Literature summary for 3.2.2.1 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.

Application

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

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

Inhibitors	Comment	Organism
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

Organism	UniProt	Comment	Textmining
Trypanosoma brucei brucei	-	-	-
Trypanosoma vivax	-	-	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.
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

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 [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism
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	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