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Literature summary extracted from

  • Pagani, E.; Falcinelli, S.; Pepponi, R.; Turriziani, M.; Caporaso, P.; Caporali, S.; Bonmassar, E.; DAtri, S.
    Combined effect of temozolomide and hyperthermia on human melanoma cell growth and O6-methylguanine-DNA methyltransferase activity (2007), Int. J. Oncol., 30, 443-451.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.1.1.63 medicine temozolomide appears to be a good candidate for use in conjunction with hyperthermia for regional chemotherapy of melanoma Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.1.1.63 4-[bis(2-chloroethyl)amino]-L-phenylalanine hyperthermia enhances the inhibitory effects of L-phenylalanine mustard on melanoma cell growth Homo sapiens
2.1.1.63 temozolomide TMZ; tumor cells with high levels of MGMT and/or with a defective DNA mismatch repair are resistant to temozolomide, hyperthermia significantly enhances temozolomide cytotoxicity in mismatch repair-proficient cells, either endowed or not with MGMT activity, and in mismatch repair-deficient cells, hyperthermia alone does not affect MGMT activity, but enhances the enzyme depletion induced by temozolomide treatment Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.1.1.63 DNA (containing 6-O-methylguanine) + [protein]-L-cysteine Homo sapiens
-
 DNA (without 6-O-methylguanine) + [protein]-S-methyl-L-cysteine
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.1.1.63 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.1.1.63 M14 cell
-
 Homo sapiens
-
2.1.1.63 melanoma cell line
-
 Homo sapiens
-
2.1.1.63 melanoma cell line three lines with different MGMT activity and functional status of the mismatch repair system Homo sapiens
-
2.1.1.63 additional information PR-Mel cell and GL-Mel-D2 cell Homo sapiens
-
2.1.1.63 PR-Mel cell
-
 Homo sapiens
-

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
2.1.1.63 additional information
-
 M14 cell line, 136, PR-Mel cell line 15 fmol of 3H-methyl groups transferred per mg of protein in cell extract Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.1.1.63 DNA (containing 6-O-methylguanine) + [protein]-L-cysteine
-
 Homo sapiens DNA (without 6-O-methylguanine) + [protein]-S-methyl-L-cysteine
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.1.1.63 MGMT
-
 Homo sapiens
2.1.1.63 O6-methylguanine-DNA methyltransferase
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.1.1.63 37
-
-
 Homo sapiens
2.1.1.63 41.5
-
 hyperthermic condition Homo sapiens