Proteins > Methylated-DNA--protein-cysteine methyltransferase
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Methylated-DNA--protein-cysteine methyltransferase
A methylated-DNA--protein-cysteine methyltransferase that is encoded in the genome of human. [PRO:DNx, UniProtKB:P16455]
Synonyms
EC 2.1.1.63;
6-O-methylguanine-DNA methyltransferase;
MGMT;
O-6-methylguanine-DNA-alkyltransferase
Research
Bioassay Publications (10)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 4 (40.00) | 18.2507 |
| 2000's | 4 (40.00) | 29.6817 |
| 2010's | 2 (20.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (8)
Drugs with Inhibition Measurements
Drugs with Other Measurements
Design of a hypoxia-activated prodrug inhibitor of O6-alkylguanine-DNA alkyltransferase.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 22, Issue:19, 2012
Substitution of aminomethyl at the meta-position enhances the inactivation of O6-alkylguanine-DNA alkyltransferase by O6-benzylguanine.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
2-amino-O4-benzylpteridine derivatives: potent inactivators of O6-alkylguanine-DNA alkyltransferase.Journal of medicinal chemistry, , Jul-15, Volume: 47, Issue:15, 2004
Monosaccharide-linked inhibitors of O(6)-methylguanine-DNA methyltransferase (MGMT): synthesis, molecular modeling, and structure-activity relationships.Journal of medicinal chemistry, , Nov-22, Volume: 44, Issue:24, 2001
Resistance-modifying agents. 8. Inhibition of O(6)-alkylguanine-DNA alkyltransferase by O(6)-alkenyl-, O(6)-cycloalkenyl-, and O(6)-(2-oxoalkyl)guanines and potentiation of temozolomide cytotoxicity in vitro by O(6)-(1-cyclopentenylmethyl)guanine.Journal of medicinal chemistry, , Nov-02, Volume: 43, Issue:22, 2000
Inactivation of O6-alkylguanine-DNA alkyltransferase. 1. Novel O6-(hetarylmethyl)guanines having basic rings in the side chain.Journal of medicinal chemistry, , Dec-17, Volume: 41, Issue:26, 1998
Inhibition of human O6-alkylguanine-DNA alkyltransferase and potentiation of the cytotoxicity of chloroethylnitrosourea by 4(6)-(benzyloxy)-2,6(4)-diamino-5-(nitro or nitroso)pyrimidine derivatives and analogues.Journal of medicinal chemistry, , Feb-12, Volume: 41, Issue:4, 1998
8-Substituted O6-benzylguanine, substituted 6(4)-(benzyloxy)pyrimidine, and related derivatives as inactivators of human O6-alkylguanine-DNA alkyltransferase.Journal of medicinal chemistry, , Jan-20, Volume: 38, Issue:2, 1995
Structural features of substituted purine derivatives compatible with depletion of human O6-alkylguanine-DNA alkyltransferase.Journal of medicinal chemistry, , Nov-13, Volume: 35, Issue:23, 1992
Resistance-modifying agents. 8. Inhibition of O(6)-alkylguanine-DNA alkyltransferase by O(6)-alkenyl-, O(6)-cycloalkenyl-, and O(6)-(2-oxoalkyl)guanines and potentiation of temozolomide cytotoxicity in vitro by O(6)-(1-cyclopentenylmethyl)guanine.Journal of medicinal chemistry, , Nov-02, Volume: 43, Issue:22, 2000
Structural features of substituted purine derivatives compatible with depletion of human O6-alkylguanine-DNA alkyltransferase.Journal of medicinal chemistry, , Nov-13, Volume: 35, Issue:23, 1992
Inhibition of human O6-alkylguanine-DNA alkyltransferase and potentiation of the cytotoxicity of chloroethylnitrosourea by 4(6)-(benzyloxy)-2,6(4)-diamino-5-(nitro or nitroso)pyrimidine derivatives and analogues.Journal of medicinal chemistry, , Feb-12, Volume: 41, Issue:4, 1998
8-Substituted O6-benzylguanine, substituted 6(4)-(benzyloxy)pyrimidine, and related derivatives as inactivators of human O6-alkylguanine-DNA alkyltransferase.Journal of medicinal chemistry, , Jan-20, Volume: 38, Issue:2, 1995
Towards more specific O6-methylguanine-DNA methyltransferase (MGMT) inactivators.Bioorganic & medicinal chemistry, , Mar-01, Volume: 19, Issue:5, 2011
Monosaccharide-linked inhibitors of O(6)-methylguanine-DNA methyltransferase (MGMT): synthesis, molecular modeling, and structure-activity relationships.Journal of medicinal chemistry, , Nov-22, Volume: 44, Issue:24, 2001
Enables
This protein enables 5 target(s):
| Target | Category | Definition |
|---|
| DNA binding | molecular function | Any molecular function by which a gene product interacts selectively and non-covalently with DNA (deoxyribonucleic acid). [GOC:dph, GOC:jl, GOC:tb, GOC:vw] |
| methyltransferase activity | molecular function | Catalysis of the transfer of a methyl group to an acceptor molecule. [ISBN:0198506732] |
| DNA-methyltransferase activity | molecular function | Catalysis of the transfer of a methyl group to a DNA molecule. [GOC:jl, ISBN:0198506732, PMID:7862522] |
| metal ion binding | molecular function | Binding to a metal ion. [GOC:ai] |
| methylated-DNA-[protein]-cysteine S-methyltransferase activity | molecular function | Catalysis of the reaction: DNA (containing 6-O-methylguanine) + (protein)-L-cysteine = DNA (without 6-O-methylguanine) + protein S-methyl-L-cysteine. [EC:2.1.1.63] |
Located In
This protein is located in 2 target(s):
| Target | Category | Definition |
|---|
| nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
Involved In
This protein is involved in 6 target(s):
| Target | Category | Definition |
|---|
| DNA ligation | biological process | The re-formation of a broken phosphodiester bond in the DNA backbone, carried out by DNA ligase. [ISBN:0815316194] |
| DNA alkylation repair | biological process | The repair of alkylation damage in DNA, e.g. the removal of a non-physiological alkyl group from a nucleobase. This is usually mediated by DNA alkyltransferases. [PMID:10946226, PMID:35543797] |
| methylation | biological process | The process in which a methyl group is covalently attached to a molecule. [GOC:mah] |
| negative regulation of apoptotic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis] |
| positive regulation of double-strand break repair | biological process | Any process that activates or increases the frequency, rate or extent of double-strand break repair. [GOC:BHF] |
| DNA repair | biological process | The process of restoring DNA after damage. Genomes are subject to damage by chemical and physical agents in the environment (e.g. UV and ionizing radiations, chemical mutagens, fungal and bacterial toxins, etc.) and by free radicals or alkylating agents endogenously generated in metabolism. DNA is also damaged because of errors during its replication. A variety of different DNA repair pathways have been reported that include direct reversal, base excision repair, nucleotide excision repair, photoreactivation, bypass, double-strand break repair pathway, and mismatch repair pathway. [PMID:11563486] |