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