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Literature summary for 2.1.1.63 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
Search for more literature for 2.1.1.63

Activating Compound

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

Application

Application Comment Organism
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

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

Inhibitors

Inhibitors Comment Organism Structure
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
O6-(4-bromothenyl)guanine pseudosubstrate, direct inhibitor Homo sapiens
O6-alkylating drugs O6-alkylating drugs deplete MGMT activity indirectly via alkylation of DNA Homo sapiens
O6-benzylguanine pseudosubstrate, direct inhibitor Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
liver MGMT is ubiquitously expressed, the liver expresses the highest levels and haematopoietic tissues and brain the lowest Homo sapiens
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
methylated-DNA-[protein]-cysteine S-methyltransferase
-
 Homo sapiens
MGMT
-
 Homo sapiens
O6-methylguanine-DNA methyltransferase
-
 Homo sapiens