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Information on EC 3.6.1.12 - dCTP diphosphatase
for references in articles please use BRENDA:EC3.6.1.12
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EC Tree 3 Hydrolases
3.6 Acting on acid anhydrides
3.6.1 In phosphorus-containing anhydrides
3.6.1.12 dCTP diphosphatase
IUBMB 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.
The enzyme appears in viruses and cellular organisms
- 3.6.1.12
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nudix
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mutt
- ap4a
-
diadenosine
-
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
showSynonyms
pyrophosphohydrolase, dctpp1, dctpase, rs21-c6, ntp pyrophosphohydrolase, dctp pyrophosphatase 1, dctpase-dutpase, ntp pyrophosphatase, dctp pyrophosphatase, xtp3-transactivated protein a, more
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SYNONYM 
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
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT
LITERATURE
dCTP + H2O = dCMP + diphosphate
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
hydrolysis of phosphoric ester
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PATHWAY SOURCE
PATHWAYS
BRENDA
MetaCyc
pyrimidine deoxyribonucleotides dephosphorylation
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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.
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CAS REGISTRY NUMBER
COMMENTARY
9024-87-7
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SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
LITERATURE
COMMENTARY
Reversibility
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
2-chloro-dATP + H2O
2-chloro-AMP + diphosphate
Substrates: -
Products: -
Products: -
?
2-hydroxy-dATP + H2O
2-hydroxy-dAMP + diphosphate
Substrates: -
Products: -
Products: -
?
5-chloro-dCTP + H2O
5-chloro-dCMP + diphosphate
Substrates: -
Products: -
Products: -
?
5-fluoro-dUTP + H2O
5-fluoro-dUMP + diphosphate
Substrates: -
Products: -
Products: -
?
5-formyl-dCTP + H2O
5-formyl-dCMP + diphosphate
Substrates: -
Products: -
Products: -
?
5-hydroxy-dCTP + H2O
5-hydroxy-dCMP + diphosphate
Substrates: -
Products: -
Products: -
?
5-hydroxymethyl-dCTP + H2O
5-hydroxymethyl-dCMP + diphosphate
Substrates: -
Products: -
Products: -
?
aza-dCTP + H2O
dCMP + diphosphate
Substrates: 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
Products: -
Products: -
?
5-bromo-dCTP + H2O
5-bromo-dCMP + diphosphate
Substrates: -
Products: -
Products: -
?
5-bromo-dCTP + H2O
5-bromo-dCMP + diphosphate
Substrates: -
Products: -
Products: -
?
5-iodo-dCTP + H2O
5-iodo-dCMP + diphosphate
Substrates: -
Products: -
Products: -
?
5-iodo-dCTP + H2O
5-iodo-dCMP + diphosphate
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Substrates: good substrate
Products: -
Products: -
?
5-methyl-dCTP + H2O
5-methyl-dCMP + diphosphate
Substrates: -
Products: -
Products: -
?
5-methyl-dCTP + H2O
5-methyl-dCMP + diphosphate
Substrates: -
Products: -
Products: -
?
5-methyl-dCTP + H2O
5-methyl-dCMP + diphosphate
Substrates: -
Products: -
Products: -
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dCTP + H2O
dCMP + diphosphate
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Substrates: the enzyme is essential for normal development of all T-even phages. It prevents the incorporation of dC into phage DNA by hydrolyzing dCTP and dCDP. No role of the T4 dCTPase protein in either the host-dependent or the host-independent exclusion of phage T2 by T4
Products: -
Products: -
?
dCTP + H2O
dCMP + diphosphate
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Substrates: enzyme of salvage synthesis of pyrimidine deoxyribonucleotides
Products: -
Products: -
?
dCTP + H2O
dCMP + diphosphate
Tequatrovirus T4
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Substrates: -
Products: -
Products: -
?
dCTP + H2O
dCMP + diphosphate
Tequatrovirus T4
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Substrates: the enzyme is essential for normal development of all T-even phages. It prevents the incorporation of dC into phage DNA by hydrolyzing dCTP and dCDP. No role of the T4 dCTPase protein in either the host-dependent or the host-independent exclusion of phage T2 by T4
Products: -
Products: -
?
additional information
?
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Substrates: gemcitabine triphosphate is no substrate
Products: -
Products: -
?
additional information
?
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Substrates: no substrtaes: ATP, CTP, UTP, dCDP, 5-methyl-dCDP, dGTP. Poor substrate: dUTP
Products: -
Products: -
?
additional information
?
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Substrates: no substrtaes: ATP, CTP, UTP, dCDP, 5-methyl-dCDP, dGTP. Poor substrate: dUTP
Products: -
Products: -
?
additional information
?
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Substrates: human all-alpha dCTP pyrophosphatase 1 (DCTPP1) is a dNTP pyrophosphatase with high affinity for dCTP and 5'-modified dCTP derivatives
Products: -
Products: -
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additional information
?
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Substrates: human all-alpha dCTP pyrophosphatase 1 (DCTPP1) is a dNTP pyrophosphatase with high affinity for dCTP and 5'-modified dCTP derivatives
Products: -
Products: -
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additional information
?
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Substrates: no substrates: ATP, GTP, UTP, ITP, 2-hydroxy-ATP, dGTP, dITP, 8-oxo-dGTP, dCDP, dADP
Products: -
Products: -
?
additional information
?
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Substrates: no substrates: ATP, GTP, UTP, ITP, 2-hydroxy-ATP, dGTP, dITP, 8-oxo-dGTP, dCDP, dADP
Products: -
Products: -
?
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NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
LITERATURE
COMMENTARY
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
5-methyl-dCTP + H2O
5-methyl-dCMP + diphosphate
Substrates: -
Products: -
Products: -
?
dCTP + H2O
dCMP + diphosphate
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Substrates: the enzyme is essential for normal development of all T-even phages. It prevents the incorporation of dC into phage DNA by hydrolyzing dCTP and dCDP. No role of the T4 dCTPase protein in either the host-dependent or the host-independent exclusion of phage T2 by T4
Products: -
Products: -
?
dCTP + H2O
dCMP + diphosphate
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Substrates: enzyme of salvage synthesis of pyrimidine deoxyribonucleotides
Products: -
Products: -
?
dCTP + H2O
dCMP + diphosphate
Tequatrovirus T4
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Substrates: the enzyme is essential for normal development of all T-even phages. It prevents the incorporation of dC into phage DNA by hydrolyzing dCTP and dCDP. No role of the T4 dCTPase protein in either the host-dependent or the host-independent exclusion of phage T2 by T4
Products: -
Products: -
?
additional information
?
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Substrates: human all-alpha dCTP pyrophosphatase 1 (DCTPP1) is a dNTP pyrophosphatase with high affinity for dCTP and 5'-modified dCTP derivatives
Products: -
Products: -
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additional information
?
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Substrates: human all-alpha dCTP pyrophosphatase 1 (DCTPP1) is a dNTP pyrophosphatase with high affinity for dCTP and 5'-modified dCTP derivatives
Products: -
Products: -
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METALS and IONS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
Mg2+
additional information
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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
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(4-((5,6-dichloro-2-cyclopropyl-4-nitro-1H-benzo[d]imidazol-1-yl)methyl)phenyl)boronic acid
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(4-((5,6-dichloro-2-methyl-1H-benzo[d]imidazol-1-yl)methyl)-phenyl)boronic acid
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(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
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1-(4-(1H-pyrrol-1-yl)benzyl)-5,6-dichloro-2-methyl-4-nitro-1H-benzo[d]imidazole
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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
-
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
-
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
-
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
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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
-
4-((5,6-dichloro-2-methyl-4-nitro-1H-benzo[d]-imidazol-1-yl)methyl)phenol
-
4-((5,6-dichloro-2-methyl-4-nitro-1H-benzo[d]imidazol-1-yl)-methyl)-2-methylthiazole
-
4-((5,6-dichloro-2-methyl-4-nitro-1H-benzo[d]imidazol-1-yl)-methyl)benzaldehyde
-
4-((5,6-dichloro-2-methyl-4-nitro-1H-benzo[d]imidazol-1-yl)-methyl)benzoic acid
-
4-((5,6-dichloro-2-methyl-4-nitro-1H-benzo[d]imidazol-1-yl)-methyl)benzonitrile
-
4-((5,6-dichloro-2-methyl-4-nitro-1H-benzo[d]imidazol-1-yl)-methyl)phenyl acetate
-
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
-
5,6-dichloro-1-(2-(3,5-dimethyl-1H-pyrazol-4-yl)ethyl)-2-methyl-4-nitro-1H-benzo[d]imidazole
-
5,6-dichloro-1-(4-methoxybenzyl)-2-methyl-4-nitro-1H-benzo-[d]imidazole
-
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
-
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
-
5-methyl-3-(pyridin-2-yl)-6-[4-[(pyrrolidin-1-yl)methyl]phenyl][1,2]oxazolo[4,5-c]pyridin-4(5H)-one
-
5-methyl-3-(pyridin-3-yl)-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[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
-
5-methyl-6-[4-[(morpholin-4-yl)methyl]phenyl]-3-phenyl[1,2]oxazolo[4,5-c]pyridin-4(5H)-one
-
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
-
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
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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
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DISEASE
TITLE OF PUBLICATION
LINK TO PUBMED
Adenoma
Oxidative stress and 8-oxoguanine repair are enhanced in colon adenoma and carcinoma patients.
Breast Neoplasms
DCTPP1, an Oncogene Regulated by miR-378a-3p, Promotes Proliferation of Breast Cancer via DNA Repair Signaling Pathway.
Breast Neoplasms
Human dCTP pyrophosphatase 1 promotes breast cancer cell growth and stemness through the modulation on 5-methyl-dCTP metabolism and global hypomethylation.
Breast Neoplasms
Silencing DSCAM-AS1 suppresses the growth and invasion of ER-positive breast cancer cells by downregulating both DCTPP1 and QPRT.
Carcinoma
Discovery of the First Potent and Selective Inhibitors of Human dCTP Pyrophosphatase 1.
Chondrocalcinosis
Partial characterization of synovial fluid nucleotide pyrophosphohydrolase.
Chondrocalcinosis
Pyrophosphohydrolase activity and inorganic pyrophosphate content of cultured human skin fibroblasts. Elevated levels in some patients with calcium pyrophosphate dihydrate deposition disease.
Colorectal Neoplasms
Oxidative stress and 8-oxoguanine repair are enhanced in colon adenoma and carcinoma patients.
dctp diphosphatase deficiency
Erythrocyte ITP pyrophosphohydrolase deficiency in a psychiatric population.
dctp diphosphatase deficiency
Further evidence for a 'new' purine defect, inosine triphosphate (ITP) pyrophosphohydrolase deficiency.
dctp diphosphatase deficiency
Purine metabolism in normal and high-ITP human erythrocytes. Attempts to evaluate the ability to store the cells.
dctp diphosphatase deficiency
The First Structure of an Active Mammalian dCTPase and its Complexes With Substrate Analogs and Products.
Down Syndrome
Silencing DSCAM-AS1 suppresses the growth and invasion of ER-positive breast cancer cells by downregulating both DCTPP1 and QPRT.
Esophageal Neoplasms
dCTP pyrophosphohydrase exhibits nucleic accumulation in multiple carcinomas.
hypoxanthine phosphoribosyltransferase deficiency
Erythrocyte ITP pyrophosphohydrolase deficiency in a psychiatric population.
Infections
Partial exclusion of bacteriophage T2 by bacteriophage T4: induction of early enzymes by excluded T2.
Infections
Synthesis of functional bacteriophage T4-delayed early mRNA in the absence of protein synthesis.
Joint Diseases
Adenosine triphosphate pyrophosphohydrolase and neutral inorganic pyrophosphatase in pathologic joint fluids. Elevated pyrophosphohydrolase in calcium pyrophosphate dihydrate crystal deposition disease.
Leukemia
Discovery of the First Potent and Selective Inhibitors of Human dCTP Pyrophosphatase 1.
Neoplasms
Autophagy induced by overexpression of DCTPP1 promotes tumor progression and predicts poor clinical outcome in prostate cancer.
Neoplasms
DCTPP1 attenuates the sensitivity of human gastric cancer cells to 5-fluorouracil by up-regulating MDR1 expression epigenetically.
Neoplasms
DCTPP1, an Oncogene Regulated by miR-378a-3p, Promotes Proliferation of Breast Cancer via DNA Repair Signaling Pathway.
Neoplasms
Dimeric dUTPases, HisE, and MazG belong to a ne