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1-(3',4'-dideoxy-3'-fluoro-beta-D-glucopyranosyl) cytosine
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1-(3',4'-dideoxy-3'-fluoro-beta-D-glucopyranosyl)-N4-benzoyl cytosine
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1-hydroxy-3-(3-methylbutyl)-7-(2-phenylethyl)-3,7-dihydro-1H-purine-2,6-dione
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1-hydroxy-3-methyl-7-(2-phenylethyl)-3,7-dihydro-1H-purine-2,6-dione
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1-hydroxy-3-nonyl-7-(2-phenylethyl)-3,7-dihydro-1H-purine-2,6-dione
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1-hydroxy-3-pentyl-7-(2-phenylethyl)-3,7-dihydro-1H-purine-2,6-dione
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1-hydroxy-3-[(morpholin-4-yl)methyl]-7-(2-phenylethyl)-3,7-dihydro-1H-purine-2,6-dione
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1-hydroxy-7-(2-phenylethyl)-3,7-dihydro-1H-purine-2,6-dione
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1-hydroxy-7-(2-phenylethyl)-3-(3-phenylpropyl)-3,7-dihydro-1H-purine-2,6-dione
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1-hydroxy-7-(phenoxymethyl)-3,7-dihydro-1H-purine-2,6-dione
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1-hydroxy-7-(pyridin-2-yl)-3,7-dihydro-1H-purine-2,6-dione
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1-hydroxy-7-(pyridin-3-yl)-3,7-dihydro-1H-purine-2,6-dione
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1-hydroxy-7-(pyridin-4-yl)-3,7-dihydro-1H-purine-2,6-dione
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1-hydroxy-7-phenyl-3,7-dihydro-1H-purine-2,6-dione
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1-hydroxy-7-[(pyridin-2-yl)methyl]-3,7-dihydro-1H-purine-2,6-dione
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1-hydroxy-7-[(thiophen-2-yl)methyl]-3,7-dihydro-1H-purine-2,6-dione
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3-aminotriazole
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competitive inhibitor
3-benzyl-1-hydroxy-7-(2-phenylethyl)-3,7-dihydro-1H-purine-2,6-dione
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3-decyl-1-hydroxy-7-(2-phenylethyl)-3,7-dihydro-1H-purine-2,6-dione
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3-dodecyl-1-hydroxy-7-(2-phenylethyl)-3,7-dihydro-1H-purine-2,6-dione
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3-ethyl-1-hydroxy-7-(2-phenylethyl)-3,7-dihydro-1H-purine-2,6-dione
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3-hydroxy-6,7,8,9-tetrahydropyrido[2,1-f]purine-2,4(1H,3H)-dione
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3-[2-(dimethylamino)ethyl]-1-hydroxy-7-(2-phenylethyl)-3,7-dihydro-1H-purine-2,6-dione
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6-hydroxy-1-(2-phenylethyl)-1,4-dihydro-5H-imidazo[4,5-b]pyridin-5-one
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7-(2-butoxyethyl)-1-hydroxy-3,7-dihydro-1H-purine-2,6-dione
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7-benzyl-1-hydroxy-3,7-dihydro-1H-purine-2,6-dione
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7-benzyl-1-[(prop-2-en-1-yl)oxy]-3,7-dihydro-1H-purine-2,6-dione
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7-benzyl-3,7-dihydro-1H-purine-2,6-dione
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9-(3',4'-dideoxy-3'-fluoro-beta-D-glucopyranosyl)-N6-benzoyl adenine
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ADP
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purine monophosphate (RMP) and diphosphate nucleotides (RDP) exhibit competitive inhibition, furthermore PARN does not discriminate whether there is ribose or deoxyribose in the nucleotides, Mg2+ releases the inhibition by RDPs and RTPs, but not by RMPs
ATP
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purine triphosphate nucleotides (RTP) behave as non-competitive inhibitors, furthermore PARN does not discriminate whether there is ribose or deoxyribose in the nucleotides, Mg2+ releases the inhibition by RDPs and RTPs, but not by RMPs
Ca2+
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3 mM gradually decreases activity about 15fold
cap analogue 7-methylguanosine(5')ppp(5')G
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allosteric inhibitor of PARN in the presence of a physiological K+ concentration
Co2+
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3 mM gradually decreases activity about 78fold
deoxyATP
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purine triphosphate nucleotides (RTP) behave as non-competitive inhibitors, furthermore PARN does not discriminate whether there is ribose or deoxyribose in the nucleotides, Mg2+ releases the inhibition by RDPs and RTPs, but not by RMPs
deoxyGTP
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purine triphosphate nucleotides (RTP) behave as non-competitive inhibitors, furthermore PARN does not discriminate whether there is ribose or deoxyribose in the nucleotides, Mg2+ releases the inhibition by RDPs and RTPs, but not by RMPs
eIF4E
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competition between PARN and eIF4E for the 5'-cap
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GDP
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purine monophosphate (RMP) and diphosphate nucleotides (RDP) exhibit competitive inhibition, furthermore PARN does not discriminate whether there is ribose or deoxyribose in the nucleotides, Mg2+ releases the inhibition by RDPs and RTPs, but not by RMPs
GMP
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purine monophosphate (RMP) and diphosphate nucleotides (RDP) exhibit competitive inhibition, furthermore PARN does not discriminate whether there is ribose or deoxyribose in the nucleotides, Mg2+ releases the inhibition by RDPs and RTPs, but not by RMPs
GTP
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purine triphosphate nucleotides (RTP) behave as non-competitive inhibitors, furthermore PARN does not discriminate whether there is ribose or deoxyribose in the nucleotides, Mg2+ releases the inhibition by RDPs and RTPs, but not by RMPs
guanidine hydrochloride
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full-length enzyme retains most of its activity at guanidine hydrochloride concentrations below 0.5 M, whereas an abrupt decrease of the activity of p54 and p46 is found when guanidine hydrochloride concentration is increased
kanamycin A
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50% inhibition by high nanomolar concentrations, competition with divalent metal ions
kanamycin B
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50% inhibition by high nanomolar concentrations, competition with divalent metal ions
lividomycin
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50% inhibition by high nanomolar concentrations, competition with divalent metal ions
m7G(5')ppp(5')G cap analogue
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Mg2+
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behaves as a destabilizer of the overall structural stability of PARN, promotes thermal unfolding and aggregation at high temperatures
Mn2+
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3 mM gradually decreases activity about 5fold
NaCl
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inhibition at 0.2 M ionic strength; inhibits at 150-200 mM
neomycin
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antibiotic neomycin B inhibits approximately 80% of PARN activity at a concentration of 10 microg/ml
neomycin B
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50% inhibition by high nanomolar concentrations, inhibition is pH-dependent, competition with divalent metal ions
NSC-86353
substitution of the benzyl moiety with a methyl group at the N7 position (NSC-85703) reduces the inhibitory activity over 10fold
paromomycin
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50% inhibition by high nanomolar concentrations, competition with divalent metal ions
phosphate
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inhibits at 10 mM
Poly(A)
strong inhibition of both spermidine- and polyadenylate-binding protein-activated hPAN complex
poly(A)-binding protein PAB 1
inhibits; phased poly(A) shortening
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poly(C)
strong inhibition of spermidine-, slight inhibition of polyadenylate-binding protein-activated hPAN complex
poly[2'-O-(2,4-dinitrophenyl)]poly-(A)
competitive
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purine nucleotides
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purine triphosphate nucleotides (RTP) behave as non-competitive inhibitors while purine monophosphate (RMP) and diphosphate nucleotides (RDP) exhibit competitive inhibition, furthermore PARN does not discriminate whether there is ribose or deoxy-ribose in the nucleotides, Mg2+ releases the inhibition by RDPs and RTPs, but not by RMPs
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synthetic fluoro-pyranosyl nucleosides
synthetic nucleoside analogues bearing a fluoroglucopyranosyl sugar moiety and benzoyl-modified cytosine or adenine as a base can effectively inhibit human PARN
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tobramycin
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50% inhibition by high nanomolar concentrations, competition with divalent metal ions
Zn2+
enzyme is inhibited by high zinc concentration with only two ions and 1mM Zn2+
AMP
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AMP
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purine monophosphate (RMP) and diphosphate nucleotides (RDP) exhibit competitive inhibition, furthermore PARN does not discriminate whether there is ribose or deoxyribose in the nucleotides, Mg2+ releases the inhibition by RDPs and RTPs, but not by RMPs
CH3COOK
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inhibits in presence of spermidine
CH3COOK
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inhibits in presence of spermidine
EDTA
activity is completely lost when the ions are removed from the wild-type enzyme by incubation with 10mM
K3PO4
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inhibits in presence of spermidine
K3PO4
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inhibits in presence of spermidine
additional information
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model of inhibition mechanism for aminoglycosides, competition with divalent metal ions
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additional information
discovery, synthesis and biochemical profiling of purine-2,6-dione derivatives as inhibitors of the human poly(A)-selective ribonuclease Caf1. Possible interaction modes of 3-hydroxy-pyrimidine-2,4-dione compounds with two divalent metal ions in the active site of Caf1, overview
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additional information
discovery, synthesis and biochemical profiling of purine-2,6-dione derivatives as inhibitors of the human poly(A)-selective ribonuclease Caf1. Possible interaction modes of 3-hydroxy-pyrimidine-2,4-dione compounds with two divalent metal ions in the active site of Caf1, overview
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additional information
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discovery, synthesis and biochemical profiling of purine-2,6-dione derivatives as inhibitors of the human poly(A)-selective ribonuclease Caf1. Possible interaction modes of 3-hydroxy-pyrimidine-2,4-dione compounds with two divalent metal ions in the active site of Caf1, overview
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additional information
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stress like hyperosmolarity, heat shock, and glucose deprivation, inhibit the ability of Ccr4p/Pop2p/Notp to deadenylate mRNA
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additional information
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a poly(A) competitor inhibits RNA-A60 deadenylation by isozyme PARN-1, whereas a poly(C) competitor has no effect on RNA-A60 deadenylation
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