Literature summary for 2.4.2.1 extracted from

Rinaldo-Matthis, A.; Wing, C.; Ghanem, M.; Deng, H.; Wu, P.; Gupta, A.; Tyler, P.C.; Evans, G.B.; Furneaux, R.H.; Almo, S.C.; Wang, C.C.; Schramm, V.L.
Inhibition and structure of Trichomonas vaginalis purine nucleoside phosphorylase with picomolar transition state analogues (2007), Biochemistry, 46, 659-668.

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Crystallization (Commentary)

Crystallization (Comment)	Organism
crystal structures of the TvPNP/immucillin-A/PO4 and TvPNP/4'-deaza-1'-aza-2'-deoxy-1'-(9-methylene)-immucillin-A/PO4 ternary complexes	Trichomonas vaginalis
crystal structures of the TvPNP/immucillin-A/PO4 and TvPNP/deaza-1'-aza-2'-deoxy-1'-(9-methylene)-immucillin-A /PO4 ternary complexes.	Trichomonas vaginalis

Inhibitors

Inhibitors	Comment	Organism	Structure
4'-deaza-1'-aza-2'-deoxy-1'-(9-methylene)-immucillin-A	weak binding inhibitor	Homo sapiens
4'-deaza-1'-aza-2'-deoxy-1'-(9-methylene)-immucillin-A	weak binding inhibitor	Plasmodium falciparum
4'-deaza-1'-aza-2'-deoxy-1'-(9-methylene)-immucillin-A	dissociation constant of 30 pM, an inhibitor release half-time of 64 min. Tight binding with 4'-deaza-1'-aza-2'-deoxy-1'-(9-methylene)-immucillin-A is in part due to a 2.7 A ionic interaction between a PO4 oxygen and the N1' cation of the hydroxypyrrolidine. The interaction of the inhibitor with TvPNP is the tightest-binding enzymatic interaction known for an immucillin analogue of adenosine; tight binding inhibitor	Trichomonas vaginalis
4'-deaza-1'-aza-2'-deoxy-1'-(9-methylene)-immucillin-G	-	Homo sapiens
4'-deaza-1'-aza-2'-deoxy-1'-(9-methylene)-immucillin-G	-	Trichomonas vaginalis
4'-deaza-1'-aza-2'-deoxy-1'-(9-methylene)-immucillin-H	-	Trichomonas vaginalis
immucillin-A	weak binding inhibitor	Homo sapiens
immucillin-A	weak binding inhibitor	Plasmodium falciparum
immucillin-A	slow-onset tight binding inhibition, inhibitor release half-time of 17.2 min; slow-onset tightbinding inhibition with TvPNP, to give an equilibrium dissociation constant of 87 pM and an inhibitor release half-time of 17.2 min	Trichomonas vaginalis
immucillin-G	dissociation constant of 42 pM	Homo sapiens
immucillin-G	dissociation constant of 900 pM	Plasmodium falciparum
immucillin-G	-	Trichomonas vaginalis
immucillin-H	dissociation constant: 23 pM	Bos taurus
immucillin-H	dissociation constant: 56 pM	Homo sapiens
immucillin-H	-	Trichomonas vaginalis

KM Value [mM]

KM Value [mM]	KM Value Maximum [mM]	Substrate	Comment	Organism	Structure
0.0061	-	adenosine	-	Trichomonas vaginalis
0.0061	-	adenosine	25°C, pH 7.4	Trichomonas vaginalis
0.025	-	Inosine	-	Trichomonas vaginalis
0.025	-	Inosine	25°C, pH 7.4	Trichomonas vaginalis
0.06	-	guanosine	-	Trichomonas vaginalis
0.06	-	guanosine	25°C, pH 7.4	Trichomonas vaginalis
0.09	-	p-nitrophenyl beta-D-ribofuranoside	-	Trichomonas vaginalis
0.09	-	p-nitrophenyl beta-D-ribofuranoside	25°C, pH 7.4	Trichomonas vaginalis

Organism

Organism	UniProt	Comment	Textmining
Bos taurus	P55859	-	-
Homo sapiens	P00491	-	-
Plasmodium falciparum	Q8T9Z7	-	-
Trichomonas vaginalis	-	-	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
adenosine + phosphate	-	Trichomonas vaginalis	adenine + alpha-D-ribose 1-phosphate	-	?
guanosine + phosphate	-	Trichomonas vaginalis	guanine + alpha-D-ribose 1-phosphate	-	?
inosine + phosphate	-	Trichomonas vaginalis	hypoxanthine + alpha-D-ribose 1-phosphate	-	?
inosine + phosphate	-	Homo sapiens	hypoxanthine + alpha-D-ribose 1-phosphate	-	?
inosine + phosphate	-	Bos taurus	hypoxanthine + alpha-D-ribose 1-phosphate	-	?
p-nitrophenyl beta-D-ribofuranoside + phosphate	-	Trichomonas vaginalis	?	-	?

Synonyms

Synonyms	Comment	Organism
HsPNP	-	Homo sapiens
TvPNP	-	Trichomonas vaginalis

Turnover Number [1/s]

Turnover Number Minimum [1/s]	Turnover Number Maximum [1/s]	Substrate	Comment	Organism	Structure
0.001	-	p-nitrophenyl beta-D-ribofuranoside	25°C, pH 7.4	Trichomonas vaginalis
1	-	p-nitrophenyl beta-D-ribofuranoside	-	Trichomonas vaginalis
1.1	-	guanosine	-	Trichomonas vaginalis
1.1	-	guanosine	25°C, pH 7.4	Trichomonas vaginalis
1.7	-	adenosine	-	Trichomonas vaginalis
1.7	-	adenosine	25°C, pH 7.4	Trichomonas vaginalis
1.8	-	Inosine	-	Trichomonas vaginalis
1.8	-	Inosine	25°C, pH 7.4	Trichomonas vaginalis

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
0.000001	-	immucillin-A	-	Trichomonas vaginalis
0.000001	-	immucillin-A	25°C, pH 7.4	Trichomonas vaginalis
0.0000015	-	4'-deaza-1'-aza-2'-deoxy-1'-(9-methylene)-immucillin-A	-	Trichomonas vaginalis
0.0000015	-	4'-deaza-1'-aza-2'-deoxy-1'-(9-methylene)-immucillin-A	25°C, pH 7.4	Trichomonas vaginalis
0.0000038	-	4'-deaza-1'-aza-2'-deoxy-1'-(9-methylene)-immucillin-H	-	Trichomonas vaginalis
0.0000038	-	4'-deaza-1'-aza-2'-deoxy-1'-(9-methylene)-immucillin-H	25°C, pH 7.4	Trichomonas vaginalis
0.000012	-	immucillin-H	-	Trichomonas vaginalis
0.000012	-	immucillin-H	25°C, pH 7.4	Trichomonas vaginalis
0.000016	-	immucillin-G	-	Trichomonas vaginalis
0.000016	-	immucillin-G	25°C, pH 7.4	Trichomonas vaginalis
0.000018	-	4'-deaza-1'-aza-2'-deoxy-1'-(9-methylene)-immucillin-G	-	Trichomonas vaginalis
0.000018	-	4'-deaza-1'-aza-2'-deoxy-1'-(9-methylene)-immucillin-H	25°C, pH 7.4	Trichomonas vaginalis

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Release 2023.1 (January 2023)