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Literature summary 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.
    View publication on PubMedView publication on EuropePMC

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
2.4.2.1 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
2.4.2.1 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

EC Number Inhibitors Comment Organism Structure
2.4.2.1 4'-deaza-1'-aza-2'-deoxy-1'-(9-methylene)-immucillin-A weak binding inhibitor Homo sapiens
2.4.2.1 4'-deaza-1'-aza-2'-deoxy-1'-(9-methylene)-immucillin-A weak binding inhibitor Plasmodium falciparum
2.4.2.1 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
2.4.2.1 4'-deaza-1'-aza-2'-deoxy-1'-(9-methylene)-immucillin-G
-
 Homo sapiens
2.4.2.1 4'-deaza-1'-aza-2'-deoxy-1'-(9-methylene)-immucillin-G
-
 Trichomonas vaginalis
2.4.2.1 4'-deaza-1'-aza-2'-deoxy-1'-(9-methylene)-immucillin-H
-
 Trichomonas vaginalis
2.4.2.1 immucillin-A weak binding inhibitor Homo sapiens
2.4.2.1 immucillin-A weak binding inhibitor Plasmodium falciparum
2.4.2.1 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
2.4.2.1 immucillin-G dissociation constant of 42 pM Homo sapiens
2.4.2.1 immucillin-G dissociation constant of 900 pM Plasmodium falciparum
2.4.2.1 immucillin-G
-
 Trichomonas vaginalis
2.4.2.1 immucillin-H dissociation constant: 23 pM Bos taurus
2.4.2.1 immucillin-H dissociation constant: 56 pM Homo sapiens
2.4.2.1 immucillin-H
-
 Trichomonas vaginalis

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.4.2.1 0.0061
-
 adenosine
-
 Trichomonas vaginalis
2.4.2.1 0.0061
-
 adenosine 25°C, pH 7.4 Trichomonas vaginalis
2.4.2.1 0.025
-
 Inosine
-
 Trichomonas vaginalis
2.4.2.1 0.025
-
 Inosine 25°C, pH 7.4 Trichomonas vaginalis
2.4.2.1 0.06
-
 guanosine
-
 Trichomonas vaginalis
2.4.2.1 0.06
-
 guanosine 25°C, pH 7.4 Trichomonas vaginalis
2.4.2.1 0.09
-
 p-nitrophenyl beta-D-ribofuranoside
-
 Trichomonas vaginalis
2.4.2.1 0.09
-
 p-nitrophenyl beta-D-ribofuranoside 25°C, pH 7.4 Trichomonas vaginalis

Organism

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

Substrates and Products (Substrate)

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

Synonyms

EC Number Synonyms Comment Organism
2.4.2.1 HsPNP
-
 Homo sapiens
2.4.2.1 TvPNP
-
 Trichomonas vaginalis

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
2.4.2.1 0.001
-
 p-nitrophenyl beta-D-ribofuranoside 25°C, pH 7.4 Trichomonas vaginalis
2.4.2.1 1
-
 p-nitrophenyl beta-D-ribofuranoside
-
 Trichomonas vaginalis
2.4.2.1 1.1
-
 guanosine
-
 Trichomonas vaginalis
2.4.2.1 1.1
-
 guanosine 25°C, pH 7.4 Trichomonas vaginalis
2.4.2.1 1.7
-
 adenosine
-
 Trichomonas vaginalis
2.4.2.1 1.7
-
 adenosine 25°C, pH 7.4 Trichomonas vaginalis
2.4.2.1 1.8
-
 Inosine
-
 Trichomonas vaginalis
2.4.2.1 1.8
-
 Inosine 25°C, pH 7.4 Trichomonas vaginalis

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.4.2.1 0.000001
-
 immucillin-A
-
 Trichomonas vaginalis
2.4.2.1 0.000001
-
 immucillin-A 25°C, pH 7.4 Trichomonas vaginalis
2.4.2.1 0.0000015
-
 4'-deaza-1'-aza-2'-deoxy-1'-(9-methylene)-immucillin-A
-
 Trichomonas vaginalis
2.4.2.1 0.0000015
-
 4'-deaza-1'-aza-2'-deoxy-1'-(9-methylene)-immucillin-A 25°C, pH 7.4 Trichomonas vaginalis
2.4.2.1 0.0000038
-
 4'-deaza-1'-aza-2'-deoxy-1'-(9-methylene)-immucillin-H
-
 Trichomonas vaginalis
2.4.2.1 0.0000038
-
 4'-deaza-1'-aza-2'-deoxy-1'-(9-methylene)-immucillin-H 25°C, pH 7.4 Trichomonas vaginalis
2.4.2.1 0.000012
-
 immucillin-H
-
 Trichomonas vaginalis
2.4.2.1 0.000012
-
 immucillin-H 25°C, pH 7.4 Trichomonas vaginalis
2.4.2.1 0.000016
-
 immucillin-G
-
 Trichomonas vaginalis
2.4.2.1 0.000016
-
 immucillin-G 25°C, pH 7.4 Trichomonas vaginalis
2.4.2.1 0.000018
-
 4'-deaza-1'-aza-2'-deoxy-1'-(9-methylene)-immucillin-G
-
 Trichomonas vaginalis
2.4.2.1 0.000018
-
 4'-deaza-1'-aza-2'-deoxy-1'-(9-methylene)-immucillin-H 25°C, pH 7.4 Trichomonas vaginalis