Application | Comment | Organism |
---|---|---|
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 |
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 |
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 |
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 | Comment | Organism |
---|---|---|
additional information | RNAi knockdown of IAG-NH, by providing adenine, methylthioadenosine phosphorylase can circumvent IAG-NH function | Trypanosoma brucei brucei |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
immucillin A | - |
Trypanosoma brucei brucei | |
immucillin A | - |
Trypanosoma vivax | |
immucillin H | - |
Trypanosoma brucei brucei | |
immucillin H | - |
Trypanosoma vivax | |
melarsoprol | - |
Trypanosoma brucei brucei | |
additional information | N-arylmethyl-substituted iminoribitol derivatives as potential chemotherapeutic agents against trypanosomiasis, validation in an in vivo model of African trypanosomiasis | Trypanosoma vivax | |
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 | |
N-(9-deaza-adenin-9-yl)methyl-1,4-dideoxy-1,4-imino-D-ribitol | UAMC-00363 | Trypanosoma vivax | |
Pentamidine | - |
Trypanosoma brucei brucei | |
UAMC-00109 | - |
Trypanosoma brucei brucei | |
UAMC-00109 | - |
Trypanosoma vivax | |
UAMC-00115 | - |
Trypanosoma brucei brucei | |
UAMC-00115 | - |
Trypanosoma vivax | |
UAMC-00218 | - |
Trypanosoma brucei brucei | |
UAMC-00218 | - |
Trypanosoma vivax | |
UAMC-00311 | - |
Trypanosoma brucei brucei | |
UAMC-00311 | - |
Trypanosoma vivax | |
UAMC-00312 | - |
Trypanosoma brucei brucei | |
UAMC-00312 | - |
Trypanosoma vivax | |
UAMC-00346 | - |
Trypanosoma brucei brucei | |
UAMC-00346 | - |
Trypanosoma vivax | |
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 | |
UAMC-00363 | i.e. N-(9-deaza-adenin-9-yl)methyl-1,4-dideoxy-1,4-imino-D-ribitol | Trypanosoma vivax | |
UAMC-00375 | - |
Trypanosoma brucei brucei | |
UAMC-00375 | - |
Trypanosoma vivax |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Trypanosoma brucei brucei | - |
- |
- |
Trypanosoma vivax | - |
- |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
adenosine + H2O | - |
Trypanosoma vivax | D-ribose + adenine | - |
? | |
adenosine + H2O | substrate for inosine-adenosine-guanosine nucleoside hydrolase | Trypanosoma brucei brucei | D-ribose + adenine | - |
? | |
guanosine + H2O | - |
Trypanosoma brucei brucei | D-ribose + guanine | - |
? | |
guanosine + H2O | - |
Trypanosoma vivax | D-ribose + guanine | - |
? | |
inosine + H2O | - |
Trypanosoma brucei brucei | D-ribose + hypoxanthine | - |
? | |
inosine + H2O | - |
Trypanosoma vivax | D-ribose + hypoxanthine | - |
? | |
additional information | inosine-guanosine nucleoside hydrolase does not use adenosine as substrate | Trypanosoma brucei brucei | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
IAG-NH | - |
Trypanosoma brucei brucei |
IAG-NH | - |
Trypanosoma vivax |
IG-NH | - |
Trypanosoma brucei brucei |
inosine-adenosine-guanosine nucleoside hydrolase | - |
Trypanosoma brucei brucei |
inosine-adenosine-guanosine nucleoside hydrolase | - |
Trypanosoma vivax |
inosine-guanosine nucleoside hydrolase | - |
Trypanosoma brucei brucei |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0000009 | - |
immucillin A | inosine-adenosine-guanosine nucleoside hydrolase, pH and temperature not specified in the publication | Trypanosoma brucei brucei | |
0.0000041 | - |
UAMC-00363 | pH and temperature not specified in the publication | Trypanosoma vivax | |
0.0000044 | - |
UAMC-00109 | pH and temperature not specified in the publication | Trypanosoma vivax | |
0.0000044 | - |
immucillin A | inosine-guanosine nucleoside hydrolase, pH and temperature not specified in the publication | Trypanosoma brucei brucei | |
0.0000062 | - |
immucillin H | pH and temperature not specified in the publication | Trypanosoma vivax | |
0.0000062 | - |
immucillin A | pH and temperature not specified in the publication | Trypanosoma vivax | |
0.000009 | - |
immucillin H | inosine-guanosine nucleoside hydrolase, pH and temperature not specified in the publication | Trypanosoma brucei brucei | |
0.000011 | - |
UAMC-00115 | pH and temperature not specified in the publication | Trypanosoma vivax | |
0.000018 | - |
UAMC-00363 | inosine-adenosine-guanosine nucleoside hydrolase, pH and temperature not specified in the publication | Trypanosoma brucei brucei | |
0.000019 | - |
UAMC-00375 | pH and temperature not specified in the publication | Trypanosoma vivax | |
0.00002 | - |
UAMC-00312 | pH and temperature not specified in the publication | Trypanosoma vivax | |
0.000024 | - |
immucillin H | inosine-adenosine-guanosine nucleoside hydrolase, pH and temperature not specified in the publication | Trypanosoma brucei brucei | |
0.00003 | - |
UAMC-00109 | inosine-adenosine-guanosine nucleoside hydrolase, pH and temperature not specified in the publication | Trypanosoma brucei brucei | |
0.00004 | - |
UAMC-00311 | pH and temperature not specified in the publication | Trypanosoma vivax | |
0.00004 | - |
UAMC-00218 | pH and temperature not specified in the publication | Trypanosoma vivax | |
0.000056 | - |
UAMC-00375 | inosine-adenosine-guanosine nucleoside hydrolase, pH and temperature not specified in the publication | Trypanosoma brucei brucei | |
0.000058 | - |
UAMC-00346 | pH and temperature not specified in the publication | Trypanosoma vivax | |
0.00019 | - |
UAMC-00312 | inosine-adenosine-guanosine nucleoside hydrolase, pH and temperature not specified in the publication | Trypanosoma brucei brucei | |
0.000446 | - |
UAMC-00115 | inosine-adenosine-guanosine nucleoside hydrolase, pH and temperature not specified in the publication | Trypanosoma brucei brucei | |
0.00056 | - |
UAMC-00311 | inosine-adenosine-guanosine nucleoside hydrolase, pH and temperature not specified in the publication | Trypanosoma brucei brucei | |
0.011 | - |
UAMC-00115 | inosine-guanosine nucleoside hydrolase, pH and temperature not specified in the publication | Trypanosoma brucei brucei | |
0.014 | - |
UAMC-00311 | inosine-guanosine nucleoside hydrolase, pH and temperature not specified in the publication | Trypanosoma brucei brucei | |
0.031 | - |
UAMC-00375 | inosine-guanosine nucleoside hydrolase, pH and temperature not specified in the publication | Trypanosoma brucei brucei | |
0.032 | - |
UAMC-00363 | inosine-guanosine nucleoside hydrolase, pH and temperature not specified in the publication | Trypanosoma brucei brucei | |
0.12 | - |
UAMC-00312 | inosine-guanosine nucleoside hydrolase, pH and temperature not specified in the publication | Trypanosoma brucei brucei | |
0.138 | - |
UAMC-00109 | inosine-guanosine nucleoside hydrolase, pH and temperature not specified in the publication | Trypanosoma brucei brucei | |
0.59 | - |
N-(9-deaza-adenin-9-yl)methyl-1,4-dideoxy-1,4-imino-D-ribitol | - |
Trypanosoma brucei brucei |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00049 | - |
pH and temperature not specified in the publication | Trypanosoma brucei brucei | UAMC-00363 | |
0.034 | - |
pH and temperature not specified in the publication | Trypanosoma brucei brucei | UAMC-00312 |