Any feedback?
Literature summary for 3.6.1.12 extracted from
- Chemical genetics reveals a role of dCTP pyrophosphatase 1 in Wnt signaling (2019), Angew. Chem. Int. Ed. Engl., 58, 13009-13013 .
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| gene DCTTP1, recombinant expression in HEK293 cells and of FLAG-tagged dCTPP1 in HCT-116 cells | Homo sapiens |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| additional information | enzyme downregulation, HEK293T cells are transiently transfected with siRNA targeting dCTPP1 or control siRNA. Wnt-responsive reporter gene assay is performed in HEK293T cells transiently transfected with SuperTOPFlash (STF) plasmid and siRNA targeting dCTPP1 or control siRNA | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 2-methyl-4-(3-phenyl[1,2,4]triazolo[3,4-b][1,3,4]thiadiazol-6-yl)quinoline | - |
Homo sapiens |  |
| 2-[2-[2-(2-aminoethoxy)ethoxy]ethoxy]ethyl 2-(4-methoxyphenyl)-3-methyl-4-oxo-1,2,3,3a,4,9b-hexahydro[1]benzopyrano[3,4-b]pyrrole-1-carboxylate | - |
Homo sapiens | |
| benzimidazole | - |
Homo sapiens | |
| methyl 2-(4-methoxyphenyl)-3-methyl-4-oxo-3,4-dihydro[1]benzopyrano[3,4-b]pyrrole-1-carboxylate | i.e. pyrcoumin, a pyrrolocoumarin, and a competitive inhibitor of dCTP pyrophosphatase 1 (dCTPP1). Pyrcoumin induces thermal stabilization of dCTPP1 with a shift in melting temperature of 6°C with a half-maximal effective concentration (EC50) of 0.0059 mM. 57% inhibition. Pyrcoumin impairs the direct interaction of dCTPP1 and ubiquitin carboxyl-terminal hydrolase (USP7, EC 3.4.19.12) | Homo sapiens | |
| additional information | no inhibitory activity by methyl 3-benzyl-2-(4-methoxyphenyl)-4-oxo-3,4-dihydro[1]benzopyrano[3,4-b]pyrrole-1-carboxylate | Homo sapiens |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | Michaelis-Menten kinetics | Homo sapiens | |
| 0.019 | - |
dCTP | pH and temperature not specified in the publication, recombinant enzyme | Homo sapiens | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 5-methyl-dCTP + H2O | Homo sapiens | - |
5-methyl-dCMP + diphosphate | - |
? | |
| dCTP + H2O | Homo sapiens | - |
dCMP + diphosphate | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | Q9H773 | - |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| dCTPP1 co-elutes with USP7 in gel filtration shift assays with recombinant USP7 and dCTPP1 from HCT-116 cell extract | Homo sapiens |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| HCT-116 cell | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 5-methyl-dCTP + H2O | - |
Homo sapiens | 5-methyl-dCMP + diphosphate | - |
? | |
| dCTP + H2O | - |
Homo sapiens | dCMP + diphosphate | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| dCTP pyrophosphatase 1 | - |
Homo sapiens |
| DCTPP1 | - |
Homo sapiens |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | inhibition kinetics | Homo sapiens |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.000044 | - |
pH and temperature not specified in the publication, recombinant enzyme | Homo sapiens | benzimidazole | |
| 0.0011 | - |
pH and temperature not specified in the publication, recombinant enzyme | Homo sapiens | 2-methyl-4-(3-phenyl[1,2,4]triazolo[3,4-b][1,3,4]thiadiazol-6-yl)quinoline | |
| 0.0033 | - |
pH and temperature not specified in the publication, recombinant enzyme | Homo sapiens | methyl 2-(4-methoxyphenyl)-3-methyl-4-oxo-3,4-dihydro[1]benzopyrano[3,4-b]pyrrole-1-carboxylate | |
| 0.0148 | - |
pH and temperature not specified in the publication, recombinant enzyme | Homo sapiens | 2-[2-[2-(2-aminoethoxy)ethoxy]ethoxy]ethyl 2-(4-methoxyphenyl)-3-methyl-4-oxo-1,2,3,3a,4,9b-hexahydro[1]benzopyrano[3,4-b]pyrrole-1-carboxylate | |
General Information
| General Information | Comment | Organism |
|---|---|---|
| metabolism | dCTPP1 plays a role in regulation of Wnt/bcatenin signaling most likely through a direct interaction with USP7. Canonical Wnt/beta-catenin signaling is a fundamental growth control pathway essential for, for example, embryonic development, stem cell maintenance, cell proliferation and tissue homeostasis, pathway regulation, overview. Upon activation the central Wnt pathway component beta-catenin is no longer phosphorylated and degraded by the so-called destruction complex, but rather stabilized and translocated to the nucleus, where it activates the expression of Wnt target genes | Homo sapiens |
| physiological function | the canonical Wnt pathway is essential for normal embryonic development and tissue homeostasis, and its deregulation plays a crucial role in carcinogenesis. dCTP pyrophosphatase 1 (dCTPP1) is a positive regulator of canonical Wnt signaling, interacts with ubiquitin carboxyl-terminal hydrolase (USP7, EC 3.4.19.12) in Wnt signal-dependent manner, and this interaction is weakened by dCTPP1 inhibitors, e.g. pyrcoumin. Analysis of interaction between dCTPP1 and USP7 and the role for dCTPP1 in the Wnt/beta-catenin pathway, overview | Homo sapiens |
Use of this online version of BRENDA is free under the CC BY 4.0 license. See terms of use for full details.
Release 2023.1 (January 2023)
Legal
Curated at
Member of
