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Literature summary extracted from

  • Berg, M.; Kohl, L.; Van der Veken, P.; Joossens, J.; Al-Salabi, M.I.; Castagna, V.; Giannese, F.; Cos, P.; Versees, W.; Steyaert, J.; Grellier, P.; Haemers, A.; Degano, M.; Maes, L.; de Koning, H.P.; Augustyns, K.
    Evaluation of nucleoside hydrolase inhibitors for treatment of African trypanosomiasis (2010), Antimicrob. Agents Chemother., 54, 1900-1908.
    View publication on PubMedView publication on EuropePMC

Application

EC Number Application Comment Organism
3.2.2.1 drug development enzyme inhibitors N-arylmethyl-substituted iminoribitol derivatives as potential chemotherapeutic agents against trypanosomiasis, validation in an in vivo model of African trypanosomiasis Trypanosoma brucei brucei
3.2.2.1 drug development enzyme inhibitors N-arylmethyl-substituted iminoribitol derivatives as potential chemotherapeutic agents against trypanosomiasis, validation in an in vivo model of African trypanosomiasis Trypanosoma vivax
3.2.2.1 pharmacology enzyme inhibitors N-arylmethyl-substituted iminoribitol derivatives as potential chemotherapeutic agents against trypanosomiasis, validation in an in vivo model of African trypanosomiasis Trypanosoma brucei brucei
3.2.2.1 pharmacology enzyme inhibitors N-arylmethyl-substituted iminoribitol derivatives as potential chemotherapeutic agents against trypanosomiasis, validation in an in vivo model of African trypanosomiasis Trypanosoma vivax

Protein Variants

EC Number Protein Variants Comment Organism
3.2.2.1 additional information RNAi knockdown of IAG-NH, by providing adenine, methylthioadenosine phosphorylase can circumvent IAG-NH function Trypanosoma brucei brucei

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.2.2.1 immucillin A
-
 Trypanosoma brucei brucei
3.2.2.1 immucillin A
-
 Trypanosoma vivax
3.2.2.1 immucillin H
-
 Trypanosoma brucei brucei
3.2.2.1 immucillin H
-
 Trypanosoma vivax
3.2.2.1 melarsoprol
-
 Trypanosoma brucei brucei
3.2.2.1 additional information N-arylmethyl-substituted iminoribitol derivatives as potential chemotherapeutic agents against trypanosomiasis, validation in an in vivo model of African trypanosomiasis Trypanosoma vivax
3.2.2.1 N-(9-deaza-adenin-9-yl)methyl-1,4-dideoxy-1,4-imino-D-ribitol UAMC-00363, is the only N-arylmethyl-substituted iminoribitol derivative active as chemotherapeutic agent against trypanosomiasis, validation in an in vivo model of African trypanosomiasis. No cross-resistance to the diamidine or the melaminophenyl arsenical classes of trypanocides Trypanosoma brucei brucei
3.2.2.1 N-(9-deaza-adenin-9-yl)methyl-1,4-dideoxy-1,4-imino-D-ribitol UAMC-00363 Trypanosoma vivax
3.2.2.1 Pentamidine
-
 Trypanosoma brucei brucei
3.2.2.1 UAMC-00109
-
 Trypanosoma brucei brucei
3.2.2.1 UAMC-00109
-
 Trypanosoma vivax
3.2.2.1 UAMC-00115
-
 Trypanosoma brucei brucei
3.2.2.1 UAMC-00115
-
 Trypanosoma vivax
3.2.2.1 UAMC-00218
-
 Trypanosoma brucei brucei
3.2.2.1 UAMC-00218
-
 Trypanosoma vivax
3.2.2.1 UAMC-00311
-
 Trypanosoma brucei brucei
3.2.2.1 UAMC-00311
-
 Trypanosoma vivax
3.2.2.1 UAMC-00312
-
 Trypanosoma brucei brucei
3.2.2.1 UAMC-00312
-
 Trypanosoma vivax
3.2.2.1 UAMC-00346
-
 Trypanosoma brucei brucei
3.2.2.1 UAMC-00346
-
 Trypanosoma vivax
3.2.2.1 UAMC-00363 i.e. N-(9-deaza-adenin-9-yl)methyl-1,4-dideoxy-1,4-imino-D-ribitol, significant inhibition of inosine-adenosine-guanosine nucleoside hydrolase and inosine-guanosine nucleoside hydrolase Trypanosoma brucei brucei
3.2.2.1 UAMC-00363 i.e. N-(9-deaza-adenin-9-yl)methyl-1,4-dideoxy-1,4-imino-D-ribitol Trypanosoma vivax
3.2.2.1 UAMC-00375
-
 Trypanosoma brucei brucei
3.2.2.1 UAMC-00375
-
 Trypanosoma vivax

Organism

EC Number Organism UniProt Comment Textmining
3.2.2.1 Trypanosoma brucei brucei
-
-
-
3.2.2.1 Trypanosoma vivax
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.2.2.1 adenosine + H2O
-
 Trypanosoma vivax D-ribose + adenine
-
 ?
3.2.2.1 adenosine + H2O substrate for inosine-adenosine-guanosine nucleoside hydrolase Trypanosoma brucei brucei D-ribose + adenine
-
 ?
3.2.2.1 guanosine + H2O
-
 Trypanosoma brucei brucei D-ribose + guanine
-
 ?
3.2.2.1 guanosine + H2O
-
 Trypanosoma vivax D-ribose + guanine
-
 ?
3.2.2.1 inosine + H2O
-
 Trypanosoma brucei brucei D-ribose + hypoxanthine
-
 ?
3.2.2.1 inosine + H2O
-
 Trypanosoma vivax D-ribose + hypoxanthine
-
 ?
3.2.2.1 additional information inosine-guanosine nucleoside hydrolase does not use adenosine as substrate Trypanosoma brucei brucei ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.2.2.1 IAG-NH
-
 Trypanosoma brucei brucei
3.2.2.1 IAG-NH
-
 Trypanosoma vivax
3.2.2.1 IG-NH
-
 Trypanosoma brucei brucei
3.2.2.1 inosine-adenosine-guanosine nucleoside hydrolase
-
 Trypanosoma brucei brucei
3.2.2.1 inosine-adenosine-guanosine nucleoside hydrolase
-
 Trypanosoma vivax
3.2.2.1 inosine-guanosine nucleoside hydrolase
-
 Trypanosoma brucei brucei

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.2.2.1 0.0000009
-
 immucillin A inosine-adenosine-guanosine nucleoside hydrolase, pH and temperature not specified in the publication Trypanosoma brucei brucei
3.2.2.1 0.0000041
-
 UAMC-00363 pH and temperature not specified in the publication Trypanosoma vivax
3.2.2.1 0.0000044
-
 UAMC-00109 pH and temperature not specified in the publication Trypanosoma vivax
3.2.2.1 0.0000044
-
 immucillin A inosine-guanosine nucleoside hydrolase, pH and temperature not specified in the publication Trypanosoma brucei brucei
3.2.2.1 0.0000062
-
 immucillin H pH and temperature not specified in the publication Trypanosoma vivax
3.2.2.1 0.0000062
-
 immucillin A pH and temperature not specified in the publication Trypanosoma vivax
3.2.2.1 0.000009
-
 immucillin H inosine-guanosine nucleoside hydrolase, pH and temperature not specified in the publication Trypanosoma brucei brucei
3.2.2.1 0.000011
-
 UAMC-00115 pH and temperature not specified in the publication Trypanosoma vivax
3.2.2.1 0.000018
-
 UAMC-00363 inosine-adenosine-guanosine nucleoside hydrolase, pH and temperature not specified in the publication Trypanosoma brucei brucei
3.2.2.1 0.000019
-
 UAMC-00375 pH and temperature not specified in the publication Trypanosoma vivax
3.2.2.1 0.00002
-
 UAMC-00312 pH and temperature not specified in the publication Trypanosoma vivax
3.2.2.1 0.000024
-
 immucillin H inosine-adenosine-guanosine nucleoside hydrolase, pH and temperature not specified in the publication Trypanosoma brucei brucei
3.2.2.1 0.00003
-
 UAMC-00109 inosine-adenosine-guanosine nucleoside hydrolase, pH and temperature not specified in the publication Trypanosoma brucei brucei
3.2.2.1 0.00004
-
 UAMC-00311 pH and temperature not specified in the publication Trypanosoma vivax
3.2.2.1 0.00004
-
 UAMC-00218 pH and temperature not specified in the publication Trypanosoma vivax
3.2.2.1 0.000056
-
 UAMC-00375 inosine-adenosine-guanosine nucleoside hydrolase, pH and temperature not specified in the publication Trypanosoma brucei brucei
3.2.2.1 0.000058
-
 UAMC-00346 pH and temperature not specified in the publication Trypanosoma vivax
3.2.2.1 0.00019
-
 UAMC-00312 inosine-adenosine-guanosine nucleoside hydrolase, pH and temperature not specified in the publication Trypanosoma brucei brucei
3.2.2.1 0.000446
-
 UAMC-00115 inosine-adenosine-guanosine nucleoside hydrolase, pH and temperature not specified in the publication Trypanosoma brucei brucei
3.2.2.1 0.00056
-
 UAMC-00311 inosine-adenosine-guanosine nucleoside hydrolase, pH and temperature not specified in the publication Trypanosoma brucei brucei
3.2.2.1 0.011
-
 UAMC-00115 inosine-guanosine nucleoside hydrolase, pH and temperature not specified in the publication Trypanosoma brucei brucei
3.2.2.1 0.014
-
 UAMC-00311 inosine-guanosine nucleoside hydrolase, pH and temperature not specified in the publication Trypanosoma brucei brucei
3.2.2.1 0.031
-
 UAMC-00375 inosine-guanosine nucleoside hydrolase, pH and temperature not specified in the publication Trypanosoma brucei brucei
3.2.2.1 0.032
-
 UAMC-00363 inosine-guanosine nucleoside hydrolase, pH and temperature not specified in the publication Trypanosoma brucei brucei
3.2.2.1 0.12
-
 UAMC-00312 inosine-guanosine nucleoside hydrolase, pH and temperature not specified in the publication Trypanosoma brucei brucei
3.2.2.1 0.138
-
 UAMC-00109 inosine-guanosine nucleoside hydrolase, pH and temperature not specified in the publication Trypanosoma brucei brucei
3.2.2.1 0.59
-
 N-(9-deaza-adenin-9-yl)methyl-1,4-dideoxy-1,4-imino-D-ribitol
-
 Trypanosoma brucei brucei

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.2.2.1 0.00049
-
 pH and temperature not specified in the publication Trypanosoma brucei brucei UAMC-00363
3.2.2.1 0.034
-
 pH and temperature not specified in the publication Trypanosoma brucei brucei UAMC-00312