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(alpha-S,5S)-alpha-amino-3-chloro-4,5-dihydro-5-isoxazoleacetic acid
trivial name acivicin
1,N6-Ethenoadenosine 5'-triphosphate
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1-Ribosyl-4,6-dihydroxypyrazolo[3,4-d]-pyrimidine 5'-phosphate
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1-Ribosyl-4-hydroxy-6-aminopyrazolo[3,4-d]pyrimidine 5'-phosphate
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2,6-diaminopurine ribonucleoside
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2-Amino-6-methylthiopurine ribonucleoside
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2-fluoroinosine 5'-monophosphate
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50% inhibition above 2 mM
5'-Azido-5'-deoxyadenosine
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5'-thioethyl-5'-deoxyadenosine
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6-Amino-9-D-psicofuranosylpurine
6-Chloropurine ribonucleoside
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6-diazo-5-oxo-L-norleucine
6-Methylmercaptopurine ribonucleoside
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6-Methylpurine ribonucleoside
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6-Methylpurine ribonucleotide
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6-thioguanine
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0.5 mM, 27% inhibition
8-Azaguanine
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0.5 mM, 40% inhibition
adenine 9-beta-D-arabinofuranoside 5'-triphosphate
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adenosine 5'-(beta,gamma-imido)triphosphate
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non-competitive versus XMP, competitive versus ATP
AMP-PNP
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potent inhibitor, competitive and non-competitive inhibitor with respect to ATP and XMP
beta,gamma-Imidoadenosine 5-triphosphate
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Bredinin 5'-phosphate
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GDP
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0.5 mM, 42% inhibition
Glucofuranosyladenine
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glutamic acid-gamma-methyl ester
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competitive towards Gln
GTP
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0.5 mM, 40% inhibition
guanidine hydrochloride
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guanosine
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0.5 mM, 50% inhibition
IMP
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0.5 mM, 10% inhibition
iodoacetamide
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inhibition of Gln-dependent activity, no inhibition of NH4+-dependent activity
kinetin ribonucleoside
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L-2-Amino-4-oxo-5-chloropentanoic acid
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inhibition of Gln-dependent activity and NH4+-dependent activity
N2-hydroxyguanosine 5'-monophosphate
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0.0003-0.0005 mM, 50% inhibition
N6,N6-Dimethyladenosine
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N6-Hydroxyaminopurine ribonucleoside
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N6-isopentenyladenosine
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Na+
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25% loss of activity at 24 mM, 90% loss of activity at 200 mM
Nucleodide inhibitors
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overview
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XMP
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substrate inhibition above 0.2 mM
zeatin ribonucleoside
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additional information
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not inhibitory at 0.5 mM: hypoxanthine, chloroadenosine, xanthosine, inosine, decoyinine
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5'-deoxyadenosine
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6-Amino-9-D-psicofuranosylpurine
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strong inhibition of wild type enzyme, mutant enzyme GP-1 with decreased inhibition, complete loss of inhibition of mutant enzyme MG-1
6-Amino-9-D-psicofuranosylpurine
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i.e. psicofuranine, irreversible inhibition, dependent on presence of XMP and diphosphate
6-Amino-9-D-psicofuranosylpurine
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6-diazo-5-oxo-L-norleucine
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6-diazo-5-oxo-L-norleucine
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irreversible inhibition is dependent on presence of XMP, ATP and Mg2+
6-diazo-5-oxo-L-norleucine
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irreversible inhibition of Gln-dependent activity
6-diazo-5-oxo-L-norleucine
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inhibition of Gln-dependent activity and NH4+-dependent activity
6-diazo-5-oxo-L-norleucine
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Gln-dependent activity is more sensitive than NH4+-dependent activity; inhibition of Gln-dependent activity and NH4+-dependent activity
6-diazo-5-oxo-L-norleucine
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6-diazo-5-oxo-L-norleucine
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irreversible inhibitor
6-thioXMP
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acivicin
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selectively abolishes glutaminase activity and Gln-dependent synthetase activity. No effect on NH4+-dependent synthetase activity
acivicin
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irreversible inhibitor
adenosine
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strong inhibition of wild type enzyme, mutant GP-1 with decreased inhibition, complete loss of inhibition in mutant MG-1
adenosine
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0.5 mM, 37% inhibition
AMP
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poor product inhibitor, competitive towards ATP
AMP
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0.5 mM, 22% inhibitiion; 0.5 mM, 22% inhibition
ATP
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substrate inhibition
Decoyinine
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strong inhibition of wild type enzyme, and mutant enzyme GP-1, complete loss of inhibition in mutant MG-1
Decoyinine
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uncompetitive towards Gln and XMP and noncompetitive towards ATP
diphosphate
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competitive with respect to ATP; kinetic parameters for the two progressively formed inhibitory complexes
diphosphate
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competitive with respect to ATP
diphosphate
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non-competitive versus XMP, competitive versus ATP, non-competitive versus L-Gln; potent inhibitor, competitive and non-competitive inhibition with respect to ATP and XMP
GMP
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0.33 mM, 50% inhibition
GMP
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competitive versus XMP, uncompetitive versus ATP, non-competitive versus L-Gln; potent inhibitor, competitive and uncompetitive inhibition with respect to XMP and ATP
p-chloromercuribenzoate
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p-chloromercuribenzoate
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p-chloromercuribenzoate
Pigeon
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Psicofuranine
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Psicofuranine
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0.5 mM, 25% inhibition