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Literature summary for 2.1.1.63 extracted from

  • Nelson, M.E.; Loktionova, N.A.; Pegg, A.E.; Moschel, R.C.
    2-Amino-O4-benzylpteridine derivatives: potent inactivators of O6-alkylguanine-DNA alkyltransferase (2004), J. Med. Chem., 47, 3887-3891.
    View publication on PubMed

Application

Application Comment Organism
medicine O4-benzylfolic acid is 30times more active than O6-benzylguanine against the wild-type alkyltransferase, inactivation of P140K mutant alkyltransferase. Inhibitor shows promise as an agent for possible tumor-selective alkyltransferase inactivation superior toO6-benzylguanine as a chemotherapy adjuvant Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-amino-O4-benzyl-6,7-dimethylpteridine potent Homo sapiens
2-amino-O4-benzyl-6-formylpteridine potent Homo sapiens
2-amino-O4-benzyl-6-hydroxymethylpteridine potent Homo sapiens
2-amino-O4-benzylpteridine potent Homo sapiens
2-amino-O4-benzylpteridine-6-carboxylic acid potent Homo sapiens
O4-benzylfolic acid 30times more active than O6-benzylguanine against the wild-type alkyltransferase, inactivation of P140K mutant alkyltransferase. Inhibitor shows promise as an agent for possible tumor-selective alkyltransferase inactivation superior toO6-benzylguanine as a chemotherapy adjuvant Homo sapiens
O6-benzylguanine potent inhibitor of wild-type enzyme, no inactivation of mutant enzyme P140K Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
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