic agents for a number of diseases, including cancer | Rattus norvegicus |
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| cloning from rat brain genetic library and expression in Escherichia coli BL21(DE3) | Rattus norvegicus |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| H169A | 26.4% activity compared to wild-type, reduced inhibition by diethyldicarbonate and increased protection by UDP-glucose | Rattus norvegicus |
| H193A | 33.0% activity compared to wild-type, reduced inhibition by diethyldicarbonate and reduced protection by UDP-glucose | Rattus norvegicus |
| H193D | no activity | Rattus norvegicus |
| H193N | 23.0% activity compared to wild-type, reduced inhibition by diethyldicarbonate and reduced protection by UDP-glucose | Rattus norvegicus |
| H193R | no activity | Rattus norvegicus |
| H26A | 5.2% activity compared to wild-type | Rattus norvegicus |
| H26D | 10.5% activity compared to wild-type | Rattus norvegicus |
| H26N | 44.5% activity compared to wild-type | Rattus norvegicus |
| H26R | 118.5% activity compared to wild-type, slightly enhanced inhibition by diethyldicarbonate and slightly reduced protection by UDP-glucose | Rattus norvegicus |
| H308A | 35.2% activity compared to wild-type, slightly reduced inhibition by diethyldicarbonate and slightly reduced protection by UDP-glucose | Rattus norvegicus |
| H308A/H309A | 10.8% activity compared to wild-type | Rattus norvegicus |
| H309A | 69.1% activity compared to wild-type | Rattus norvegicus |
| H322A | 3.8% activity compared to wild-type | Rattus norvegicus |
| H322D | 2.6% activity compared to wild-type | Rattus norvegicus |
| H322N | 49.8% activity compared to wild-type, slightly enhanced inhibition by diethyldicarbonate and slightly reduced protection by UDP-glucose | Rattus norvegicus |
| H322R | no activity | Rattus norvegicus |
| H36A | 103.2% activity compared to wild-type, slightly enhanced inhibition by diethyldicarbonate and slightly reduced protection by UDP-glucose | Rattus norvegicus |
| H90A | 119.3% activity compared to wild-type | Rattus norvegicus |
General Stability
| General Stability | Organism |
|---|---|
| glycerol stabilizes | Rattus norvegicus |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| D-threo-1-phenyl-2-(decanoylamino)-3-morpholino-1-propanol-HCl | - |
Homo sapiens |  |
| D-threo-1-phenyl-2-(decanoylamino)-3-morpholino-1-propanol-HCl | His193 mutants are not inhibited; i.e. PDMP | Rattus norvegicus | |
| 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]
| Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
|---|---|---|---|
| additional information | - |
partial amino acid sequence alignment | Homo sapiens |
| additional information | - |
partial amino acid sequence alignment | Rattus norvegicus |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | Q16739 | - |
- |
| Rattus norvegicus | Q9R0E0 | - |
- |
Reaction
| Reaction | Comment | Organism | Reaction ID |
|---|---|---|---|
| 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 |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| brain | - |
Homo sapiens | - |
| brain | - |
Rattus norvegicus | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| UDP-glucose + N-acylsphingosine | i.e. ceramide | Homo sapiens | UDP + D-glucosyl-N-acylsphingosine | i.e. glucosylceramide | ? | |
| UDP-glucose + N-acylsphingosine | i.e. ceramide | Rattus norvegicus | UDP + D-glucosyl-N-acylsphingosine | i.e. glucosylceramide | ? | |
| 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
| Synonyms | Comment | Organism |
|---|---|---|
| GCS | - |
Homo sapiens |
| GCS | - |
Rattus norvegicus |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 37 | - |
assay at | Homo sapiens |
| 37 | - |
assay at | Rattus norvegicus |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.4 | - |
- |
Homo sapiens |
| 7.4 | - |
assay at | Rattus norvegicus |
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Release 2023.1 (January 2023)
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