Literature summary for 3.6.1.5 extracted from

Lee, S.Y.; Luo, X.; Namasivayam, V.; Geiss, J.; Mirza, S.; Pelletier, J.; Stephan, H.; Sevigny, J.; Mueller, C.E.
Development of a selective and highly sensitive fluorescence assay for nucleoside triphosphate diphosphohydrolase1 (NTPDase1, CD39) (2018), Analyst, 143, 5417-5430 .

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Application

Application	Comment	Organism
medicine	activation of CD39 has potential for treating inflammatory diseases, while inhibition is suggested as a strategy for the immunotherapy of cancer	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
ARL67156	-	Homo sapiens
levamisole	-	Homo sapiens
PSB-POM141	i.e. [TiW11CoO40]8-; i.e. [TiW11CoO40]8-; i.e. [TiW11CoO40]8-; i.e. [TiW11CoO40]8-	Homo sapiens
Reactive blue 2	-	Homo sapiens
theophylline	-	Homo sapiens

KM Value [mM]

KM Value [mM]	KM Value Maximum [mM]	Substrate	Comment	Organism	Structure
0.0133	-	N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate	pH 6.5, temperature not specified in the publication, NTPDase3	Homo sapiens
0.0196	-	N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate	pH 6.5, temperature not specified in the publication, NTPDase1	Homo sapiens
0.0555	-	N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate	pH 6.5, temperature not specified in the publication, NTPDase2	Homo sapiens
0.105	-	N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate	pH 6.5, temperature not specified in the publication, NTPDase8	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	O75355	-	-
Homo sapiens	P49961	-	-
Homo sapiens	Q5MY95	-	-
Homo sapiens	Q9Y5L3	-	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate + H2O	developement of a selective and highly sensitive capillary electrophoresis (CE) assay using a fluorescent CD39 substrate, a fluorescein-labelled ATP, i.e. N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate that is converted to its AMP derivative (N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-phosphate). To accelerate the assays, a two-directional (forward and reverse) CE system is implemented using 96-well plates, which is suitable for the screening of compound libraries. Achievement of a large enhancement in sensitivity as compared to previous methods (e.g. malachite-green assay: 1000000fold, CE-UV assay: 500000fold, fluorescence polarization immunoassay: 12500fold). The assay is validated by performing inhibition assays with several standard CD39 inhibitors. N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate is preferably hydrolyzed by CD39 as compared to other ectonucleotidases	Homo sapiens	N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-phosphate + diphosphate	-	ir
N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate + H2O	i.e. PSB-170621A, developement of a selective and highly sensitive capillary electrophoresis (CE) assay using a fluorescent CD39 substrate, a fluorescein-labelled ATP, i.e. N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate that is converted to its AMP derivative (N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-phosphate). To accelerate the assays, a two-directional (forward and reverse) CE system is implemented using 96-well plates, which is suitable for the screening of compound libraries. Achievement of a large enhancement in sensitivity as compared to previous methods (e.g. malachite-green assay: 1000000fold, CE-UV assay: 500000fold, fluorescence polarization immunoassay: 12500fold). The assay is validated by performing inhibition assays with several standard CD39 inhibitors. N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate is preferably hydrolyzed by CD39 as compared to other ectonucleotidases	Homo sapiens	N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-phosphate + diphosphate	-	ir

Synonyms

Synonyms	Comment	Organism
CD39	-	Homo sapiens
ecto-nucleoside triphosphate diphosphohydrolase1	-	Homo sapiens
ecto-nucleoside triphosphate diphosphohydrolase2	-	Homo sapiens
ecto-nucleoside triphosphate diphosphohydrolase3	-	Homo sapiens
ecto-nucleoside triphosphate diphosphohydrolase8	-	Homo sapiens
NTPDase1	-	Homo sapiens
NTPDase2	-	Homo sapiens
NTPDase3	-	Homo sapiens
NTPDase8	-	Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s]	Turnover Number Maximum [1/s]	Substrate	Comment	Organism	Structure
0.0225	-	N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate	pH 6.5, temperature not specified in the publication, NTPDase3	Homo sapiens
0.0387	-	N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate	pH 6.5, temperature not specified in the publication, NTPDase8	Homo sapiens
0.0494	-	N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate	pH 6.5, temperature not specified in the publication, NTPDase2	Homo sapiens
0.119	-	N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate	pH 6.5, temperature not specified in the publication, NTPDase1	Homo sapiens

pH Optimum

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

General Information

General Information	Comment	Organism
physiological function	ecto-nucleoside triphosphate diphosphohydrolase1 (NTPDase1, CD39) is a major ectonucleotidase that hydrolyzes proinflammatory ATP via ADP to AMP, which is subsequently converted by ecto-5'-nucleotidase (CD73) to immunosuppressive adenosine	Homo sapiens

kcat/KM [mM/s]

kcat/KM Value [1/mMs^-1]	kcat/KM Value Maximum [1/mMs^-1]	Substrate	Comment	Organism	Structure
0.37	-	N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate	pH 6.5, temperature not specified in the publication, NTPDase8	Homo sapiens
0.89	-	N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate	pH 6.5, temperature not specified in the publication, NTPDase2	Homo sapiens
1.69	-	N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate	pH 6.5, temperature not specified in the publication, NTPDase3	Homo sapiens
6.07	-	N-[5-[4-carboxy-3-(3-oxo-9,9a-dihydro-3H-xanthen-9-yl)benzamido]pentyl]adenosine 5'-triphosphate	pH 6.5, temperature not specified in the publication, NTPDase1	Homo sapiens

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Release 2023.1 (January 2023)