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Literature summary for 2.1.2.3 extracted from

  • Capps, K.J.; Humiston, J.; Dominique, R.; Hwang, I.; Boger, D.L.
    Discovery of AICAR Tfase inhibitors that disrupt requisite enzyme dimerization (2005), Bioorg. Med. Chem. Lett., 15, 2840-2844.
    View publication on PubMed

Application

Application Comment Organism
medicine potential target for antineoplastic chemotherapy Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
Cappsin 1 non-competitive, inhibition of activity by preventing the formation of dimers Homo sapiens
Cappsin 2 some derivatives of Cappepsin are also inhibitory, inhibition of activity by preventing the formation of dimers Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazole-4-carboxamide Homo sapiens penultimate step of the purine de novo synthesis pathway tetrahydrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazole-4-carboxamide
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazole-4-carboxamide
-
Homo sapiens tetrahydrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazole-4-carboxamide
-
?
10-formyltetrahydrofolate + 5'-phosphoribosyl-5-amino-imidazole-4-carboxamide penultimate step of the purine de novo synthesis pathway Homo sapiens tetrahydrofolic acid + 5'-phosphoribosyl-5-formamido-4-imidazole-4-carboxamide
-
?

Subunits

Subunits Comment Organism
dimer transformylase activity is formed upon dimerization of the enzyme Homo sapiens

Synonyms

Synonyms Comment Organism
AICAR transformylase/inosine monophosphate cyclohydrolase bifunctional enzyme catalyzing the last two steps of the purine de novo synthesis pathway Homo sapiens

Cofactor

Cofactor Comment Organism Structure
10-formyltetrahydrofolate
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.003
-
Cappsin 1
-
Homo sapiens