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Literature summary for 3.6.1.9 extracted from

  • Eliahu, S.; Lecka, J.; Reiser, G.; Haas, M.; Bigonnesse, F.; Levesque, S.A.; Pelletier, J.; Sevigny, J.; Fischer, B.
    Diadenosine 5,5-(boranated)polyphosphonate analogues as selective nucleotide pyrophosphatase/phosphodiesterase inhibitors (2010), J. Med. Chem., 53, 8485-8497.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression in COS-7 cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
di-2'-deoxyadenosine 5',5''-P1,P5,alpha,beta-methylene-delta,epsilon-methylene-pentaphosphate-gamma-borano
-
Homo sapiens
di-2'-deoxyadenosine 5',5''-P1,P5,alpha,beta-methylene-gamma,delta-methylene-tetraphosphate
-
Homo sapiens
diadenosine 5',5''-P1,P5,alpha,beta-methylene-delta,epsilon-methylene-pentaphosphate-gamma-borano
-
Homo sapiens
additional information diadenosine 5,5-(boranated)polyphosphonate analogues as selective nucleotide pyrophosphatase/phosphodiesterase inhibitors, synthesis, overview; diadenosine 5,5-(boranated)polyphosphonate analogues as selective nucleotide pyrophosphatase/phosphodiesterase inhibitors, synthesis, overview; diadenosine 5,5-(boranated)polyphosphonate analogues as selective nucleotide pyrophosphatase/phosphodiesterase inhibitors, synthesis, overview Homo sapiens
P1,P4-bis(5'-adenosyl)-alpha,beta-gamma,delta-bismethylene-tetraphosphate
-
Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
cell surface
-
Homo sapiens 9986
-

Metals/Ions

Metals/Ions Comment Organism Structure
Ca2+ required Homo sapiens
Mg2+ required Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
4-nitrophenyl-5'-TMP + H2O Homo sapiens hydrolysis of pnp-TMP at the cell surface of both osteocarcinoma and colon cancer cells 4-nitrophenol + 5'-TMP
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Homo sapiens O14638 NPP3
-
Homo sapiens P22413 NPP1
-

Source Tissue

Source Tissue Comment Organism Textmining
bone cancer cell
-
Homo sapiens
-
colonic cancer cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4-nitrophenyl-5'-TMP + H2O hydrolysis of pnp-TMP at the cell surface of both osteocarcinoma and colon cancer cells Homo sapiens 4-nitrophenol + 5'-TMP
-
?
4-nitrophenyl-5'-TMP + H2O a specific NPP substrate Homo sapiens 4-nitrophenol + 5'-TMP
-
?
ATP + 2 H2O
-
Homo sapiens AMP + 2 phosphate
-
?
di-2'-deoxyadenosine 5',5''-P1,P5,alpha,beta-methylene-delta,epsilon-methylene-pentaphosphate-gamma-borano + 2 H2O low hydrolysis activity with the inhibitor as substrate Homo sapiens ?
-
?
di-2'-deoxyadenosine 5',5''-P1,P5,alpha,beta-methylene-gamma,delta-methylene-tetraphosphate + 2 H2O low hydrolysis activity with the inhibitor as substrate Homo sapiens ?
-
?
diadenosine 5',5''-P1,P5,alpha,beta-methylene-delta,epsilon-methylene-pentaphosphate-gamma-borano + 2 H2O low hydrolysis activity with the inhibitor as substrate Homo sapiens ?
-
?
P1,P4-bis(5'-adenosyl)-alpha,beta-gamma,delta-bismethylene-tetraphosphate + 2 H2O low hydrolysis activity with the inhibitor as substrate Homo sapiens ?
-
?
P1,P5-bis(5'-adenosyl)pentaphosphate + 2 H2O
-
Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
NPP
-
Homo sapiens
NPP1
-
Homo sapiens
NPP2
-
Homo sapiens
NPP3
-
Homo sapiens
nucleotide pyrophosphatase/phosphodiesterase
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.3
-
assay at Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.009
-
di-2'-deoxyadenosine 5',5''-P1,P5,alpha,beta-methylene-delta,epsilon-methylene-pentaphosphate-gamma-borano with NPP1, pH 7.3, 37°C Homo sapiens
0.013
-
P1,P4-bis(5'-adenosyl)-alpha,beta-gamma,delta-bismethylene-tetraphosphate with NPP1, pH 7.3, 37°C Homo sapiens
0.02
-
diadenosine 5',5''-P1,P5,alpha,beta-methylene-delta,epsilon-methylene-pentaphosphate-gamma-borano with NPP1, pH 7.3, 37°C Homo sapiens
0.051
-
di-2'-deoxyadenosine 5',5''-P1,P5,alpha,beta-methylene-gamma,delta-methylene-tetraphosphate with NPP1, pH 7.3, 37°C Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.013
-
with NPP1, pH 7.3, 37°C Homo sapiens di-2'-deoxyadenosine 5',5''-P1,P5,alpha,beta-methylene-delta,epsilon-methylene-pentaphosphate-gamma-borano
0.033
-
with NPP1, pH 7.3, 37°C Homo sapiens P1,P4-bis(5'-adenosyl)-alpha,beta-gamma,delta-bismethylene-tetraphosphate
0.05
-
with NPP1, pH 7.3, 37°C Homo sapiens di-2'-deoxyadenosine 5',5''-P1,P5,alpha,beta-methylene-gamma,delta-methylene-tetraphosphate
0.063
-
with NPP1, pH 7.3, 37°C Homo sapiens diadenosine 5',5''-P1,P5,alpha,beta-methylene-delta,epsilon-methylene-pentaphosphate-gamma-borano

General Information

General Information Comment Organism
physiological function nucleotide pyrophosphatase/phosphodiesterases hydrolyze extracellular nucleotides and dinucleotides and thus control purinergic signaling. EnhancedNPP activity is implicated in health disorders such as osteoarthritis and cancer Homo sapiens