Target Information
Target General Infomation | |||||
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Target ID |
T24587
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Former ID |
TTDR00624
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Target Name |
Methylated-DNA--protein-cysteine methyltransferase
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Gene Name |
MGMT
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Synonyms |
6-O-methylguanine-DNA methyltransferase; Human O(6)-alkylguanine-DNA alkyltransferase; O-6-methylguanine-DNA-alkyltransferase; MGMT
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Target Type |
Clinical Trial
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Disease | Sarcoma [ICD9: 202.8; ICD10: C81-C86] | ||||
Function |
Involved in the cellular defense against the biological effects of O6-methylguanine (O6-MeG) in DNA. Repairs alkylated guanine in DNA by stoichiometrically transferring the alkyl group at the O-6 position to a cysteine residue in the enzyme. This is a suicide reaction: the enzyme is irreversibly inactivated.
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BioChemical Class |
Methyltransferase superfamily
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Target Validation |
T24587
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UniProt ID | |||||
EC Number |
EC 2.1.1.63
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Sequence |
MDKDCEMKRTTLDSPLGKLELSGCEQGLHEIKLLGKGTSAADAVEVPAPAAVLGGPEPLM
QCTAWLNAYFHQPEAIEEFPVPALHHPVFQQESFTRQVLWKLLKVVKFGEVISYQQLAAL AGNPKAARAVGGAMRGNPVPILIPCHRVVCSSGAVGNYSGGLAVKEWLLAHEGHRLGKPG LGGSSGLAGAWLKGAGATSGSPPAGRN |
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Drugs and Mode of Action | |||||
Inhibitor | 6-Allyloxy-9H-purin-2-ylamine | Drug Info | [525899] | ||
6-Benzyloxy-5-nitro-pyrimidine-2,4-diamine | Drug Info | [534565] | |||
6-Benzyloxy-5-nitroso-pyrimidine-2,4-diamine | Drug Info | [534565] | |||
6-Benzyloxy-9H-purin-2-ylamine | Drug Info | [534565] | |||
Benzylcysteine | Drug Info | [551393] | |||
S-Methylcysteine | Drug Info | [551393] | |||
Modulator | O6-Benzylguanine alkylade | Drug Info | [527774], [529958] | ||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
WikiPathways | DNA Damage Reversal | ||||
References | |||||
Ref 525899 | J Med Chem. 2000 Nov 2;43(22):4071-83.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. | ||||
Ref 527774 | Phase I trial of temozolomide plus O6-benzylguanine for patients with recurrent or progressive malignant glioma. J Clin Oncol. 2005 Oct 1;23(28):7178-87. | ||||
Ref 529958 | Phase II trial of temozolomide plus o6-benzylguanine in adults with recurrent, temozolomide-resistant malignant glioma. J Clin Oncol. 2009 Mar 10;27(8):1262-7. |
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