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Literature summary for 2.4.2.1 extracted from

  • Rejman, D.; Panova, N.; Klener, P.; Maswabi, B.; Pohl, R.; Rosenberg, I.
    N-phosphonocarbonylpyrrolidine derivatives of guanine: a new class of bi-substrate inhibitors of human purine nucleoside phosphorylase (2012), J. Med. Chem., 55, 1612-1621.
    View publication on PubMed

Application

Application Comment Organism
medicine for inhibitor (S)-3-(guanin-9-yl)pyrrolidin-N-ylcarbonylphosphonic acid, Ki values widely vary from 16 to 100 nM for enzyme from cancer cell lines. For inhibitor (3S,4R)-4-(guanin-9-yl)-3-hydroxypyrrolidin-1-N-ylcarbonylphosphonic acid, Ki values are around 10 to 24 nM for enzyme from cancer cell lines Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
-
Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(3S,4R)-4-(guanin-9-yl)-3-hydroxypyrrolidin-1-N-ylcarbonylphosphonic acid competitive. For enzyme from cancer cell lines, Ki values are around 10 to 24 nM Homo sapiens
(S)-3-(guanin-9-yl)pyrrolidin-N-ylcarbonylphosphonic acid competitive. For enzyme from cancer cell lines, Ki values widely vary from 16 to 100 nM Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.012
-
7-N-methyl-6-thiopurine riboside enzyme purified from mantle cell lymphoma, pH 7.5, temperature not specified in the publication Homo sapiens
0.04
-
7-N-methyl-6-thiopurine riboside enzyme purified from diffuse large B-cell lymphoma progressed from follicular lymphoma, pH 7.5, temperature not specified in the publication Homo sapiens
0.05
-
phosphate enzyme purified from peripheral blood mononuclear cell, pH 7.5, temperature not specified in the publication Homo sapiens
0.06
-
7-N-methyl-6-thiopurine riboside recombinant enzyme, pH 7.5, temperature not specified in the publication Homo sapiens
0.08
-
7-N-methyl-6-thiopurine riboside enzyme purified from peripheral blood mononuclear cell, pH 7.5, temperature not specified in the publication Homo sapiens
0.1
-
phosphate recombinant enzyme, pH 7.5, temperature not specified in the publication Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
partial Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
PBMC cell peripheral blood mononuclear cell Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
7-N-methyl-6-thiopurine riboside + phosphate
-
Homo sapiens ?
-
?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.01
-
(3S,4R)-4-(guanin-9-yl)-3-hydroxypyrrolidin-1-N-ylcarbonylphosphonic acid recombinant enzyme, pH 7.5, temperature not specified in the publication Homo sapiens
0.02
-
(S)-3-(guanin-9-yl)pyrrolidin-N-ylcarbonylphosphonic acid recombinant enzyme, pH 7.5, temperature not specified in the publication Homo sapiens