3.1.26.4: ribonuclease H
This is an abbreviated version!
For detailed information about ribonuclease H, go to the full flat file.
Word Map on EC 3.1.26.4
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3.1.26.4
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antiretroviral
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nucleoside
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viruses
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nnrti
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virological
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hiv-infected
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nonnucleoside
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leukemia
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subtype
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integrase
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lymphocyte
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strand
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cd4
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efavirenz
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retroviral
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zidovudine
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drug-resistant
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infectious
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nevirapine
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retroviruses
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telomerase
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nucleic
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tenofovir
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lamivudine
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anti-hiv
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first-line
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virion
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t-cells
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surveillance
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retrotransposons
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haart
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polymerases
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proviral
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swab
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covid-19
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coronavirus
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ritonavir
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sars-cov-2
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outbreak
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telomeric
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nucleocapsid
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rna-dependent
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resistance-associated
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dntp
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treatment-naive
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hiv-positive
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moloney
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viremia
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cross-resistance
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pharmacology
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drug development
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analysis
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once-daily
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molecular biology
- 3.1.26.4
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antiretroviral
- nucleoside
- viruses
-
nnrti
-
virological
-
hiv-infected
-
nonnucleoside
- leukemia
- subtype
-
integrase
- lymphocyte
- strand
- cd4
- efavirenz
-
retroviral
- zidovudine
-
drug-resistant
- infectious
- nevirapine
- retroviruses
- telomerase
- nucleic
- tenofovir
- lamivudine
-
anti-hiv
-
first-line
- virion
- t-cells
-
surveillance
-
retrotransposons
-
haart
- polymerases
-
proviral
-
swab
- covid-19
- coronavirus
- ritonavir
- sars-cov-2
-
outbreak
-
telomeric
-
nucleocapsid
-
rna-dependent
-
resistance-associated
- dntp
-
treatment-naive
-
hiv-positive
-
moloney
- viremia
-
cross-resistance
- pharmacology
- drug development
- analysis
-
once-daily
- molecular biology
Reaction
Endonucleolytic cleavage to a 5'-phosphomonoester =
Synonyms
Ape-RNase HII, aRNase HII, Bh ribonuclease H, BhRNase H, CtepRNH, EcRNH, endoribonuclease H, endoribonuclease H (calf thymus), ERNH, huRNaseH1, hybrid nuclease, hybrid ribonuclease, hybridase, hybridase (ribonuclease H), KOD1, LC9-RNase H1, lmo1273, LRNase HII, More, nuclease, hybrid ribo-, nuclease, ribo-, H, P32, protein ST0753, reverse transcriptase, ribonuclease H, ribonuclease H I, ribonuclease H(42), ribonuclease H(70), ribonuclease H1, ribonuclease H2, ribonuclease H3, ribonuclease HI, ribonuclease HII, ribonuclease HIII, ribonulease H1, RNA*DNA hybrid ribonucleotidohydrolase, RNA*DNA hybrid ribonucleotiohydrolase, RNase H, RNase H type 2, RNase H(35), RNase H1, RNase H2, RNase H3, RNase HI, RNase HII, RNase HIII, RNaseH, Rnaseh1, RNASEH2A, RNH, RNH1, RNH2, rnhA, RnhB, rnhC, rnhD, Rv2228c, ST0519, STK_07530, Sto-RNase HI, T4 RNase H, Tk-RNase HII, Tk-Tk-RNase HII, TK0805, TRNH, TthRNH, Ty1 reverse transcriptase/RNase H, type 1 ribonuclease H, type 1 RNase H, type 2 ribonuclease H, type 2 RNase H, type II ribonuclease H
ECTree
3.1.26.4 ribonuclease HAdvanced search results
results (
results (Inhibitors
Inhibitors on EC 3.1.26.4 - ribonuclease H
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INHIBITOR 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
IMAGE
(1R,3R,4R,5R,8S)-8-benzyloxy-1-benzyloxymethyl-5-benzyloxyamino-3-(thymin-1-yl)-2-oxa-bicyclo[3.2.1]octane
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(1R,3R,4R,5R,8S)-8-benzyloxy-1-benzyloxymethyl-5-trifluoroacetamino-3-(thymin-1-yl)-2-oxa-bicyclo[3.2.1]octane
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(1R,3R,4R,5S,8S)-8-benzyloxy-1-benzyloxymethyl-5-((methylthio)thiocarbonyl)oxy-3-(thymin-1-yl)-2-oxa-bicyclo[3.2.1]octane
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(1R,3R,4R,5S,8S)-8-benzyloxy-1-benzyloxymethyl-5-(4-methylbenzoyl)-3-(thymin-1-yl)-2-oxa-bicyclo[3.2.1]octane
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(1R,3R,4R,5S,8S)-8-benzyloxy-1-benzyloxymethyl-5-hydroxy-3-(thymin-1-yl)-2-oxa-bicyclo[3.2.1]octane (20a) and (1R,3R,4R,5R,8S)-8-benzyloxy-1-benzyloxymethyl-5-hydroxy-3-(thymin-1-yl)-2-oxabicyclo[3.2.1]octane
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(1R,3R,4R,5S,8S)-8-benzyloxy-1-benzyloxymethyl-5-methoxalyloxy-5-methyl-3-(thymin-1-yl)-2-oxa-bicyclo[3.2.1]octane
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(1R,3R,4R,8S)-8-benzyloxy-1-benzyloxymethyl-3-(thymin-1-yl)-2-oxa-bicyclo[3.2.1]octane
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(1R,3R,4R,8S)-8-benzyloxy-1-benzyloxymethyl-5-one-3-(thymin-1-yl)-2-oxa-bicyclo[3.2.1]octane
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1,10-phenanthroline
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inhibition of Mn2+-dependent enzyme, no inhibition of the Mg2+-dependent enzyme
1,6-dihydroxy-4-methyl-5-[N-[(4-methylphenyl)methoxy]ethanimidoyl]pyridin-2(1H)-one
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1-(3,5-O-benzyl-2-O-phenoxythiocarbonyl-4-C-propionaldehyde-beta-D-ribofuranosyl)thymineO-benzyloxime
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1-(3,5-O-benzyl-4-C-propionaldehyde-2-O-hydroxyl-beta-D-ribofuranosyl)thymine O-benzyl oxime
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4-[(4'-aminomethyl-1,1'-biphenyl)methyl]-1-hydroxy-1,8-naphthyridin-2-one
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5-nitrofuran-2-carboxylic acid [[4-(4-bromophenyl)-thiazol-2-yl]-(tetrahydrofuran-2-ylmethyl)-carbamoyl]-methyl ester
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derivative of 5-nitrofuran-2-carboxylic acid carbamoyl methyl ester. 20-25 microM effectively inhibit HIV-1 replication
6-(naphthalen-2-yl)-3-(pyridin-3-yl)[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole
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7-(furan-2-yl)-2-hydroxy-isoquinoline-1,3(2H,4H)-dione
YLC2-155
antisense oligodeoxynucleotides
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directed against RNA polymerase II, replication protein A, and Ha-ras, determination of response in expression levels of the enzyme type 1 and 2, overview
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diphosphate
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inhibition of Mn2+-dependent enzyme, no inhibition of the Mg2+-dependent enzyme
methyl 7-benzamido-2-hydroxy-1,3-dioxo-1,2,3,4-tetrahydroisoquinoline-4-carboxylate
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N-(4-chlorophenyl)-6-hydroxy-2-methoxy-5,7-dioxo-5,6,7,8-tetrahydro-1,6-naphthyridine-8-carboxamide
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N-(4-fluorophenyl)-6-hydroxy-2-methoxy-5,7-dioxo-5,6,7,8-tetrahydro-1,6-naphthyridine-8-carboxamide
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N-cyclopentyl-2-(4,6-dimethyl-3-oxo[1,2]thiazolo[5,4-b]pyridin-2(3H)-yl)acetamide
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N-[(4-fluorophenyl)methyl]-2,6-dihydroxy-5,7-dioxo-5,6,7,8-tetrahydro-1,6-naphthyridine-8-carboxamide
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NH4Cl
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activity of enzyme form H1 decreases rapidly above 50 mM and becomes nearly abolished at 150 mM
Nucleic acids
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enzyme form H1 is more susceptible to inhibition than enzyme form H2
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spermidine
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inhibition of Mn2+-dependent enzyme, no inhibition of the Mg2+-dependent enzyme
spermine
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inhibition of Mn2+-dependent enzyme, no inhibition of the Mg2+-dependent enzyme
trihydroxy benzoyl biphenyl carboxylate hydrazone
BHMP07
1,6-dihydroxy-5-[N-[(2-methoxyphenyl)methoxy]ethanimidoyl]-4-methylpyridin-2(1H)-one
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1,6-dihydroxy-5-[N-[(2-methoxyphenyl)methoxy]ethanimidoyl]-4-methylpyridin-2(1H)-one
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1,6-dihydroxy-5-[N-[(4-methoxyphenyl)methoxy]ethanimidoyl]-4-methylpyridin-2(1H)-one
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1,6-dihydroxy-5-[N-[(4-methoxyphenyl)methoxy]ethanimidoyl]-4-methylpyridin-2(1H)-one
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5-[N-(4-fluorophenoxy)ethanimidoyl]-1,6-dihydroxy-4-methylpyridin-2(1H)-one
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5-[N-(4-fluorophenoxy)ethanimidoyl]-1,6-dihydroxy-4-methylpyridin-2(1H)-one
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5-[N-[(2-aminophenyl)methoxy]ethanimidoyl]-1,6-dihydroxy-4-methylpyridin-2(1H)-one
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5-[N-[(2-aminophenyl)methoxy]ethanimidoyl]-1,6-dihydroxy-4-methylpyridin-2(1H)-one
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5-[N-[(2-fluorophenyl)methoxy]ethanimidoyl]-1,6-dihydroxy-4-methylpyridin-2(1H)-one
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5-[N-[(2-fluorophenyl)methoxy]ethanimidoyl]-1,6-dihydroxy-4-methylpyridin-2(1H)-one
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5-[N-[(4-fluorophenyl)methoxy]ethanimidoyl]-1,6-dihydroxy-4-methylpyridin-2(1H)-one
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5-[N-[(4-fluorophenyl)methoxy]ethanimidoyl]-1,6-dihydroxy-4-methylpyridin-2(1H)-one
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alpha-thujaplicin
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i.e. 2-hydroxy-3-(1-methylethyl)-2,4,6-cycloheptatrien-1-one, slight inhibition
alpha-thujaplicin
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i.e. 2-hydroxy-3-(1-methylethyl)-2,4,6-cycloheptatrien-1-one
beta-thujaplicin
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i.e. 2-hydroxy-4-(1-methylethyl)-2,4,6-cycloheptatrien-1-one, slight inhibition
beta-thujaplicinol
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i.e. 2,7-dihydroxy-4-(1-methylethyl)-2,4,6-cycloheptatrien-1-one
beta-thujaplicinol
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i.e. 2,7-dihydroxy-4-(1-methylethyl)-2,4,6-cycloheptatrien-1-one
Ca2+
calcium ions generally inactivate the enzyme and abolish catalysis
Ca2+
Halalkalibacterium halodurans
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Ca2+ substitution of either of the two active-site Mg2+ ions substantially increases the height of the reaction barrier and thereby abolishes the catalytic activity
Ca2+
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calcium ions generally inactivate the enzyme and abolish catalysis
Dextran
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inhibits degradation of poly(rA)*poly(dT), no inhibition of degradation by phi174DNA-RNA. Dextran does not interfere with the recognition site, but rather blocks hydrolysis
ethyl 6-hydroxy-2-methoxy-5,7-dioxo-5,6,7,8-tetrahydro-1,6-naphthyridine-8-carboxylate
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ethyl 6-hydroxy-2-methoxy-5,7-dioxo-5,6,7,8-tetrahydro-1,6-naphthyridine-8-carboxylate
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gamma-thujaplicin
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i.e. 2-hydroxy-5-(1-methylethyl)-2,4,6-cycloheptatrien-1-one, slight inhibition
gamma-thujaplicin
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i.e. 2-hydroxy-5-(1-methylethyl)-2,4,6-cycloheptatrien-1-one
KCl
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activity of enzyme form H1 decreases rapidly above 50 mM and becomes nearly abolished at 150 mM
manicol
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i.e. 1,2,3,4-tetrahydro-2,7-dihydroxy-9-methyl-2-(1-methylethyl)-6H-benzocyclohepten-6-one
manicol
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i.e. 1,2,3,4-tetrahydro-2,7-dihydroxy-9-methyl-2-(1-methylethyl)-6H-benzocyclohepten-6-one
Mn2+
wild-type enzyme, above 0.1 mM, activating below, activating metal ion binding site is site 1, inhibitory binding site is site 2
Mn2+
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Mn2+ inhibition of in vitro reverse transcriptase activity is greatly reduced in all the suppressor mutants, whereas RNAse H activity and cleavage specificity remain largely unchanged
Mn2+
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the activity of wild-type protein is stimulated by Mn2+, whereas this cation significantly inhibits the activity of C-terminal truncated mutant proteins
Mn2+
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can substitute for Mg2+, activates N-terminally truncated mutant RNHIDELTA47 and inhibits the full length enzyme dependent on the presence of the N-terminal 47 amino acids
NaCl
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activity of enzyme form H1 decreases rapidly above 50 mM and becomes nearly abolished at 150 mM
NEM
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the Mg2+-dependent activity is inhibited by 60% at 20 mM. The Mn2+-dependent activity is unaffected
NEM
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2 mM, 80% inhibition of Mn2+-dependent enzyme, complete inhibition of Mg2+-dependent enzyme
NEM
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Mn2+-dependent activity is moderately sensitive, even at high concentrations
nootkatin
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i.e. 2-hydroxy-5-(3-methyl-2-butenyl)-4-(1-methylethyl)-2,4,6-cycloheptatrien-1-one, slight inhibition
nootkatin
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i.e. 2-hydroxy-5-(3-methyl-2-butenyl)-4-(1-methylethyl)-2,4,6-cycloheptatrien-1-one
PCMB
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2 mM, complete inhibition of Mn2+-dependent enzyme and Mg2+-dependent enzyme
PCMB
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in absence of 2-mercaptoethanol, isoenzyme I and III are completely inhibited by 0.2 mM PCMB, Activity of isoenzyme II is inhibited 20%
additional information
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selectivity of tropolone derivatives for RNase H, IC50 values, inhibition mechanism, overview
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additional information
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inhibition of hepatitis B virus (HBV) replication by alpha-tropolone, N-hydroxyisoquinolinedione, and N-hydroxypyridinedione ribonuclease H inhibitors. Three compound classes, the alpha-hydroxytropolones, N-hydroxyisoquinolinediones, and N-hydroxypyridinediones are found by inhibitor screening, that suppress viral replication in cells by blocking the HBV RNaseH. These compounds preferentially suppress the plus-polarity DNA strands, induce truncation of the minus-polarity DNA strands, and cause accumulation of extensive RNA:DNA heteroduplexes in capsids as expected from their inhibition of the RNaseH. Seven N-hydroxyisoquinolinediones inhibit HBV replication, but the therapeutic indexes does not improve over what was reported. All nine of the N-hydroxypyridinedioness inhibit HBV replication. The N-hydroxypyridinedione compound class holds potential for antiviral discovery. No inhibition by 7-benzamido-N,N-diethyl-2-hydroxy-1,3-dioxo-1,2,3,4-tetrahydroisoquinoline-4-carboxamide and methyl 7-benzamido-2-hydroxy-1,3-dioxo-1,2,3,4-tetrahydroisoquinoline-4-carboxylate. Determination of cellular toxicity and EC50 values for HBV replication inhibition in presence of DNA for the inhibitor compounds, overview. Comparison with effects on the human enzyme
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additional information
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presence of intrinsic cell-type specific factors affecting the activity and localization of type 2 enzyme
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additional information
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selectivity of tropolone derivatives for RNase H, IC50 values, inhibition mechanism, overview
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additional information
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chimeric substrates containing 2'-methoxyethyl nucleotides inhibit human RNase H1 activity
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additional information
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drug design and synthesis by 2',4'-propylene-bridged thymidine, and five 8'-Me/NH2/OH variants thereof, introduction into 15mer oligodeoxynucleotides, the compounds inhibit the enzyme by formation of stable complexes with RNA, inhibitory effect of the variants, overview
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additional information
for screening of inhibitors, a label-free chemiluminescent (CL) aptasensor for the sensitive detection of RNase H activity based on hairpin technology is used, overview
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additional information
alpha-tropolone, N-hydroxyisoquinolinedione, and N-hydroxypyridinedione ribonuclease H inhibitors are tested against human RNase H compared to hepatitis B virus RNase H. Replication inhibition efficacy and cytotoxicity, overview. No or poor inhibition by 7-benzamido-N,N-diethyl-2-hydroxy-1,3-dioxo-1,2,3,4-tetrahydroisoquinoline-4-carboxamide, 1,6-dihydroxy-4-methyl-5-[N-[(4-methylphenyl)methoxy]ethanimidoyl]pyridin-2(1H)-one, N-(4-fluorophenyl)-6-hydroxy-2-methoxy-5,7-dioxo-5,6,7,8-tetrahydro-1,6-naphthyridine-8-carboxamide, N-[(4-fluorophenyl)methyl]-2,6-dihydroxy-5,7-dioxo-5,6,7,8-tetrahydro-1,6-naphthyridine-8-carboxamide, and N-(4-chlorophenyl)-6-hydroxy-2-methoxy-5,7-dioxo-5,6,7,8-tetrahydro-1,6-naphthyridine-8-carboxamide
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additional information
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alpha-tropolone, N-hydroxyisoquinolinedione, and N-hydroxypyridinedione ribonuclease H inhibitors are tested against human RNase H compared to hepatitis B virus RNase H. Replication inhibition efficacy and cytotoxicity, overview. No or poor inhibition by 7-benzamido-N,N-diethyl-2-hydroxy-1,3-dioxo-1,2,3,4-tetrahydroisoquinoline-4-carboxamide, 1,6-dihydroxy-4-methyl-5-[N-[(4-methylphenyl)methoxy]ethanimidoyl]pyridin-2(1H)-one, N-(4-fluorophenyl)-6-hydroxy-2-methoxy-5,7-dioxo-5,6,7,8-tetrahydro-1,6-naphthyridine-8-carboxamide, N-[(4-fluorophenyl)methyl]-2,6-dihydroxy-5,7-dioxo-5,6,7,8-tetrahydro-1,6-naphthyridine-8-carboxamide, and N-(4-chlorophenyl)-6-hydroxy-2-methoxy-5,7-dioxo-5,6,7,8-tetrahydro-1,6-naphthyridine-8-carboxamide
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additional information
5'-boronic acid modified oligonucleotides (ORNs) hybridized to a RNA target sequence convert RNase H into an inactivated enzyme complex. The dynamic formation of a boronate ester upon addition of a diol moiety disrupts the enzyme-inhibitor complex and reactivates RNase H. Reactivation of RNase H function can also be engineered through short RNA trimers inputs that fashion RNase H from a non-specific DNA-guided enzyme into an informational and programmable RNA-guided one. Programmable RNA recognition and cleavage, method, overview
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additional information
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a 5' RNA flap Okazaki fragment intermediate impairs PabRNase HII endonuclease activity. Introduction of mismatches into the RNA portion near the RNA-DNA junction decreases both the specificity and the efficiency of cleavage by PabRNase HII
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