Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary extracted from

  • Verbeek, B.; Southgate, T.D.; Gilham, D.E.; Margison, G.P.
    O6-Methylguanine-DNA methyltransferase inactivation and chemotherapy (2008), Br. Med. Bull., 85, 17-33.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
2.1.1.63 dexamethasone
-
 Homo sapiens
2.1.1.63 glucocorticoid
-
 Homo sapiens
2.1.1.63 additional information DNA damage, ionizing radiation Homo sapiens
2.1.1.63 P53 controversly discussed Homo sapiens

Application

EC Number Application Comment Organism
2.1.1.63 medicine inhibition of tumour MGMT by pseudosubstrates to overcome tumour resistance is under clinical evaluation, MGMT overexpression in haematopoietic stems cells has been shown to protect normal cells against the myelosuppressive effects of chemotherapy Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
2.1.1.63 G156A mutant MGMT protein that is resistant to inactivators of the wild-type protein, used in myeloprotective gene therapy Homo sapiens
2.1.1.63 P140K mutant MGMT protein that is resistant to inactivators of the wild-type protein, used in myeloprotective gene therapy Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.1.1.63 additional information epigenetic silencing by promoter methylation, it has been reported that the E1A gene product of adenovirus efficiently inhibits the promoter activity of MGMT Homo sapiens
2.1.1.63 O6-(4-bromothenyl)guanine pseudosubstrate, direct inhibitor Homo sapiens
2.1.1.63 O6-alkylating drugs O6-alkylating drugs deplete MGMT activity indirectly via alkylation of DNA Homo sapiens
2.1.1.63 O6-benzylguanine pseudosubstrate, direct inhibitor 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 liver MGMT is ubiquitously expressed, the liver expresses the highest levels and haematopoietic tissues and brain the lowest 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 methylated-DNA-[protein]-cysteine S-methyltransferase
-
 Homo sapiens
2.1.1.63 MGMT
-
 Homo sapiens
2.1.1.63 O6-methylguanine-DNA methyltransferase
-
 Homo sapiens