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Information on EC 3.6.1.12 - dCTP diphosphatase and Organism(s) Homo sapiens
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3.6.1.12 dCTP diphosphataseIUBMB Comments
The mammalian enzyme also displays weak activity against dTTP and dATP, but none against dGTP. Activity is highest with analogs including 5-iodo-dCTP and 5-methyl-dCTP.
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Word Map
- 3.6.1.12
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nudix
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mutt
- ap4a
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diadenosine
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decapping
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dihydrate
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triphosphorylated
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dinucleoside
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5',5'-p1,p4-tetraphosphate
- 8-oxo-dgtpase
- exoribonuclease
- 8-oxo-2'-deoxyguanosine
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5'-end-dependent
- 8-oxo-dgmp
- drug development
- medicine
The taxonomic range for the selected organisms is: Homo sapiens
The enzyme appears in selected viruses and cellular organisms
The enzyme appears in selected viruses and cellular organisms
Synonyms
pyrophosphohydrolase, dctpp1, dctpase, rs21-c6, ntp pyrophosphohydrolase, dctp pyrophosphatase 1, dctpase-dutpase, ntp pyrophosphatase, xtp3-transactivated protein a, all-alpha ntp pyrophosphatase, 
more
topSYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
dCTP pyrophosphatase
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dCTP pyrophosphatase 1
dCTPase
DCTPP1
deoxy-CTPase
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deoxycytidine triphosphatase
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deoxycytidine-triphosphatase
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phosphatase, deoxycytidine, tri-
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dCTPase
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
hydrolysis of phosphoric ester
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SYSTEMATIC NAME
IUBMB Comments
dCTP nucleotidohydrolase
The mammalian enzyme also displays weak activity against dTTP and dATP, but none against dGTP. Activity is highest with analogs including 5-iodo-dCTP and 5-methyl-dCTP.
CAS REGISTRY NUMBER
COMMENTARY
9024-87-7
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SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
aza-dCTP + H2O
dCMP + diphosphate
the enzyme can hydrolyse the activated form of decitabine, aza-dCTP, and might constitute a novel route in the detoxification of this DNA-methylation inhibitor
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?
additional information
?
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no substrtaes: ATP, CTP, UTP, dCDP, 5-methyl-dCDP, dGTP. Poor substrate: dUTP
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?
additional information
?
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no substrtaes: ATP, CTP, UTP, dCDP, 5-methyl-dCDP, dGTP. Poor substrate: dUTP
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?
additional information
?
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human all-alpha dCTP pyrophosphatase 1 (DCTPP1) is a dNTP pyrophosphatase with high affinity for dCTP and 5'-modified dCTP derivatives
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additional information
?
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human all-alpha dCTP pyrophosphatase 1 (DCTPP1) is a dNTP pyrophosphatase with high affinity for dCTP and 5'-modified dCTP derivatives
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NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
additional information
?
-
human all-alpha dCTP pyrophosphatase 1 (DCTPP1) is a dNTP pyrophosphatase with high affinity for dCTP and 5'-modified dCTP derivatives
-
-
-
additional information
?
-
-
human all-alpha dCTP pyrophosphatase 1 (DCTPP1) is a dNTP pyrophosphatase with high affinity for dCTP and 5'-modified dCTP derivatives
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METALS and IONS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
(2-((5,6-dichloro-2-methyl-4-nitro-1H-benzo[d]imidazol-1-yl)-methyl)phenyl)boronic acid
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(2-chlorophenyl)[4-[3-(cyclopropylamino)-4-nitrophenyl]piperazin-1-yl]methanone
91% inhibition at 0.01 mM
(3-((5,6-dichloro-2-methyl-4-nitro-1H-benzo[d]imidazol-1-yl)-methyl)phenyl)boronic acid
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(4-((4-nitro-2-(trifluoromethyl)-1H-benzo[d]imidazol-1-yl)-methyl)phenyl)boronic acid
-
(4-((5,6-dichloro-2-cyclopropyl-4-nitro-1H-benzo[d]imidazol-1-yl)methyl)phenyl)boronic acid
-
(4-((5,6-dichloro-2-methyl-1H-benzo[d]imidazol-1-yl)methyl)-phenyl)boronic acid
-
(4-((5,6-dichloro-2-methyl-4-nitro-1H-benzo[d]imidazol-1-yl)-methyl)phenyl)boronic acid
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(4-((5,6-difluoro-2-methyl-4-nitro-1H-benzo[d]imidazol-1-yl)-methyl)phenyl)boronic acid
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1,3-dimethyl-8-(4-propanoylpiperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
64% inhibition at 0.01 mM
1,3-dimethyl-8-[4-(2-thienylcarbonyl)-1-piperazinyl]-3,7-dihydro-1H-purine-2,6-dione
96% inhibition at 0.01 mM
1,6,7-trimethyl-8-[(4-methylphenyl)methyl]-1H-imidazo[2,1-f]purine-2,4(3H,8H)-dione
93% inhibition at 0.01 mM
1-(2-hydroxyethyl)-2,6-dimethyl-5-phenylpyrimidin-4(1H)-one
3% inhibition at 0.01 mM
1-(3-bromophenyl)-2,6-dimethyl-5-phenylpyrimidin-4(1H)-one
97% inhibition at 0.01 mM
1-(4-(1H-pyrazol-1-yl)benzyl)-5,6-dichloro-2-methyl-4-nitro-1H-benzo[d]imidazole
-
1-(4-(1H-pyrrol-1-yl)benzyl)-5,6-dichloro-2-methyl-4-nitro-1H-benzo[d]imidazole
-
1-(4-hydroxyphenyl)-2,6-dimethyl-5-phenylpyrimidin-4(1H)-one
80% inhibition at 0.01 mM
1-(7-methyl-2-[[(2-methylphenyl)methyl]sulfanyl][1,2,4]triazolo[1,5-a]pyrimidin-6-yl)ethan-1-one
97% inhibition at 0.01 mM
1-phenyl-4-[4-(pyridin-2-yl)piperazin-1-yl]phthalazine
86% inhibition at 0.01 mM
1-[2-(methoxymethyl)-7-methyl[1,2,4]triazolo[1,5-a]pyrimidin-6-yl]ethan-1-one
8% inhibition at 0.01 mM
1-[4-(1-benzyl-1H-tetrazol-5-yl)-4-[(prop-2-yn-1-yl)amino]piperidin-1-yl]-3-(3-methyl-3H-diazirin-3-yl)propan-1-one
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1-[4-nitro-3-(1-pyrrolidinyl)phenyl]-4-(2-thienylcarbonyl)piperazine
82% inhibition at 0.01 mM
1-[[4-(5-methyl-4-oxo-3-phenyl-4,5-dihydro[1,2]oxazolo[4,5-c]pyridin-6-yl)phenyl]methyl]pyrrolidine-2,5-dione
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2,3-dimethyl-5-oxo-N-(1-phenylethyl)-5H-[1,3]thiazolo[3,2-a]pyrimidine-6-carboxamide
93% inhibition at 0.01 mM
2,6-dimethyl-1-(4-methylphenyl)-5-phenylpyrimidin-4(1H)-one
64% inhibition at 0.01 mM
2-(1-butyl-5-methyl-1H-1,2,3-triazol-4-yl)-5-(furan-2-yl)-1,3,4-oxadiazole
18% inhibition at 0.01 mM
2-(2-chlorophenyl)-5-(5-methyl-1-phenyl-1H-1,2,3-triazol-4-yl)-1,3,4-oxadiazole
98% inhibition at 0.01 mM
2-(2-chlorophenyl)-5-[1-(4-fluorophenyl)-5-methyl-1H-1,2,3-triazol-4-yl]-1,3,4-oxadiazole
47% inhibition at 0.01 mM
2-(2-methylphenyl)-5-(5-methyl-1-phenyl-1H-1,2,3-triazol-4-yl)-1,3,4-oxadiazole
95% inhibition at 0.01 mM
2-(4-((5,6-dichloro-2-methyl-4-nitro-1H-benzo[d]-imidazol-1-yl)methyl)phenyl)-6-methyl-1,3,6,2-dioxazaborocane-4,8-dione
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2-(4-methylphenyl)-5-(5-methyl-1-phenyl-1H-1,2,3-triazol-4-yl)-1,3,4-oxadiazole
92% inhibition at 0.01 mM
2-(4-phenylpiperazin-1-yl)-4-(trifluoromethyl)quinazoline
92% inhibition at 0.01 mM
2-(furan-2-yl)-5-(5-methyl-1-phenyl-1H-1,2,3-triazol-4-yl)-1,3,4-oxadiazole
80% inhibition at 0.01 mM
2-chloro-N-(2-methyl-5-oxo-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-6-yl)benzamide
39% inhibition at 0.01 mM
2-chloro-N-[2-(methoxymethyl)-5-oxo-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-6-yl]benzamide
69% inhibition at 0.01 mM
2-chloro-N-[5-oxo-2-(propan-2-yl)-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-6-yl]benzamide
91% inhibition at 0.01 mM
2-methyl-4-(3-phenyl[1,2,4]triazolo[3,4-b][1,3,4]thiadiazol-6-yl)quinoline
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2-methyl-N-(4-oxo-6,7,8,9-tetrahydro-4H-pyrimido[2,1-b][1,3]benzothiazol-3-yl)benzamide
97% inhibition at 0.01 mM
2-[(2E)-2-[(1H-indol-3-yl)methylidene]hydrazinyl]-3,7-dimethylquinoline
91% inhibition at 0.01 mM
2-[(2E)-2-[(1H-indol-3-yl)methylidene]hydrazinyl]-4-methylquinoline
96% inhibition at 0.01 mM
2-[(E)-[2-(3,7-dimethylquinolin-2-yl)hydrazinylidene]methyl]cyclohexa-2,5-diene-1-thione
14% inhibition at 0.01 mM
2-[1-(4-fluorophenyl)-5-methyl-1H-1,2,3-triazol-4-yl]-5-phenyl-1,3,4-oxadiazole
93% inhibition at 0.01 mM
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
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2-[4-(3-methoxyphenyl)piperazin-1-yl]-3,5,6,7-tetrahydro-4H-cyclopenta[d]pyrimidin-4-one
64% inhibition at 0.01 mM
2-[4-(3-methoxyphenyl)piperazin-1-yl]-5,6,7,8-tetrahydroquinazolin-4(3H)-one
96% inhibition at 0.01 mM
2-[4-(3-methoxyphenyl)piperazin-1-yl]-6-methyl-5-propylpyrimidin-4(3H)-one
91% inhibition at 0.01 mM
2-[4-[(2H-1,3-benzodioxol-5-yl)methyl]piperazin-1-yl]-6-tert-butylpyrimidin-4(3H)-one
96% inhibition at 0.01 mM
2-[4-[1-(3-fluorophenyl)ethenyl]piperazin-1-yl]-4-(thiophen-2-yl)-6-(trifluoromethyl)pyrimidine
85% inhibition at 0.01 mM
2-[4-[3-(trifluoromethyl)phenyl]piperazin-1-yl]-7,8-dihydroquinazolin-5(6H)-one
89% inhibition at 0.01 mM
2-[5-cyclopropyl-1-(4-methylphenyl)-1H-1,2,3-triazol-4-yl]-5-phenyl-1,3,4-oxadiazole
93% inhibition at 0.01 mM
2-[5-methyl-1-(4-methylphenyl)-1H-1,2,3-triazol-4-yl]-5-(2-methylphenyl)-1,3,4-oxadiazole
95% inhibition at 0.01 mM
2-[[(2-chlorophenyl)methyl]sulfanyl]-6,7-dihydro-5H-cyclopenta[d][1,2,4]triazolo[1,5-a]pyrimidin-8-ol
89% inhibition at 0.01 mM
2-[[(2-chlorophenyl)methyl]sulfanyl]-6,7-dihydro[1,2,4]triazolo[5,1-b]quinazolin-8(5H)-one
87% inhibition at 0.01 mM
2-[[2-(morpholin-4-yl)-2-oxoethyl]sulfanyl]-6-phenylpyrimidin-4(5H)-one
95% inhibition at 0.01 mM
3-(2-chlorophenyl)-5-methyl-6-[4-[(pyrrolidin-1-yl)methyl]phenyl][1,2]oxazolo[4,5-c]pyridin-4(5H)-one
-
3-(2-chlorophenyl)-5-methyl-6-[4-[(pyrrolidin-1-yl)methyl]phenyl][1,2]oxazolo[5,4-d]pyrimidin-4(5H)-one
94% inhibition at 0.01 mM
3-(2-methoxyethyl)-1,6,7-trimethyl-8-phenyl-1H-imidazo[2,1-f]purine-2,4(3H,8H)-dione
46% inhibition at 0.01 mM
3-(2-methoxyethyl)-1,7-dimethyl-8-(2-phenylpropyl)-1H-imidazo[2,1-f]purine-2,4(3H,8H)-dione
63% inhibition at 0.01 mM
3-(2-methoxyethyl)-1,7-dimethyl-8-phenyl-1H-imidazo[2,1-f]purine-2,4(3H,8H)-dione
19% inhibition at 0.01 mM
3-(4-chlorophenyl)-2,5-dimethyl-6-propylpyrazolo[1,5-a]pyrimidin-7(4H)-one
complete inhibition at 0.01 mM
3-(4-methoxyphenyl)-2-methyl-5,6,7,8-tetrahydropyrazolo[5,1-b]quinazolin-9(4H)-one
99% inhibition at 0.01 mM
3-butyl-1,6,7,8-tetramethyl-1H-imidazo[2,1-f]purine-2,4(3H,8H)-dione
56% inhibition at 0.01 mM
3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
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4-((5,6-dichloro-2-methyl-4-nitro-1H-benzo[d]-imidazol-1-yl)methyl)phenol
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4-((5,6-dichloro-2-methyl-4-nitro-1H-benzo[d]imidazol-1-yl)-methyl)-2-methylthiazole
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4-((5,6-dichloro-2-methyl-4-nitro-1H-benzo[d]imidazol-1-yl)-methyl)benzaldehyde
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4-((5,6-dichloro-2-methyl-4-nitro-1H-benzo[d]imidazol-1-yl)-methyl)benzoic acid
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4-((5,6-dichloro-2-methyl-4-nitro-1H-benzo[d]imidazol-1-yl)-methyl)benzonitrile
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4-((5,6-dichloro-2-methyl-4-nitro-1H-benzo[d]imidazol-1-yl)-methyl)phenyl acetate
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4-chloro-2-phenyl-5-(piperazin-1-yl)pyridazin-3(2H)-one
53% inhibition at 0.01 mM
4-chloro-5-[4-(2,2-dimethylpropanoyl)piperazin-1-yl]-2-phenylpyridazin-3(2H)-one
95% inhibition at 0.01 mM
4-chloro-5-[4-(2-methoxybenzoyl)piperazin-1-yl]-2-phenylpyridazin-3(2H)-one
96% inhibition at 0.01 mM
4-chloro-5-[4-(4-ethoxybenzoyl)piperazin-1-yl]-2-phenylpyridazin-3(2H)-one
98% inhibition at 0.01 mM
4-chloro-5-[4-(methanesulfonyl)piperazin-1-yl]-2-phenylpyridazin-3(2H)-one
90% inhibition at 0.01 mM
4-methyl-2-[(2E)-2-[(1-methyl-1H-indol-3-yl)methylidene]hydrazinyl]quinoline
94% inhibition at 0.01 mM
4-methyl-2-[(2E)-2-[(pyridin-3-yl)methylidene]hydrazinyl]quinoline
5% inhibition at 0.01 mM
4-methyl-2-[(2E)-2-[(pyridin-4-yl)methylidene]hydrazinyl]quinoline
21% inhibition at 0.01 mM
4-methyl-N-(4-oxo-6,7,8,9-tetrahydro-4H-pyrimido[2,1-b][1,3]benzothiazol-3-yl)benzamide
23% inhibition at 0.01 mM
5,6-dichloro-1-((6-chloropyridin-3-yl)methyl)-2-methyl-4-nitro-1H-benzo[d]imidazole
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5,6-dichloro-1-(2-(3,5-dimethyl-1H-pyrazol-4-yl)ethyl)-2-methyl-4-nitro-1H-benzo[d]imidazole
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5,6-dichloro-1-(4-methoxybenzyl)-2-methyl-4-nitro-1H-benzo-[d]imidazole
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5-(2-methoxyphenyl)-2-methyl-3-phenylpyrazolo[1,5-a]pyrimidin-7(4H)-one
97% inhibition at 0.01 mM
5-(4-acetylpiperazin-1-yl)-4-chloro-2-phenylpyridazin-3(2H)-one
84% inhibition at 0.01 mM
5-(4-benzylpiperazin-1-yl)-4-chloro-2-phenylpyridazin-3(2H)-one
73% inhibition at 0.01 mM
5-benzyl-3-phenyl-6-[4-[(pyrrolidin-1-yl)methyl]phenyl][1,2]oxazolo[4,5-c]pyridin-4(5H)-one
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5-ethenyl-2-[4-(3-methoxyphenyl)piperazin-1-yl]-6-methylpyrimidin-4(3H)-one
95% inhibition at 0.01 mM
5-ethyl-2-[4-(3-methoxyphenyl)piperazin-1-yl]-6-methylpyrimidin-4(3H)-one
97% inhibition at 0.01 mM
5-ethyl-2-[4-(4-methoxyphenyl)piperazin-1-yl]-6-methylpyrimidin-4(3H)-one
96% inhibition at 0.01 mM
5-ethyl-3-[[2-(1-piperidinyl)ethyl]thio]-5H-[1,2,4]triazino[5,6-b]indole
92% inhibition at 0.01 mM
5-ethyl-8-methoxy-3-[[2-(4-morpholinyl)ethyl]thio]-5H-[1,2,4]triazino[5,6-b]indole
91% inhibition at 0.01 mM
5-ethyl-8-methyl-5H-[1,2,4]triazino[5,6-b]indole-3-thiol
2% inhibition at 0.01 mM
5-methyl-2-phenyl-6-[4-[(pyrrolidin-1-yl)methyl]phenyl]furo[3,2-c]pyridin-4(5H)-one
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5-methyl-3-(pyridin-2-yl)-6-[4-[(pyrrolidin-1-yl)methyl]phenyl][1,2]oxazolo[4,5-c]pyridin-4(5H)-one
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5-methyl-3-(pyridin-3-yl)-6-[4-[(pyrrolidin-1-yl)methyl]phenyl][1,2]oxazolo[4,5-c]pyridin-4(5H)-one
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5-methyl-3-phenyl-6-[4-[(pyrrolidin-1-yl)methyl]phenyl][1,2]oxazolo[4,5-c]pyridin-4(5H)-one
-
5-methyl-3-phenyl-6-[4-[(pyrrolidin-1-yl)methyl]phenyl][1,2]oxazolo[5,4-d]pyrimidin-4(5H)-one
88% inhibition at 0.01 mM
5-methyl-3-[[2-(1-piperidinyl)ethyl]thio]-5H-[1,2,4]triazino[5,6-b]indole
93% inhibition at 0.01 mM
5-methyl-6-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]-3-phenyl[1,2]oxazolo[4,5-c]pyridin-4(5H)-one
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5-methyl-6-[4-[(morpholin-4-yl)methyl]phenyl]-3-phenyl[1,2]oxazolo[4,5-c]pyridin-4(5H)-one
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5-[(4-hydroxyphenyl)methyl]-2-(4-phenylpiperazin-1-yl)-1,3-thiazol-4(5H)-one
96% inhibition at 0.01 mM
6-(3,4-dimethoxyphenyl)-3-(thiophen-2-yl)[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole
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6-butyl-2,5-dimethyl-3-phenylpyrazolo[1,5-a]pyrimidin-7(4H)-one
complete inhibition at 0.01 mM
6-butyl-3-(4-methoxyphenyl)-2,5-dimethylpyrazolo[1,5-a]pyrimidin-7(4H)-one
complete inhibition at 0.01 mM
6-chloro-2,5-dimethyl-3-phenylpyrazolo[1,5-a]pyrimidin-7(4H)-one
complete inhibition at 0.01 mM
6-chloro-2-(methoxymethyl)-5-methyl-3-phenylpyrazolo[1,5-a]pyrimidin-7(4H)-one
26% inhibition at 0.01 mM
6-chloro-5,7-dimethyl-N-[(2-methylphenyl)methyl][1,2,4]triazolo[1,5-a]pyrimidin-2-amine
94% inhibition at 0.01 mM
6-ethenyl-2-[4-[3-(trifluoromethyl)phenyl]piperazin-1-yl]pyrimidin-4(3H)-one
91% inhibition at 0.01 mM
6-[4-[(2H-1,3-benzodioxol-5-yl)methyl]piperazin-1-yl]-3-phenyl[1,2,4]triazolo[4,3-b]pyridazine
89% inhibition at 0.01 mM
6-[4-[(4-benzylpiperidin-1-yl)methyl]phenyl]-5-methyl-3-phenyl[1,2]oxazolo[4,5-c]pyridin-4(5H)-one
-
6-[4-[(dimethylamino)methyl]phenyl]-5-methyl-3-phenylfuro[3,2-c]pyridin-4(5H)-one
91% inhibition at 0.01 mM
6-[4-[(dimethylamino)methyl]phenyl]-5-methyl-3-phenyl[1,2]oxazolo[4,5-c]pyridin-4(5H)-one
-
7-methyl-N-phenyl-2-(pyridin-3-yl)[1,2,4]triazolo[1,5-a]pyrimidine-6-carboxamide
10% inhibition at 0.01 mM
8-benzyl-1,3,6,7-tetramethyl-1H-imidazo[2,1-f]purine-2,4(3H,8H)-dione
49% inhibition at 0.01 mM
8-benzyl-1,6,7-trimethyl-1H-imidazo[2,1-f]purine-2,4(3H,8H)-dione
85% inhibition at 0.01 mM
8-benzyl-1,7-dimethyl-1H-imidazo[2,1-f]purine-2,4(3H,8H)-dione
25% inhibition at 0.01 mM
8-benzyl-3-(2-methoxyethyl)-1,7-dimethyl-1H-imidazo[2,1-f]purine-2,4(3H,8H)-dione
93% inhibition at 0.01 mM
8-methoxy-5-methyl-3-[[2-(1-piperidinyl)ethyl]thio]-5H-[1,2,4]triazino[5,6-b]indole
70% inhibition at 0.01 mM
8-[4-(2-hydroxyphenyl)piperazin-1-yl]-1,3-dimethyl-3,7-dihydro-1H-purine-2,6-dione
96% inhibition at 0.01 mM
8-[4-(4-fluorophenyl)piperazin-1-yl]-1,3-dimethyl-3,7-dihydro-1H-purine-2,6-dione
91% inhibition at 0.01 mM
8-[4-(cyclopropanecarbonyl)piperazin-1-yl]-1,3-dimethyl-3,7-dihydro-1H-purine-2,6-dione
87% inhibition at 0.01 mM
ethyl 5-methyl-2-(pyridin-3-yl)[1,2,4]triazolo[1,5-a]pyrimidine-6-carboxylate
96% inhibition at 0.01 mM
ethyl 7-phenyl-2-(pyridin-3-yl)[1,2,4]triazolo[1,5-a]pyrimidine-6-carboxylate
69% inhibition at 0.01 mM
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)
methyl 4-((5,6-dichloro-2-methyl-4-nitro-1H-benzo[d]imidazol-1-yl)methyl)benzoate
-
methyl [3-(3,4-dimethoxyphenyl)-2,5-dimethyl-7-oxo-4,7-dihydropyrazolo[1,5-a]pyrimidin-6-yl]acetate
91% inhibition at 0.01 mM
methyl [3-(3,4-dimethoxyphenyl)-2,6-dimethyl-7-oxo-4,7-dihydropyrazolo[1,5-a]pyrimidin-5-yl]acetate
26% inhibition at 0.01 mM
N-(2-butyl-5-oxo-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-6-yl)-2-chlorobenzamide
91% inhibition at 0.01 mM
N-(2-butyl-5-oxo-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-6-yl)-2-methylbenzamide
85% inhibition at 0.01 mM
N-(2-butyl-5-oxo-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-6-yl)-4-methylbenzamide
17% inhibition at 0.01 mM
N-benzyl-2,3-dimethyl-5-oxo-5H-[1,3]thiazolo[3,2-a]pyrimidine-6-carboxamide
67% inhibition at 0.01 mM
N-ethyl-2-nitro-5-[4-(2-thienylcarbonyl)-1-piperazinyl]aniline
91% inhibition at 0.01 mM
N-[(3-bromophenyl)methyl]-6-chloro-5,7-dimethyl[1,2,4]triazolo[1,5-a]pyrimidin-2-amine
28% inhibition at 0.01 mM
N-[(4-fluorophenyl)methyl]-6-[4-(2-methylpyridine-3-sulfonyl)piperazin-1-yl]pyridazine-3-carboxamide
-
[4-(5a,9a-dihydro[1,2,4]triazolo[4,3-a]quinoxalin-4-yl)piperazin-1-yl](furan-2-yl)methanone
95% inhibition at 0.01 mM
[4-[(5,6-dichloro-2-methyl-4-nitro-1H-benzimidazol-1-yl)methyl]phenyl][2,2'-(methylazanediyl-?N)di(acetato-?O)(2-)]boron
-
[4-[3-(ethylamino)-4-nitrophenyl]piperazin-1-yl](2-methylphenyl)methanone
94% inhibition at 0.01 mM
[4-[3-(ethylamino)-4-nitrophenyl]piperazin-1-yl](4-ethylphenyl)methanone
92% inhibition at 0.01 mM
[4-[3-(ethylamino)-4-nitrophenyl]piperazin-1-yl](4-methoxyphenyl)methanone
94% inhibition at 0.01 mM
[4-[3-(ethylamino)-4-nitrophenyl]piperazin-1-yl](furan-2-yl)methanone
92% inhibition at 0.01 mM
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
-
additional information
high-throughput screening of a commercial compound (ChemBridge DiverSET) and and proprietary (Chemical Biology Consortium Sweden, CBCS) libraries revealing pyridone- and pyrimidinone-derived systems as inhibitors of the human dCTP pyrophosphatase 1 (dCTPase), structure-activity-relationships (SAR) and ligand efficiency scores are analyzed, overview. No inhibition by 6-[4-(benzyloxy)phenyl]-5-methyl-3-phenyl[1,2]oxazolo[4,5-c]pyridin-4(5H)-one and 2-methyl-N-(5-oxo-5H-[1,3]thiazolo[3,2-a]pyrimidin-6-yl)benzamide
-
additional information
-
high-throughput screening of a commercial compound (ChemBridge DiverSET) and and proprietary (Chemical Biology Consortium Sweden, CBCS) libraries revealing pyridone- and pyrimidinone-derived systems as inhibitors of the human dCTP pyrophosphatase 1 (dCTPase), structure-activity-relationships (SAR) and ligand efficiency scores are analyzed, overview. No inhibition by 6-[4-(benzyloxy)phenyl]-5-methyl-3-phenyl[1,2]oxazolo[4,5-c]pyridin-4(5H)-one and 2-methyl-N-(5-oxo-5H-[1,3]thiazolo[3,2-a]pyrimidin-6-yl)benzamide
-
additional information
high-throughput screening of a commercial compound library (ChemBridge DiverSET) revealing diverse chemotypes as inhibitors of the human dCTP pyrophosphatase 1 (dCTPase). Triazole, triazolopyrimidine, triazinoindole, quinoline hydrazone, and arylpiperazine hits are clustered, confirmed by IC50 determinations, and their preliminary structure-activity-relationships (SAR) and ligand efficiency scores are analyzed, overview
-
additional information
-
high-throughput screening of a commercial compound library (ChemBridge DiverSET) revealing diverse chemotypes as inhibitors of the human dCTP pyrophosphatase 1 (dCTPase). Triazole, triazolopyrimidine, triazinoindole, quinoline hydrazone, and arylpiperazine hits are clustered, confirmed by IC50 determinations, and their preliminary structure-activity-relationships (SAR) and ligand efficiency scores are analyzed, overview
-
additional information
discovery of selective inhibitors of human dCTP pyrophosphatase 1, synthesis of a series of benzimidazole derivatives, overview. N-Methyliminodiacetic acid (MIDA) boronate esters can be prepared from the parent boronic acids using Knapp's procedure. No inhibition by 1-(4-methoxybenzyl)-2-methyl-1H-benzo[d]imidazole
-
additional information
-
discovery of selective inhibitors of human dCTP pyrophosphatase 1, synthesis of a series of benzimidazole derivatives, overview. N-Methyliminodiacetic acid (MIDA) boronate esters can be prepared from the parent boronic acids using Knapp's procedure. No inhibition by 1-(4-methoxybenzyl)-2-methyl-1H-benzo[d]imidazole
-
additional information
discovery of a series of 3,6-disubstituted triazolothiadiazoles as potent dCTPase inhibitors. The best compounds display good correlation between enzymatic inhibition and target engagement, together with efficacy in a cellular synergy model, deeming them as a promising starting point for hit-to-lead development. Docking study, overview. The active site C of the dCTPase enzyme is used for docking. Here, the cytosine base of dCTP is wedged between Trp47 and Trp73, and formed an edge-to-face pi-pi interaction with Tyr102. H-bonds are present between the cytosine 4-amino group and His51, and the 2-oxo group and His38. Additional H-bonds are present between the ribose ring oxygen and Tyr102, the ribose 3'-OH and Asp98, the alpha-phosphate and Glu63, and the beta-phosphate and Lys121 and Arg128. The substrate triphosphate group is in close proximity to a cluster of acidic residues capable of coordinating divalent cations
-
additional information
piperazin-1-ylpyridazine derivatives as human dCTP pyrophosphatase 1 inhibitors, overview. Lead compounds increase dCTPase thermal and protease stability, display outstanding selectivity over related enzymes and synergize with a cytidine analogue against leukemic cells
-
additional information
-
piperazin-1-ylpyridazine derivatives as human dCTP pyrophosphatase 1 inhibitors, overview. Lead compounds increase dCTPase thermal and protease stability, display outstanding selectivity over related enzymes and synergize with a cytidine analogue against leukemic cells
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.24
dUTP
pH not specified in the publication, temperature not specified in the publication
0.109
5-bromo-dCTP
pH not specified in the publication, temperature not specified in the publication
0.0944
5-iodo-dCTP
pH not specified in the publication, temperature not specified in the publication
0.239
5-iodo-dCTP
-
in 50 mM Tris, pH 8.0, 100 mM KCl, 5 mM MgCl2, 100 mg/ml bovine serum albumin, 1 mM dithiothreitol, at 37°C
0.085
5-Methyl-dCTP
pH not specified in the publication, temperature not specified in the publication
0.293
dATP
pH not specified in the publication, temperature not specified in the publication
0.019
dCTP
pH and temperature not specified in the publication, recombinant enzyme
0.152
dCTP
pH not specified in the publication, temperature not specified in the publication
0.196
dTTP
pH not specified in the publication, temperature not specified in the publication
additional information
additional information
Michaelis-Menten kinetics
-
additional information
additional information
Michaelis-Menten kinetics
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.081
dUTP
pH not specified in the publication, temperature not specified in the publication
0.505
5-bromo-dCTP
pH not specified in the publication, temperature not specified in the publication
0.000864
5-iodo-dCTP
-
in 50 mM Tris, pH 8.0, 100 mM KCl, 5 mM MgCl2, 100 mg/ml bovine serum albumin, 1 mM dithiothreitol, at 37°C
0.43
5-iodo-dCTP
pH not specified in the publication, temperature not specified in the publication
0.362
5-Methyl-dCTP
pH not specified in the publication, temperature not specified in the publication
0.14
dATP
pH not specified in the publication, temperature not specified in the publication
0.367
dCTP
pH not specified in the publication, temperature not specified in the publication
0.108
dTTP
pH not specified in the publication, temperature not specified in the publication
kcat/KM VALUE [1/mMs-1]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.337
dUTP
pH not specified in the publication, temperature not specified in the publication
4.63
5-bromo-dCTP
pH not specified in the publication, temperature not specified in the publication
4.56
5-iodo-dCTP
pH not specified in the publication, temperature not specified in the publication
35
5-iodo-dCTP
-
in 50 mM Tris, pH 8.0, 100 mM KCl, 5 mM MgCl2, 100 mg/ml bovine serum albumin, 1 mM dithiothreitol, at 37°C
4.25
5-Methyl-dCTP
pH not specified in the publication, temperature not specified in the publication
0.483
dATP
pH not specified in the publication, temperature not specified in the publication
2.4
dCTP
pH not specified in the publication, temperature not specified in the publication
0.551
dTTP
pH not specified in the publication, temperature not specified in the publication
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.356
5-hydroxytriptonide
-
in 50 mM Tris, pH 8.0, 100 mM KCl, 5 mM MgCl2, 100 mg/ml bovine serum albumin, 1 mM dithiothreitol, at 37°C
0.168
triptolide
-
in 50 mM Tris, pH 8.0, 100 mM KCl, 5 mM MgCl2, 100 mg/ml bovine serum albumin, 1 mM dithiothreitol, at 37°C
0.135
triptonide
-
in 50 mM Tris, pH 8.0, 100 mM KCl, 5 mM MgCl2, 100 mg/ml bovine serum albumin, 1 mM dithiothreitol, at 37°C
0.085
triptriolide
-
in 50 mM Tris, pH 8.0, 100 mM KCl, 5 mM MgCl2, 100 mg/ml bovine serum albumin, 1 mM dithiothreitol, at 37°C
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.000046
(2-((5,6-dichloro-2-methyl-4-nitro-1H-benzo[d]imidazol-1-yl)-methyl)phenyl)boronic acid
Homo sapiens
pH 8.0, 22°C
0.0011
(2-chlorophenyl)[4-[3-(cyclopropylamino)-4-nitrophenyl]piperazin-1-yl]methanone
Homo sapiens
pH and temperature not specified in the publication
0.000082
(3-((5,6-dichloro-2-methyl-4-nitro-1H-benzo[d]imidazol-1-yl)-methyl)phenyl)boronic acid
Homo sapiens
pH 8.0, 22°C
0.000206
(4-((4-nitro-2-(trifluoromethyl)-1H-benzo[d]imidazol-1-yl)-methyl)phenyl)boronic acid
Homo sapiens
pH 8.0, 22°C
0.000027
(4-((5,6-dichloro-2-cyclopropyl-4-nitro-1H-benzo[d]imidazol-1-yl)methyl)phenyl)boronic acid
Homo sapiens
pH 8.0, 22°C
0.000248
(4-((5,6-dichloro-2-methyl-1H-benzo[d]imidazol-1-yl)methyl)-phenyl)boronic acid
Homo sapiens
pH 8.0, 22°C
0.000046
(4-((5,6-dichloro-2-methyl-4-nitro-1H-benzo[d]imidazol-1-yl)-methyl)phenyl)boronic acid
Homo sapiens
pH 8.0, 22°C
0.000529
(4-((5,6-difluoro-2-methyl-4-nitro-1H-benzo[d]imidazol-1-yl)-methyl)phenyl)boronic acid
Homo sapiens
pH 8.0, 22°C
0.0034
1,3-dimethyl-8-[4-(2-thienylcarbonyl)-1-piperazinyl]-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
pH and temperature not specified in the publication
0.000075
1-(4-(1H-pyrazol-1-yl)benzyl)-5,6-dichloro-2-methyl-4-nitro-1H-benzo[d]imidazole
Homo sapiens
pH 8.0, 22°C
0.000331
1-(4-(1H-pyrrol-1-yl)benzyl)-5,6-dichloro-2-methyl-4-nitro-1H-benzo[d]imidazole
Homo sapiens
pH 8.0, 22°C
0.022
1-(4-methoxybenzyl)-2,5,6-trimethyl-1H-benzo[d]imidazole
Homo sapiens
pH 8.0, 22°C
0.000057
1-(4-methoxybenzyl)-2,5,6-trimethyl-4-nitro-1H-benzo[d]-imidazole
Homo sapiens
pH 8.0, 22°C
0.00145
1-(4-methoxybenzyl)-2-methyl-4-nitro-1H-benzo[d]imidazole
Homo sapiens
pH 8.0, 22°C
0.00084
1-(7-methyl-2-[[(2-methylphenyl)methyl]sulfanyl][1,2,4]triazolo[1,5-a]pyrimidin-6-yl)ethan-1-one
Homo sapiens
pH and temperature not specified in the publication
0.000074
1-(benzenesulfonyl)-5,6-dichloro-2-methyl-4-nitro-1H-benzimidazole
Homo sapiens
pH 8.0, 22°C
0.000049
1-benzyl-5,6-dichloro-2-methyl-4-nitro-1H-benzo[d]imidazole
Homo sapiens
pH 8.0, 22°C
0.00089
1-[[4-(5-methyl-4-oxo-3-phenyl-4,5-dihydro[1,2]oxazolo[4,5-c]pyridin-6-yl)phenyl]methyl]pyrrolidine-2,5-dione
Homo sapiens
pH and temperature not specified in the publication
0.0014
2,3-dimethyl-5-oxo-N-(1-phenylethyl)-5H-[1,3]thiazolo[3,2-a]pyrimidine-6-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.00036
2-(2-chlorophenyl)-5-(5-methyl-1-phenyl-1H-1,2,3-triazol-4-yl)-1,3,4-oxadiazole
Homo sapiens
pH and temperature not specified in the publication
0.00086
2-(2-methylphenyl)-5-(5-methyl-1-phenyl-1H-1,2,3-triazol-4-yl)-1,3,4-oxadiazole
Homo sapiens
pH and temperature not specified in the publication
0.000047
2-(4-((5,6-dichloro-2-methyl-4-nitro-1H-benzo[d]-imidazol-1-yl)methyl)phenyl)-6-methyl-1,3,6,2-dioxazaborocane-4,8-dione
Homo sapiens
pH 8.0, 22°C
0.0013
2-(4-methylphenyl)-5-(5-methyl-1-phenyl-1H-1,2,3-triazol-4-yl)-1,3,4-oxadiazole
Homo sapiens
pH and temperature not specified in the publication
0.0026
2-(4-phenylpiperazin-1-yl)-4-(trifluoromethyl)quinazoline
Homo sapiens
pH and temperature not specified in the publication
0.0011
2-methyl-4-(3-phenyl[1,2,4]triazolo[3,4-b][1,3,4]thiadiazol-6-yl)quinoline
Homo sapiens
pH and temperature not specified in the publication, recombinant enzyme
0.00058
2-methyl-N-(4-oxo-6,7,8,9-tetrahydro-4H-pyrimido[2,1-b][1,3]benzothiazol-3-yl)benzamide
Homo sapiens
pH and temperature not specified in the publication
0.001
2-[(2E)-2-[(1H-indol-3-yl)methylidene]hydrazinyl]-3,7-dimethylquinoline
Homo sapiens
pH and temperature not specified in the publication
0.00024
2-[(2E)-2-[(1H-indol-3-yl)methylidene]hydrazinyl]-4-methylquinoline
Homo sapiens
pH and temperature not specified in the publication
0.00078
2-[1-(4-fluorophenyl)-5-methyl-1H-1,2,3-triazol-4-yl]-5-phenyl-1,3,4-oxadiazole
Homo sapiens
pH and temperature not specified in the publication
0.0148
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
pH and temperature not specified in the publication, recombinant enzyme
0.0015
2-[4-(3-methoxyphenyl)piperazin-1-yl]-3,5,6,7-tetrahydro-4H-cyclopenta[d]pyrimidin-4-one
Homo sapiens
pH and temperature not specified in the publication
0.0015
2-[4-(3-methoxyphenyl)piperazin-1-yl]-5,6,7,8-tetrahydroquinazolin-4(3H)-one
Homo sapiens
pH and temperature not specified in the publication
0.0022
2-[4-(3-methoxyphenyl)piperazin-1-yl]-6-methyl-5-propylpyrimidin-4(3H)-one
Homo sapiens
pH and temperature not specified in the publication
0.0011
2-[4-[(2H-1,3-benzodioxol-5-yl)methyl]piperazin-1-yl]-6-tert-butylpyrimidin-4(3H)-one
Homo sapiens
pH and temperature not specified in the publication
0.00099
2-[5-cyclopropyl-1-(4-methylphenyl)-1H-1,2,3-triazol-4-yl]-5-phenyl-1,3,4-oxadiazole
Homo sapiens
pH and temperature not specified in the publication
0.0021
2-[5-methyl-1-(4-methylphenyl)-1H-1,2,3-triazol-4-yl]-5-(2-methylphenyl)-1,3,4-oxadiazole
Homo sapiens
pH and temperature not specified in the publication
0.1
3,5-dimethyl-6-phenyl[1,2]oxazolo[4,5-c]pyridin-4(5H)-one
Homo sapiens
above, pH and temperature not specified in the publication
0.0016
3-(2-chlorophenyl)-5-methyl-6-[4-[(pyrrolidin-1-yl)methyl]phenyl][1,2]oxazolo[4,5-c]pyridin-4(5H)-one
Homo sapiens
pH and temperature not specified in the publication
0.00028
3-(2-chlorophenyl)-5-methyl-6-[4-[(pyrrolidin-1-yl)methyl]phenyl][1,2]oxazolo[5,4-d]pyrimidin-4(5H)-one
Homo sapiens
pH and temperature not specified in the publication
0.000021
4-((5,6-dichloro-2-methyl-4-nitro-1H-benzo[d]-imidazol-1-yl)methyl)phenol
Homo sapiens
pH 8.0, 22°C
0.00024
4-((5,6-dichloro-2-methyl-4-nitro-1H-benzo[d]imidazol-1-yl)-methyl)-2-methylthiazole
Homo sapiens
pH 8.0, 22°C
0.000133
4-((5,6-dichloro-2-methyl-4-nitro-1H-benzo[d]imidazol-1-yl)-methyl)benzaldehyde
Homo sapiens
pH 8.0, 22°C
0.000073
4-((5,6-dichloro-2-methyl-4-nitro-1H-benzo[d]imidazol-1-yl)-methyl)benzoic acid
Homo sapiens
pH 8.0, 22°C
0.000165
4-((5,6-dichloro-2-methyl-4-nitro-1H-benzo[d]imidazol-1-yl)-methyl)benzonitrile
Homo sapiens
pH 8.0, 22°C
0.000034
4-((5,6-dichloro-2-methyl-4-nitro-1H-benzo[d]imidazol-1-yl)-methyl)phenyl acetate
Homo sapiens
pH 8.0, 22°C
0.0025
4-chloro-5-[4-(2,2-dimethylpropanoyl)piperazin-1-yl]-2-phenylpyridazin-3(2H)-one
Homo sapiens
pH and temperature not specified in the publication
0.00066
4-chloro-5-[4-(2-methoxybenzoyl)piperazin-1-yl]-2-phenylpyridazin-3(2H)-one
Homo sapiens
pH and temperature not specified in the publication
0.0012
4-chloro-5-[4-(4-ethoxybenzoyl)piperazin-1-yl]-2-phenylpyridazin-3(2H)-one
Homo sapiens
pH and temperature not specified in the publication
0.0032
4-chloro-5-[4-(methanesulfonyl)piperazin-1-yl]-2-phenylpyridazin-3(2H)-one
Homo sapiens
pH and temperature not specified in the publication
0.00037
4-methyl-2-[(2E)-2-[(1-methyl-1H-indol-3-yl)methylidene]hydrazinyl]quinoline
Homo sapiens
pH and temperature not specified in the publication
0.000185
5,6-dichloro-1-((6-chloropyridin-3-yl)methyl)-2-methyl-4-nitro-1H-benzo[d]imidazole
Homo sapiens
pH 8.0, 22°C
0.000109
5,6-dichloro-1-(2-(3,5-dimethyl-1H-pyrazol-4-yl)ethyl)-2-methyl-4-nitro-1H-benzo[d]imidazole
Homo sapiens
pH 8.0, 22°C
0.012
5,6-dichloro-1-(4-methoxybenzyl)-2-methyl-1H-benzo[d]-imidazole
Homo sapiens
pH 8.0, 22°C
0.000041
5,6-dichloro-1-(4-methoxybenzyl)-2-methyl-4-nitro-1H-benzo-[d]imidazole
Homo sapiens
pH 8.0, 22°C
0.000019
5,6-dichloro-2-methyl-1-(4-methylbenzyl)-4-nitro-1H-benzo[d]-imidazole
Homo sapiens
pH 8.0, 22°C
0.000205
5,6-dichloro-2-methyl-4-nitro-1-(phenylsulfonyl)-1H-benzo[d]imidazole
Homo sapiens
pH 8.0, 22°C
0.000085
5,6-dichloro-2-methyl-4-nitro-1-phenyl-1H-benzo-[d]imidazole
Homo sapiens
pH 8.0, 22°C
0.0018
5-benzyl-3-phenyl-6-[4-[(pyrrolidin-1-yl)methyl]phenyl][1,2]oxazolo[4,5-c]pyridin-4(5H)-one
Homo sapiens
pH and temperature not specified in the publication
0.0015
5-ethenyl-2-[4-(3-methoxyphenyl)piperazin-1-yl]-6-methylpyrimidin-4(3H)-one
Homo sapiens
pH and temperature not specified in the publication
0.0014
5-ethyl-2-[4-(3-methoxyphenyl)piperazin-1-yl]-6-methylpyrimidin-4(3H)-one
Homo sapiens
pH and temperature not specified in the publication
0.0011
5-ethyl-2-[4-(4-methoxyphenyl)piperazin-1-yl]-6-methylpyrimidin-4(3H)-one
Homo sapiens
pH and temperature not specified in the publication
0.00094
5-ethyl-3-[[2-(1-piperidinyl)ethyl]thio]-5H-[1,2,4]triazino[5,6-b]indole
Homo sapiens
pH and temperature not specified in the publication
0.00055
5-ethyl-8-methoxy-3-[[2-(4-morpholinyl)ethyl]thio]-5H-[1,2,4]triazino[5,6-b]indole
Homo sapiens
pH and temperature not specified in the publication
0.1
5-methyl-2-phenyl-6-[4-[(pyrrolidin-1-yl)methyl]phenyl]furo[3,2-c]pyridin-4(5H)-one
Homo sapiens
above, pH and temperature not specified in the publication
0.1
5-methyl-3,6-diphenyl[1,2]oxazolo[4,5-c]pyridin-4(5H)-one
Homo sapiens
above, pH and temperature not specified in the publication
0.0084
5-methyl-3-(pyridin-2-yl)-6-[4-[(pyrrolidin-1-yl)methyl]phenyl][1,2]oxazolo[4,5-c]pyridin-4(5H)-one
Homo sapiens
pH and temperature not specified in the publication
0.00085
5-methyl-3-(pyridin-3-yl)-6-[4-[(pyrrolidin-1-yl)methyl]phenyl][1,2]oxazolo[4,5-c]pyridin-4(5H)-one
Homo sapiens
pH and temperature not specified in the publication
0.0015
5-methyl-3-phenyl-6-[4-[(pyrrolidin-1-yl)methyl]phenyl][1,2]oxazolo[4,5-c]pyridin-4(5H)-one
Homo sapiens
pH and temperature not specified in the publication
0.0016
5-methyl-3-phenyl-6-[4-[(pyrrolidin-1-yl)methyl]phenyl][1,2]oxazolo[5,4-d]pyrimidin-4(5H)-one
Homo sapiens
pH and temperature not specified in the publication
0.00191
5-methyl-3-[[2-(1-piperidinyl)ethyl]thio]-5H-[1,2,4]triazino[5,6-b]indole
Homo sapiens
pH and temperature not specified in the publication
0.0014
5-methyl-6-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]-3-phenyl[1,2]oxazolo[4,5-c]pyridin-4(5H)-one
Homo sapiens
pH and temperature not specified in the publication
0.0012
5-methyl-6-[4-[(morpholin-4-yl)methyl]phenyl]-3-phenyl[1,2]oxazolo[4,5-c]pyridin-4(5H)-one
Homo sapiens
pH and temperature not specified in the publication
0.00052
5-[(4-hydroxyphenyl)methyl]-2-(4-phenylpiperazin-1-yl)-1,3-thiazol-4(5H)-one
Homo sapiens
pH and temperature not specified in the publication
0.00002
6-(3,4-dimethoxyphenyl)-3-(thiophen-2-yl)[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole
Homo sapiens
pH and temperature not specified in the publication
0.00062
6-chloro-5,7-dimethyl-N-[(2-methylphenyl)methyl][1,2,4]triazolo[1,5-a]pyrimidin-2-amine
Homo sapiens
pH and temperature not specified in the publication
0.001
6-ethenyl-2-[4-[3-(trifluoromethyl)phenyl]piperazin-1-yl]pyrimidin-4(3H)-one
Homo sapiens
pH and temperature not specified in the publication
0.1
6-[4-[(4-benzylpiperidin-1-yl)methyl]phenyl]-5-methyl-3-phenyl[1,2]oxazolo[4,5-c]pyridin-4(5H)-one
Homo sapiens
above, pH and temperature not specified in the publication
0.0009
6-[4-[(dimethylamino)methyl]phenyl]-5-methyl-3-phenyl[1,2]oxazolo[4,5-c]pyridin-4(5H)-one
Homo sapiens
pH and temperature not specified in the publication
0.0086
8-[4-(2-hydroxyphenyl)piperazin-1-yl]-1,3-dimethyl-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
pH and temperature not specified in the publication
0.0021
8-[4-(4-fluorophenyl)piperazin-1-yl]-1,3-dimethyl-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
pH and temperature not specified in the publication
0.000044
benzimidazole
Homo sapiens
pH and temperature not specified in the publication, recombinant enzyme
0.00085
ethyl 5-methyl-2-(pyridin-3-yl)[1,2,4]triazolo[1,5-a]pyrimidine-6-carboxylate
Homo sapiens
pH and temperature not specified in the publication
0.0033
methyl 2-(4-methoxyphenyl)-3-methyl-4-oxo-3,4-dihydro[1]benzopyrano[3,4-b]pyrrole-1-carboxylate
Homo sapiens
pH and temperature not specified in the publication, recombinant enzyme
0.000095
methyl 4-((5,6-dichloro-2-methyl-4-nitro-1H-benzo[d]imidazol-1-yl)methyl)benzoate
Homo sapiens
pH 8.0, 22°C
0.00099
N-ethyl-2-nitro-5-[4-(2-thienylcarbonyl)-1-piperazinyl]aniline
Homo sapiens
pH and temperature not specified in the publication
0.000036
N-[(4-fluorophenyl)methyl]-6-[4-(2-methylpyridine-3-sulfonyl)piperazin-1-yl]pyridazine-3-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.00098
[4-(5a,9a-dihydro[1,2,4]triazolo[4,3-a]quinoxalin-4-yl)piperazin-1-yl](furan-2-yl)methanone
Homo sapiens
pH and temperature not specified in the publication
0.000047
[4-[(5,6-dichloro-2-methyl-4-nitro-1H-benzimidazol-1-yl)methyl]phenyl][2,2'-(methylazanediyl-?N)di(acetato-?O)(2-)]boron
Homo sapiens
pH and temperature not specified in the publication
0.00081
[4-[3-(ethylamino)-4-nitrophenyl]piperazin-1-yl](2-methylphenyl)methanone
Homo sapiens
pH and temperature not specified in the publication
0.00091
[4-[3-(ethylamino)-4-nitrophenyl]piperazin-1-yl](4-ethylphenyl)methanone
Homo sapiens
pH and temperature not specified in the publication
0.0015
[4-[3-(ethylamino)-4-nitrophenyl]piperazin-1-yl](4-methoxyphenyl)methanone
Homo sapiens
pH and temperature not specified in the publication
pH RANGE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
additional information
additional information
DCTPP1 is highly expressed in embryonic and proliferative tissues with an expanded nucleotide pool. The enzyme is also upregulated in multiple human carcinomas and cancer stem cells
additional information
-
DCTPP1 is highly expressed in embryonic and proliferative tissues with an expanded nucleotide pool. The enzyme is also upregulated in multiple human carcinomas and cancer stem cells
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
malfunction
metabolism
physiological function
additional information
malfunction
down-regulation of the enzyme increases decitabine-induced toxicity in HeLa and MRC-5 cells at a wide range of doses
malfunction
dUTPase or DCTPP1 downregulation enhances the cytotoxic effect of decitabine producing an accumulation of nucleoside triphosphates containing uracil as well as uracil misincorporation and double-strand breaks in genomic DNA. Downregulation of DCTPP1 or dUTPase increases the toxic effect of decitabine in HeLa cells or in the non-tumoral cell line MRC-5. In contrast, cells transfected with the non-targeting siRNA pool do not exhibit a decrease in viability even in the presence of 0.1 mM decitabine. The protective effect is specific for decitabine since the absence of DCTPP1 or dUTPase do not have a significant impact on cell proliferation after exposure to the canonical nucleoside deoxycytidine or to the cytidine analogue cytarabine. DCTPP1 or dUTPase-deficient cells incubated with decitabine also display a reduced colony-forming capacity compared with control cells
malfunction
nucleotide pools and the dUTP/dTTP ratio are severely altered in DCTPP1-deficient cells, which exhibit an accumulation of uracil in genomic DNA, the activation of the DNA damage response and both a mitochondrial and nuclear hypermutator phenotype. DNA damage can be reverted by incubation with thymidine, dUTPase overexpression or uracil-DNA glycosylase suppression. Moreover, DCTPP1-deficient cells are highly sensitive to downregulation of nucleoside salvage. DCTPP1-deficient cells accumulate high levels of dCTP and are hypersensitive to exposure to the nucleoside analogues 5-iodo-2'-deoxycytidine and 5-methyl-2'-deoxycytidine. Downregulation of DCTPP1 expression impairs proliferation and perturbs the dNTP pool of MCF-7 cells. DCTPP1-deficient cells are more prone to uracil misincorporation and exhibit an activated DNA damage response (DDR), altered cell cycle progression, and a mutator phenotype that affects both chromosomal and mitochondrial DNA (mtDNA)
malfunction
potent and selective dCTPase inhibitors enhance the cytotoxic effect of cytidine analogues in leukemia cells
metabolism
DCTPP1 (dCTP pyrophosphatase 1) and dUTPase are two house-cleaning nucleotidohydrolases involved in the elimination of non-canonical nucleotides. Exposure of HeLa cells to decitabine upregulates the expression of several pyrimidine metabolic enzymes including DCTPP1, dUTPase, dCMP deaminase and thymidylate synthase, thus suggesting their contribution to the cellular response to this anti-cancer nucleoside. In addition to the formation of aza-dCTP (5-aza-2'-deoxycytidine-5'-triphosphate), an alternative cytotoxic mechanism for decitabine may involve the formation of aza-dUMP, a potential thymidylate synthase inhibitor
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
metabolism
the enzyme contributes to the cellular response to the anti-cancer nucleoside decitabine. Exposure of HeLa cells to decitabine upregulates the expression of several pyrimidine metabolic enzymes including DCTPP1, dUTPase, dCMP deaminase and thymidylate synthase. DCTPP1 down-regulation enhances the cytotoxic effect of decitabine producing an accumulation of nucleoside triphosphates containing uracil as well as uracil misincorporation and double-strand breaks in genomic DNA
physiological function
DCTPP1-deficient cells accumulate high levels of dCTP and are hypersensitive to exposure to the nucleoside analogues 5-iodo-2'-deoxycytidine and 5-methyl-2'-deoxycytidine
physiological function
knockdown of DCTPP1 in breast cancer cell line MCF-7 cells remarkably retards proliferation and colony formation in vitro. The capacity of mammosphere formation of MCF-7 is suppressed with the silence of DCTPP1, consistent with the enhanced mammosphere-forming ability in DCTPP1-overexpressing MDA-MB-231 cells. The global methylation level is elevated in DCTPP1-knockdown MCF-7 cells or mammosphere-forming MCF-7 cells but decreased significantly in DCTPP1-overexpressing MDA-MB-231 cells and its mammosphere
physiological function
DCTPP1 hydrolyses the triphosphate form of decitabine with similar kinetic efficiency to its natural substrate dCTP and prevents decitabine-induced global DNA demethylation. The nucleotidohydrolases DCTPP1 and dUTPase are factors involved in the mode of action of decitabine with potential value as enzymatic targets to improve decitabine-based chemotherapy
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
physiological function
the dCTP pyrophosphatase 1 (dCTPase) is involved in the regulation of the cellular dNTP pool and has been linked to cancer progression
physiological function
the dCTPase pyrophosphatase 1 (dCTPase) is an all-alpha nucleoside triphosphate (NTP) pyrophosphatase responsible for dNTP pool house-cleaning. It regulates the intracellular nucleotide pool through hydrolytic degradation of canonical and noncanonical nucleotide triphosphates (dNTPs). dCTPase is highly expressed in multiple carcinomas and is associated with cancer cell stemness
physiological function
-
the dCTPase pyrophosphatase 1 (dCTPase) is an all-alpha nucleoside triphosphate (NTP) pyrophosphatase responsible for dNTP pool house-cleaning. It regulates the intracellular nucleotide pool through hydrolytic degradation of canonical and noncanonical nucleotide triphosphates (dNTPs). dCTPase is highly expressed in multiple carcinomas and is associated with cancer cell stemness
physiological function
To maintain dNTP pool homeostasis and preserve genetic integrity of nuclear and mitochondrial genomes, the synthesis and degradation of DNA precursors must be precisely regulated. Central role for DCTPP1 in the homeostasis of dCTP, dTTP and dUTP. Human all-alpha dCTP pyrophosphatase 1 (DCTPP1) is a dNTP pyrophosphatase with high affinity for dCTP and 5'-modified dCTP derivatives. DCTPP1 is crucially involved in the provision of dCMP for thymidylate biosynthesis, introducing another player in the regulation of pyrimidine dNTP levels and the maintenance of genomic integrity. DCTPP1 catalyzes the hydrolysis of dCTP into dCMP and diphosphate keeping the cellular dCTP pool balanced. DCTPP1 can also hydrolyze in vitro C5-modified dNTPs such as 5-halogenated, 5-methyl and 5-formyl deoxycytidine, and therefore may have an additional house-cleaning function. Central role of DCTPP1 in the formation of dCMP for dTMP biosynthesis
additional information
-
decitabine (5-aza-2x02-deoxycytidine, aza-dCyd) is an anti-cancer drug used clinically for the treatment of myelodysplastic syndromes and acute myeloid leukaemia that can act as a DNA-demethylating or genotoxic agent in a dose-dependent manner. It upregulates the enzyme in HeLa cells. Decitabine is metabolically activated in vivo through consecutive phosphorylations into aza-dCTP (5-aza-2'-deoxycytidine-5'-triphosphate) that is readily incorporated into DNA and extended by the DNA polymerase. Once in DNA, decitabine acts as a suicidal substrate by covalently trapping DNMT (DNA methyltransferase) molecules that attempt to initiate cytosine methylation. The resulting DNA-protein cross-links trigger the proteasomal degradation machinery and lead to the depletion of the DNA methylation activities of the cell. Consequently, the replacement of deoxycytidine by decitabine results in hypomethylation at the promoter DNA regions and the reactivation of epigenetically repressed genes
additional information
decitabine (5-aza-2x02-deoxycytidine, aza-dCyd) is an anti-cancer drug used clinically for the treatment of myelodysplastic syndromes and acute myeloid leukaemia that can act as a DNA-demethylating or genotoxic agent in a dose-dependent manner. It upregulates the enzyme in HeLa cells. Decitabine is metabolically activated in vivo through consecutive phosphorylations into aza-dCTP (5-aza-2'-deoxycytidine-5'-triphosphate) that is readily incorporated into DNA and extended by the DNA polymerase. Once in DNA, decitabine acts as a suicidal substrate by covalently trapping DNMT (DNA methyltransferase) molecules that attempt to initiate cytosine methylation. The resulting DNA-protein cross-links trigger the proteasomal degradation machinery and lead to the depletion of the DNA methylation activities of the cell. Consequently, the replacement of deoxycytidine by decitabine results in hypomethylation at the promoter DNA regions and the reactivation of epigenetically repressed genes
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable).
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable). DCTP1_HUMAN
170
0
18681
Swiss-Prot
other Location (Reliability: 2)
PDB
SCOP
CATH
UNIPROT
ORGANISM
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
CRYSTALLIZATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
generation of 3D models of DCTPP1 and its 5-methyl-dCTP-bound tetramer based on X-ray crystal structure of the tetrameric mouse dCTPase 1, PDB entry 2OIG. The cytosines of substrates 5-methyl-dCTP and dCTP bind deeply into the substrate pocket, which is composed of the residues from the dimer interface, including His38, Trp47, Glu63, Glu66, Trp73, Glu95, Asp98 and Tyr102
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
additional information
construction of DCTPP1-deficient MCF-7 cells, which exhibit increased uracil misincorporation and an activation of the DNA damage response. Downregulation of DCTPP1 expression impairs proliferation and perturbs the dNTP pool of MCF-7 cells. Modulation of the dUTP/dTTP ratio reduces genomic instability. The downregulation of DCTPP1 has profound consequences on cell cycle progression, nucleotide pools. Phneotype of a bona fide DCTPP1-knockout (DCTPP1-KO) cell line derived from the HAP1 cell line, overview. HAP1 is a near haploid human cell line that is derived from the male chronic myelogenous leukemia (CML) cell line KBM-7, and deletion in exon 2 of the DCTPP1 gene is generated using the CRISPR/Cas9 technology. No differences in the pool of dGTP are observed between HAP1 wild-type and DCTPP1-KO cell lines. dUTP pool with potential genotoxic consequences is exclusively detected in deficient cells. The dCTP pool is similar for HAP1 wild-type and DCTPP1-KO cell lines. DCTPP1-knockout cells exhibit normal proliferation in spite of an imbalanced nucleotide pool. DCTPP1-KO cells exhibit a hypermutator phenotype. The activation of the DNA damage response upon DCTPP1 inactivation can be reverted by the expansion of the dTTP pool or defects in uracil excision. Phenotypes, detailed overview
additional information
-
construction of DCTPP1-deficient MCF-7 cells, which exhibit increased uracil misincorporation and an activation of the DNA damage response. Downregulation of DCTPP1 expression impairs proliferation and perturbs the dNTP pool of MCF-7 cells. Modulation of the dUTP/dTTP ratio reduces genomic instability. The downregulation of DCTPP1 has profound consequences on cell cycle progression, nucleotide pools. Phneotype of a bona fide DCTPP1-knockout (DCTPP1-KO) cell line derived from the HAP1 cell line, overview. HAP1 is a near haploid human cell line that is derived from the male chronic myelogenous leukemia (CML) cell line KBM-7, and deletion in exon 2 of the DCTPP1 gene is generated using the CRISPR/Cas9 technology. No differences in the pool of dGTP are observed between HAP1 wild-type and DCTPP1-KO cell lines. dUTP pool with potential genotoxic consequences is exclusively detected in deficient cells. The dCTP pool is similar for HAP1 wild-type and DCTPP1-KO cell lines. DCTPP1-knockout cells exhibit normal proliferation in spite of an imbalanced nucleotide pool. DCTPP1-KO cells exhibit a hypermutator phenotype. The activation of the DNA damage response upon DCTPP1 inactivation can be reverted by the expansion of the dTTP pool or defects in uracil excision. Phenotypes, detailed overview
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
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
dCTPP1 co-elutes with USP7 in gel filtration shift assays with recombinant USP7 and dCTPP1 from HCT-116 cell extract
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
gene DCTTP1, recombinant expression in HEK293 cells and of FLAG-tagged dCTPP1 in HCT-116 cells
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
exposure of HeLa cells to decitabine upregulates the expression of several pyrimidine metabolic enzymes including DCTPP1, dUTPase, dCMP deaminase and thymidylate synthase
exposure of HeLa or MRC-5 cells to decitabine (5-aza-2'-deoxycytidine, aza-dCyd), an anti-cancer drug, upregulates the expression of several pyrimidine metabolic enzymes including DCTPP1, dUTPase, dCMP deaminase and thymidylate synthase, thus suggesting their contribution to the cellular response to this anti-cancer nucleoside
neither knockdown nor over-expression of DCTPP1 significantly modifies the fraction of anti-BrdU reactive cells
-
APPLICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
drug development
medicine
enzyme accumulates in the nucleus of cancer cells compared to the paired adjacent tissue cells in multiple carcinomas including lung, breast, liver, cervical, gastric and esophagus cancer. The higher expression in the nucleus of lung, gastric and esophagus cancer cells is associated with histological subtypes. The nucleic accumulation is apparently observed as well when tumor cell line MCF-7 is treated with H2O2 in vitro
drug development
DCTPP1 counteracts the cytotoxic effect of the antitumoral demethylating agent decitabine (5-aza-deoxycytidine) by removing 5-aza-dCTP from the nucleotide pool and is being studied as a potential drug target to improve decitabine-based chemotherapy
drug development
the enzyme is a factor involved in the mode of action of decitabine with potential value as enzymatic targets to improve decitabine-based chemotherapy
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Corson, T.W.; Cavga, H.; Aberle, N.; Crews, C.M.
Triptolide directly inhibits dCTP pyrophosphatase
ChemBioChem
12
1767-1773
2011
Homo sapiens
Requena, C.E.; Perez-Moreno, G.; Ruiz-Perez, L.M.; Vidal, A.E.; Gonzalez-Pacanowska, D.
The NTP pyrophosphatase DCTPP1 contributes to the homoeostasis and cleansing of the dNTP pool in human cells
Biochem. J.
459
171-180
2014
Homo sapiens (Q9H773), Homo sapiens
Zhang, Y.; Ye, W.Y.; Wang, J.Q.; Wang, S.J.; Ji, P.; Zhou, G.Y.; Zhao, G.P.; Ge, H.L.; Wang, Y.
dCTP pyrophosphohydrase exhibits nucleic accumulation in multiple carcinomas
Eur. J. Histochem.
57
e29
2013
Homo sapiens (Q9H773), Homo sapiens
Song, F.F.; Xia, L.L.; Ji, P.; Tang, Y.B.; Huang, Z.M.; Zhu, L.; Zhang, J.; Wang, J.Q.; Zhao, G.P.; Ge, H.L.; Zhang, Y.; Wang, Y.
Human dCTP pyrophosphatase 1 promotes breast cancer cell growth and stemness through the modulation on 5-methyl-dCTP metabolism and global hypomethylation
Oncogenesis
4
e159
2015
Homo sapiens (Q9H773), Homo sapiens
Friese, A.; Kapoor, S.; Schneidewind, T.; Vidadala, S.R.; Sardana, J.; Brause, A.; Foerster, T.; Bischoff, M.; Wagner, J.; Janning, P.; Ziegler, S.; Waldmann, H.
Chemical genetics reveals a role of dCTP pyrophosphatase 1 in Wnt signaling
Angew. Chem. Int. Ed. Engl.
58
13009-13013
2019
Homo sapiens (Q9H773)
Guiomar, P.; Andras, H.; Beata, G.; Luis, M.; Dolores, G.; Requena, C.; Vidal, A.
The nucleotidohydrolases DCTPP1 and dUTPase are involved in the cellular response to decitabine
Biochem. J.
473
2635-2643
2016
Homo sapiens, Homo sapiens (Q9H773)
Llona-Minguez, S.; Haeggblad, M.; Martens, U.; Johansson, L.; Sigmundsson, K.; Lundbaeck, T.; Loseva, O.; Jemth, A.S.; Lundgren, B.; Jensen, A.J.; Scobie, M.; Helleday, T.
Diverse heterocyclic scaffolds as dCTP pyrophosphatase 1 inhibitors. Part 2 pyridone- and pyrimidinone-derived systems
Bioorg. Med. Chem. Lett.
27
3219-3225
2017
Homo sapiens (Q9H773), Homo sapiens
Llona-Minguez, S.; Haeggblad, M.; Martens, U.; Throup, A.; Loseva, O.; Jemth, A.S.; Lundgren, B.; Scobie, M.; Helleday, T.
Diverse heterocyclic scaffolds as dCTP pyrophosphatase 1 inhibitors. Part 1 triazoles, triazolopyrimidines, triazinoindoles, quinoline hydrazones and arylpiperazines
Bioorg. Med. Chem. Lett.
27
3897-3904
2017
Homo sapiens (Q9H773), Homo sapiens
Martinez-Arribas, B.; Requena, C.E.; Perez-Moreno, G.; Ruiz-Perez, L.M.; Vidal, A.E.; Gonzalez-Pacanowska, D.
DCTPP1 prevents a mutator phenotype through the modulation of dCTP, dTTP and dUTP pools
Cell. Mol. Life Sci.
77
1645-1660
2019
Homo sapiens (Q9H773), Homo sapiens
Llona-Minguez, S.; Hoeglund, A.; Jacques, S.A.; Johansson, L.; Calderon-Montano, J.M.; Claesson, M.; Loseva, O.; Valerie, N.C.K.; Lundbaeck, T.; Piedrafita, J.; Maga, G.; Crespan, E.; Meijer, L.; Moron, E.B.; Baranczewski, P.; Hagbjoerk, A.L.; Svensson, R.; Wiita, E.; Almloef, I.; Visnes, T.; Jeppsson, F.; Sigmundsson, K.; Jensen, A.J.; Artursson, P.; Jemth, A.-S.; Stenmark, P.; Berglund, U.W.; Scobie, M.; Helleday, T.
Discovery of the first potent and selective inhibitors of human dCTP pyrophosphatase 1
J. Med. Chem.
59
1140-1148
2016
Homo sapiens (Q9H773), Homo sapiens
Llona-Minguez, S.; Hoeglund, A.; Wiita, E.; Almloef, I.; Mateus, A.; Calderon-Montano, J.M.; Cazares-Koerner, C.; Homan, E.; Loseva, O.; Baranczewski, P.; Jemth, A.S.; Haeggblad, M.; Martens, U.; Lundgren, B.; Artursson, P.; Lundbaeck, T.; Jenmalm Jensen, A.; Warpman Berglund, U.; Scobie, M.; , H.
Identification of triazolothiadiazoles as potent inhibitors of the dCTP pyrophosphatase 1
J. Med. Chem.
60
2148-2154
2017
Homo sapiens (Q9H773)
Llona-Minguez, S.; Hoeglund, A.; Ghassemian, A.; Desroses, M.; Calderon-Montano, J.M.; Burgos Moron, E.; Valerie, N.C.K.; Wiita, E.; Almloef, I.; Koolmeister, T.; Mateus, A.; Cazares-Koerner, C.; Sanjiv, K.; Homan, E.; Loseva, O.; Baranczewski, P.; Darabi, M.; Mehdizadeh, A.; Fayezi, S.; Jemth, A.
Piperazin-1-ylpyridazine derivatives are a novel class of human dCTP pyrophosphatase 1 inhibitors
J. Med. Chem.
60
4279-4292
2017
Homo sapiens (Q9H773), Homo sapiens
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