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2-([2-amino-6-[(4-bromothiophen-2-yl)methoxy]-9H-purin-9-yl]methoxy)ethanol
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2-amino-O4-benzyl-6,7-dimethylpteridine
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potent
2-amino-O4-benzyl-6-formylpteridine
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potent
2-amino-O4-benzyl-6-hydroxymethylpteridine
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potent
2-amino-O4-benzylpteridine
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potent
2-amino-O4-benzylpteridine-6-carboxylic acid
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potent
2-hexaprenyl-6-methoxy-1,4-benzoquinone
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4-[(4-bromothiophen-2-yl)methoxy]-1H-pyrazolo[3,4-d]pyrimidin-6-amine
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4-[bis(2-chloroethyl)amino]-L-phenylalanine
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hyperthermia enhances the inhibitory effects of L-phenylalanine mustard on melanoma cell growth
6-(1-benzofuran-2-ylmethoxy)-9H-purin-2-amine
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6-(4,5,6,7-tetrahydro-1-benzothiophen-2-ylmethoxy)-9H-purin-2-amine
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6-(naphtho[1,2-b]thiophen-2-ylmethoxy)-9H-purin-2-amine
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6-(naphtho[2,1-b]thiophen-2-ylmethoxy)-9H-purin-2-amine
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6-(phenanthro[9,10-b]thiophen-2-ylmethoxy)-9H-purin-2-amine
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6-[(1-methyl-4-nitro-1H-pyrrol-2-yl)methoxy]-9H-purin-2-amine
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6-[(4-bromothiophen-2-yl)methoxy]-9-(2-deoxy-beta-D-erythro-pentofuranosyl)-9H-purin-2-amine
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7-[(4-bromothiophen-2-yl)methoxy]-2,3-dihydro-1H-[1,2,3]triazolo[4,5-d]pyrimidin-5-amine
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9-beta-D-arabinofuranosyl-6-[(4-bromothiophen-2-yl)methoxy]-9H-purin-2-amine
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alkyltransferase-like protein
inhibits the transfer of methyl groups to MGMT, thus the action of MGMT on 6-O-methylguanine in DNA, inhibition is reversible by prolonged incubation in the presence of MGMT
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Br(CH2)2Br
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inactivates purified AGT and mutant R128A to approximately the same extent; inactivates purified AGT and mutant R128A to approximately the same extent, small reduction in the loss of activity in the absence of DNA, but no effect at all in the presence of DNA, inactivates mutant Y114A much less than wild-type, and DNA completely prevents this inactivation, mutants P140K and Y158H are less inactivated than wild-type AGT, specifically in the presence of DNA
Br(CH2)3Br
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mutant P140K requires higher concentrations than wild-type AGT for inactivation
Br(CH2)5Br
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mutant P140K requires higher concentrations than wild-type AGT for inactivation
BrCH2Br
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wild-type AGT and mutant P140K show no difference in sensitivity to BrCH2Br
BrCH2OAc
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reacts with the enzyme at its cysteine acceptor site, abolishing its DNA repair activity, the formation of AGT-Cys145S-CH2Br by BrCH2OAc
CH2Br2
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reacts with the enzyme at its cysteine acceptor site, abolishing its DNA repair activity
DNA (containing 6-O-carboxymethylguanine)
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DNA (containing 6-O-methylguanine)
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double-stranded oligonucleotides
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6-O-methylguanine, 6-O-(4-fluorobenzyl)-guanine, 6-O-(3-fluorobenzyl)-guanine, 6-O-(2-fluorobenzyl)-guanine, 6-O-benzylguanine, 6-O-benzylhypoxanthine. IC50: 1.4-3.0 nM
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formaldehyde
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decreases activity at levels up to 3fold higher than the maximally allowed workplace concentration, no decrease at the maximally allowed level
methyl iodide
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can directly alkylate the active site of the enzyme, the agent can increase the effectiveness of environmental and endogenously produced alkylating carcinogens in producing the mutagenic 6-O-alkylguanine residue in DNA in vivo
methyl isocyanate
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methyl isocyanate resulting from base-catalyzed activation of VNP40101M inhibits the enzyme, thereby enhancing the yield of the DNA G-C interstrand crosslink responsible for the antitumor activity of this agent
N9-cyclopentyl-O6-(4-bromothenyl)guanine
efficient inhibitor of wild-type AGT
Ni2+
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purified protein is not very sensitive to this metal but the loss of AGT could contribute to the well-known carcinogenicity of nickel
O4-(4-bromothenylpterin)
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O4-benzylfolic acid
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30times more active than O6-benzylguanine against the wild-type alkyltransferase, inactivation of P140K mutant alkyltransferase. Inhibitor shows promise as an agent for possible tumor-selective alkyltransferase inactivation superior toO6-benzylguanine as a chemotherapy adjuvant
O6-(1,2-thiazol-4-ylmethyl)guanine
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O6-(1,3-oxazol-5-yl)guanine
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O6-(1,3-thiazol-5-yl)guanine
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O6-(1-benzofuran-2-ylmethyl)guanine
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O6-(2-benzo[b]thienylmethyl)guanine
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O6-(3-pyridyl)guanine
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O6-(4-(2-chloropyridyl))guanine
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O6-(4-bromothenyl)-8-oxaguanine
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O6-(4-bromothenyl)-8-thiaguanine
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O6-(4-bromothenyl)guanine
O6-(4-pyridyl)guanine
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O6-alkylating drugs
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O6-alkylating drugs deplete MGMT activity indirectly via alkylation of DNA
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O6-benzyl-2'-deoxyguanosine
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O6-methylguanine oligonucleotide
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O6-thenylguanine
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original Patrin, became Patrin-1
O6-[(1-methyl-1H-imidazol-5-yl)methyl]guanine
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VNP40101M
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methyl isocyanate resulting from base-catalyzed activation of VNP40101M inhibits the enzyme, thereby enhancing the yield of the DNA G-C interstrand crosslink responsible for the antitumor activity of this agent
6-O-benzylguanine
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6-O-benzylguanine
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competitive
6-O-benzylguanine
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competitive
6-O-benzylguanine
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competitive
DNA
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methyl bromide
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Na2SO4
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Na3 citrate
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NaCl
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0.2 M, 80% inhibition
NaCl
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0.2 M, wild-type and mutant enzyme, 55% inhibition
O6-(4-bromothenyl)guanine
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O6-(4-bromothenyl)guanine
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most potent inactivator described to date
O6-(4-bromothenyl)guanine
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pseudosubstrate, direct inhibitor
O6-(4-bromothenyl)guanine
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PaTrin, PaTrin-2, Lomeguatrib
O6-benzylguanine
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O6-benzylguanine
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potent inhibitor of wild-type enzyme, no inactivation of mutant enzyme P140K
O6-benzylguanine
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mutants P140K and Y158H are the most resistant
O6-benzylguanine
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binds in the active site pocket, abolishes resistance against therapeutic agents temozolomide and N,N'-bis(2-chloroethyl)-N-nitrosourea
O6-benzylguanine
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pseudosubstrate, direct inhibitor
O6-benzylguanine
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a synthetic MGMT inhibitor
O6-benzylguanine
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the pseudosubstrate depletes the enzyme by activating its suicidal dealkylation mechanism
O6-benzylguanine
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pretreatment of Mgmt+/+ mice prior to 1,3-bis (2-chloroethyl)-1-nitrosourea does not result in significantly more mutations than mice treated with 1,3-bis (2-chloroethyl)-1-nitrosourea alone
O6-methylguanine oligonucleotide
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preincubation of extracts with a short oligonucleotide containing a single O6-methylguanine residue causes essentially complete loss of ATase activity
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O6-methylguanine oligonucleotide
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preincubation of extracts with a short oligonucleotide containing a single O6-methylguanine residue causes essentially complete loss of ATase activity
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O6-methylguanine oligonucleotide
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preincubation of extracts with a short oligonucleotide containing a single O6-methylguanine residue causes essentially complete loss of ATase activity
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O6-methylguanine oligonucleotide
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preincubation of extracts with a short oligonucleotide containing a single O6-methylguanine residue causes essentially complete loss of ATase activity
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O6-methylguanine oligonucleotide
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preincubation of extracts with a short oligonucleotide containing a single O6-methylguanine residue causes essentially complete loss of ATase activity
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RNA
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temozolomide
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treatment for 5 days depletes MGMT in peripheral mononuclear cells in at least 76% of patients and low MGMT activity is correlated with severe thrombocytopenia during the first treatment cycle
temozolomide
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TMZ; tumor cells with high levels of MGMT and/or with a defective DNA mismatch repair are resistant to temozolomide, hyperthermia significantly enhances temozolomide cytotoxicity in mismatch repair-proficient cells, either endowed or not with MGMT activity, and in mismatch repair-deficient cells, hyperthermia alone does not affect MGMT activity, but enhances the enzyme depletion induced by temozolomide treatment
additional information
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transferase activity methylates itself on removal of the methyl group from the 6-O position of guanine. Modification of a reactive sulfhydryl group can account for the enzyme inactivation accompanying the reaction
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additional information
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the alkyl group is transferred without a cofactor to Cys145 residue of the enzyme and thereby inactivates the protein
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additional information
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high level of enzyme in tumors and relative resistance to cyclophosphamide in lung cancer indicates that 6-O-methylguanine-DNA methyltransferase may be a predictive factor of resistance to cyclophosphamide
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additional information
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substances present in the saliva of tobacco and betel nut chewers
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additional information
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hydroxyethyl guanine-modified oligodeoxyribonucleotides are not effective inactivators of MGMT
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additional information
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epigenetic silencing by promoter methylation, it has been reported that the E1A gene product of adenovirus efficiently inhibits the promoter activity of MGMT
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additional information
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the enzyme repairs alkylated DNA by suicidal alkyl transfer from guanine 6-O to its own Cys residue
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