3.1.13.2: exoribonuclease H
This is an abbreviated version!
For detailed information about exoribonuclease H, go to the full flat file.
Word Map on EC 3.1.13.2
-
3.1.13.2
-
strand
-
duplex
-
nucleic
-
rna-dna
-
single-stranded
-
integrase
-
r-loops
-
oligodeoxynucleotides
-
retrotransposons
-
heteroduplexes
-
transcriptases
-
phosphorothioate
-
retroviruses
-
polypurine
-
moloney
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phosphodiester
-
exonuclease
-
rna-dependent
-
pre-mrnas
-
nucleases
-
oligodeoxyribonucleotides
-
plus-strand
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nnrti
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template-primer
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nucleocapsids
-
minus-strand
-
dntp
-
spliceosome
-
myeloblastosis
-
thumb
-
endonucleolytic
-
oligonucleotide-directed
-
2'-o-methylated
-
nevirapine
-
snrnp
-
oligoribonucleotide
-
primer-template
-
okazaki
-
nonnucleoside
-
rna-directed
-
a-form
-
efavirenz
-
retroelements
-
3'-exonuclease
-
heteropolymeric
-
phosphoramidite
-
pregenomic
-
hepadnavirus
-
hiv-rt
-
pharmacology
-
medicine
-
drug development
-
internucleotide
- 3.1.13.2
- strand
- duplex
- nucleic
- rna-dna
-
single-stranded
-
integrase
-
r-loops
- oligodeoxynucleotides
-
retrotransposons
- heteroduplexes
- transcriptases
- phosphorothioate
- retroviruses
-
polypurine
-
moloney
-
phosphodiester
-
exonuclease
-
rna-dependent
- pre-mrnas
- nucleases
- oligodeoxyribonucleotides
-
plus-strand
-
nnrti
-
template-primer
-
nucleocapsids
-
minus-strand
- dntp
-
spliceosome
-
myeloblastosis
-
thumb
-
endonucleolytic
-
oligonucleotide-directed
-
2'-o-methylated
- nevirapine
-
snrnp
- oligoribonucleotide
-
primer-template
-
okazaki
-
nonnucleoside
-
rna-directed
-
a-form
- efavirenz
-
retroelements
- 3'-exonuclease
-
heteropolymeric
-
phosphoramidite
-
pregenomic
-
hepadnavirus
- hiv-rt
- pharmacology
- medicine
- drug development
-
internucleotide
Reaction
3'-end directed exonucleolytic cleavage of viral RNA-DNA hybrid =
Synonyms
3'-to-5' RNase H, HIV RNase H, HIV-1 ribonuclease H, HIV-1 RT ribonuclease H, LC11-RNase H1, More, Prp8, retroviral reverse transcriptase RNaseH, retroviral RNase H, reverse transcriptase ribonuclease H, reverse transcriptase-associated ribonuclease H, ribonuclease H, RNase H, RNase H1, RNase HI, RNaseH, RNH, RNH1, RT RNase H, RT/RNase H, T4 RNase H, Ta11
ECTree
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Inhibitors
Inhibitors on EC 3.1.13.2 - exoribonuclease H
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(10,12,15,16-tetrahydroxy-8-methoxy-11-methyl-1,9,14-trioxo-6,7,9,14-tetrahydrotetraceno[1,2-g]phthalazin-2(1H)-yl)acetic acid
-
-
(2E)-2-[(4-chlorophenyl)hydrazono]propanoic acid
-
4-chlorophenylhydrazone of pyruvic acid, shows poor inhibitory activity against HIV-1 RNase H because of the storage of one or two carboxylic acid moieties
(E)-3,4-dihydroxy-N'-((2-methoxynaphthalen-1-yl)methylene)benzohydrazide
i.e. DHBNH, highly specific, noncompetitive, binding site analysis, the inhibitor binds near both the polymerase active site and the non-nucleoside reverse transcriptase inhibitor binding pocket, it specifically interacts with conserved residues Asp186 and Trp229 and has substantial interactions with the backbones of several less well-conserved residues, overview, substituted inhibitor derivatives, that interact with the nucleoside analog RT inhibitor-binding pocket, inhibit both the polymerase and RNH activities of reverse transcriptase, DHBNH interacts with other residues, including Val108, Leu187, Tyr188, Lys223, Phe227, and Leu228
1,6-dihydroxy-4-methyl-5-[N-[(4-methylphenyl)methoxy]ethanimidoyl]pyridin-2(1H)-one
-
-
1,6-dihydroxy-5-[N-[(2-methoxyphenyl)methoxy]ethanimidoyl]-4-methylpyridin-2(1H)-one
-
-
1,6-dihydroxy-5-[N-[(4-methoxyphenyl)methoxy]ethanimidoyl]-4-methylpyridin-2(1H)-one
-
-
1,9,11,14-tetrahydroxy-3-[(E)-{[(2-hydroxyphenyl)carbonyl]hydrazono}methyl]-7-methoxy-10-methyl-8,13-dioxo-5,6,8,13-tetrahydrobenzo[a]tetracene-2-carboxylic acid
-
-
1,9,11,14-tetrahydroxy-7-methoxy-10-methyl-3-[(E)-{[(4-methylphenyl)sulfonyl]hydrazono}methyl]-8,13-dioxo-5,6,8,13-tetrahydrobenzo[a]tetracene-2-carboxylic acid
-
-
1,9,11,14-tetrahydroxy-7-methoxy-10-methyl-3-{(E)-[(4-nitrophenyl)hydrazono]methyl}-8,13-dioxo-5,6,8,13-tetrahydrobenzo[a]tetracene-2-carboxylic acid
-
-
1,9,11,14-tetrahydroxy-7-methoxy-10-methyl-8,13-dioxo-3-(1,2,3,4-tetrahydroquinazolin-2-yl)-5,6,8,13-tetrahydrobenzo[a]tetracene-2-carboxylic acid
-
-
1,9,11,14-tetrahydroxy-7-methoxy-10-methyl-8,13-dioxo-3-[(E)-(tetracyclo[5.3.1.03,9.05,9]undec-1-ylimino)methyl]-5,6,8,13-tetrahydrobenzo[a]tetracene-2-carboxylic acid
-
-
1,9,11,14-tetrahydroxy-7-methoxy-10-methyl-8,13-dioxo-3-{(E)-[(phenylcarbonyl)hydrazono]methyl}-5,6,8,13-tetrahydrobenzo[a]tetracene-2-carboxylic acid
-
-
1,9,11,14-tetrahydroxy-7-methoxy-10-methyl-8,13-dioxo-5,6,8,13-tetrahydrobenzo[a]tetracene-2,3-dicarboxylic acid
-
-
1,9,11,14-tetrahydroxy-7-methoxy-3-[(E)-(methoxyimino)methyl]-10-methyl-8,13-dioxo-5,6,8,13-tetrahydrobenzo[a]tetracene-2-carboxylic acid
-
-
1-(4-chlorophenyl)-2-(1-methylethylidene)hydrazine
-
4-chlorophenylhydrazone of acetone, shows poor inhibitory activity against HIV-1 RNase H because of the storage of one or two carboxylic acid moieties
10,12,15,16-tetrahydroxy-8-methoxy-11-methyl-1,9,14-trioxo-6,7,9,14-tetrahydrotetraceno[1,2-g]phthalazine-2(1H)-carboximidamide
-
-
10,12,15,16-tetrahydroxy-8-methoxy-11-methyl-2,3,4,4a,6,7-hexahydropyrimido[2,1-a]tetraceno[1,2-f]isoindole-9,14,17(1H)-trione
-
-
10,12,15,16-tetrahydroxy-8-methoxy-11-methyl-2-phenyl-6,7-dihydrotetraceno[1,2-g]phthalazine-1,9,14(2H)-trione
-
-
10,12,15,16-tetrahydroxy-8-methoxy-11-methyl-2-propyl-6,7-dihydrotetraceno[1,2-g]phthalazine-1,9,14(2H)-trione
-
-
10,12,15,16-tetrahydroxy-8-methoxy-11-methyl-6,7-dihydrotetraceno[1,2-g]phthalazine-1,9,14(2H)-trione
-
-
12,14,17,18-tetrahydroxy-10-methoxy-13-methyl-6,6a,8,9-tetrahydrotetraceno[1',2':5,6]isoindolo[2,1-a]quinazoline-11,16,19(5H)-trione
-
-
15,16-dihydroxy-8-methoxy-12-[(methoxycarbonyl)oxy]-11-methyl-1,9,14-trioxo-2-propyl-1,2,6,7,9,14-hexahydrotetraceno[1,2-g]phthalazin-10-yl acetate
-
-
2,4,17,18-tetrahydroxy-6-methoxy-3-methyl-7,9b-dihydrotetraceno[1',2':5,6]isoindolo[1,2-b][1,3]benzothiazole-5,16,19(8H)-trione
-
-
2-(10,12,15,16-tetrahydroxy-8-methoxy-11-methyl-1,9,14-trioxo-6,7,9,14-tetrahydrotetraceno[1,2-g]phthalazin-2(1H)-yl)ethyl acetate
-
-
2-(4-fluorophenyl)-N-(2-hydroxy-1,3-dioxo-1,2,3,4-tetrahydroisoquinolin-7-yl)acetamide
-
-
2-amino-12-ethyl-7-(1-hydroxypropyl)-8-methylindolizino[1,2-b]quinolin-9(11H)-one
-
mappicine analogue
2-chloro-7-(2-cyclohexyl-1-hydroxyethyl)-8-methyl-12-propylindolizino[1,2-b]quinolin-9(11H)-one
-
mappicine analogue
2-hydroxy-4H-isoquinoline-1,3-dione
-
specific inhibition of isolated RNase H domain and of the full length reverse transcriptase, IC50 value for the isolated RNase H domain is 0.00043 mM
2-hydroxy-6-pentadecylbenzoic acid
-
isolated from the CH2Cl2 extracts of the sacrotestas of Ginkgo biloba
2-hydroxy-6-[(8Z)-pentadec-8-en-1-yl]benzoic acid
-
isolated from the CH2Cl2 extracts of the sacrotestas of Ginkgo biloba
2-hydroxy-7-(4-hydroxyphenyl)isoquinoline-1,3(2H,4H)-dione
-
-
2-hydroxy-7-[4-(trifluoromethyl)phenyl]isoquinoline-1,3(2H,4H)-dione
-
-
2-[(10Z)-heptadec-10-en-1-yl]-6-hydroxybenzoic acid
-
isolated from the CH2Cl2 extracts of the sacrotestas of Ginkgo biloba
3'-azido-3'-deoxythymidine 5'-(dihydrogen phosphate)
-
inhibits RNase H in vitro, but is not selectively active against RNase H. Does not exhibit inhibitory activity against RNase H in the HIV-1 replication process
3'-azido-3'-deoxythymidine 5'-phosphate
-
more sensitive to inhibition with poly(rGdC) than with poly(rAdT) as substrate. Competitive inhibitor with respect to substrate in Mn2+, uncompetitive inhibitor in Mg2+
3,4-dihydroxy-N'-[(E)-(2-methoxynaphthalen-1-yl)methylidene]benzohydrazide
-
specific inhibitor of reverse transcriptase RNase H activity (IC50 value is about 0.5 microM) and has relatively limited activity against the DNA polymerase activity of reverse transcriptase. It is non-cytotoxic and inhibits the replication of a variety of drug-resistant HIV-1 reverse transcriptase mutants
3,9,11,14,15-pentahydroxy-7-methoxy-N,N,N,10-tetramethyl-1,8,13-trioxo-1,3,5,6,8,13-hexahydro-2H-tetraceno[1,2-f]isoindol-2-aminium
-
-
3-pentadecylphenol
-
isolated from the CH2Cl2 extracts of the sacrotestas of Ginkgo biloba
3-tridecylphenol
-
isolated from the CH2Cl2 extracts of the sacrotestas of Ginkgo biloba
3-[(10Z)-heptadec-10-en-1-yl]phenol
-
isolated from the CH2Cl2 extracts of the sacrotestas of Ginkgo biloba
3-[(8Z)-pentadec-8-en-1-yl]phenol
-
isolated from the CH2Cl2 extracts of the sacrotestas of Ginkgo biloba
3-[(E)-(carbamimidoylhydrazono)methyl]-1,9,11,14-tetrahydroxy-7-methoxy-10-methyl-8,13-dioxo-5,6,8,13-tetrahydrobenzo[a]tetracene-2-carboxylic acid
-
-
3-[(E)-(tert-butylhydrazono)methyl]-1,9,11,14-tetrahydroxy-7-methoxy-10-methyl-8,13-dioxo-5,6,8,13-tetrahydrobenzo[a]tetracene-2-carboxylic acid
-
-
3-[(E)-[4-[(E)-2-carboxyethenyl]phenyl]diazenyl]-7-[([6-[(E)-[4-[(E)-2-carboxyethenyl]phenyl]diazenyl]-5-hydroxy-7-sulfonatonaphthalen-2-yl]carbamoyl)amino]-4-hydroxynaphthalene-2-sulfonate
-
-
4'-chloro-N'-[(1E)-(2-methoxynaphthalen-1-yl)methylidene]biphenyl-4-carbohydrazide
-
4-(1-chloro-1,1-difluoromethyl)-4-(2-phenylethynyl)-6-chloro-2H-3,1-benzoxazin-2-one
-
i.e. NNRTI, an efavirenz analogue, IC50 values for wild-type enzyme are 0.000002-0.000005 mM with substrates DNA-17-nucleotide-RNA hybrid or DNA-18-nucleotide-RNA hybrid, and 0.001 mm for substrate DNA-15-nucleotide-RNA hybrid or DNA-16-nucleotide-RNA hybrid, effect on mutant enzymes, overview
4-(10,12,15,16-tetrahydroxy-8-methoxy-11-methyl-1,9,14-trioxo-6,7,9,14-tetrahydrotetraceno[1,2-g]phthalazin-2(1H)-yl)benzoic acid
-
-
4-(5-benzamidothiophen-2-yl)-2,4-dioxobutanoic acid
-
IC50 values determined by two different assay variants
4-(dimethylamino)-N'-[(1E)-(2-methoxynaphthalen-1-yl)methylidene]benzohydrazide
-
4-methoxy-N'-[(1E)-(2-methoxynaphthalen-1-yl)methylidene]benzohydrazide
-
4-tert-butyl-N'-[(1E)-(2-methoxynaphthalen-1-yl)methylidene]benzohydrazide
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4-[1-(4-fluorobenzyl)-1H-pyrrol-2-yl]-2,4-dioxobutanoic acid
-
L-731,988
4-[5-(benzoylamino)thien-2-yl]-2,4-dioxobutanoic acid
-
a diketo acid RNase H inhibitor, IC50 values for wild-type and mutant enzymes are 0.002-0.0035 mM with all substrates, effect on mutant enzymes, overview
4-[5-(benzoylamino)tien-2-yl]-2,4-dioxobutanoic acid
-
diketo acid derivative
4-[5-benzoylamino) thien-2-yl]-2,4-dioxobutanoic acid
-
inhibits RNase H by binding to the active site and chelating the essential Mg2+
5-chloro-2-hydroxyisoquinoline-1,3(2H,4H-dione)
-
is not candidate therapeutics because it is cytotoxic
5-nitrofuran-2-carboxylic acid [[4-(4-bromophenyl)-thiazol-2-yl]-(tetrahydro-furan-2-yl-methyl)-carbamoyl] methyl ester
20-25 microM effectively inhibited HIV-1 replication
5-nitrofuran-2-carboxylic acid [[4-(4-bromophenyl)-thiazol-2-yl]-(tetrahydrofuran-2-ylmethyl)-carbamoyl] methyl ester
-
derivative of 5-nitrofuran-2-carboxylic acid carbamoyl methyl ester. 20-25 microM effectively inhibited HIV-1 replication
5-tridecylbenzene-1,3-diol
-
isolated from the CH2Cl2 extracts of the sacrotestas of Ginkgo biloba
5-[(8Z)-pentadec-8-en-1-yl]benzene-1,3-diol
-
isolated from the CH2Cl2 extracts of the sacrotestas of Ginkgo biloba
5-[N-(4-fluorophenoxy)ethanimidoyl]-1,6-dihydroxy-4-methylpyridin-2(1H)-one
-
-
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-[(4-fluorophenyl)methoxy]ethanimidoyl]-1,6-dihydroxy-4-methylpyridin-2(1H)-one
-
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7-(3,4-dihydroxyphenyl)-2-hydroxyisoquinoline-1,3(2H,4H)-dione
-
-
7-benzamido-N,N-diethyl-2-hydroxy-1,3-dioxo-1,2,3,4-tetrahydroisoquinoline-4-carboxamide
-
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8-methoxy-11-methyl-1,9,14-trioxo-2-phenyl-1,2,6,7,9,14-hexahydrotetraceno[1,2-g]phthalazine-10,12,15,16-tetrayl tetraacetate
-
-
8-methoxy-11-methyl-1,9,14-trioxo-2-propyl-1,2,6,7,9,14-hexahydrotetraceno[1,2-g]phthalazine-10,12,15,16-tetrayl tetraacetate
-
-
9,11,14,15-tetrahydroxy-7-methoxy-10-methyl-8,13,16-trioxo-1,2,3a,5,6,8,13,16-octahydrotetraceno[1,2-f][1,3]thiazolo[2,3-a]isoindole-1-carboxylic acid
-
-
BPH218
-
potent inhibitor of ATP-mediated phosphorolytic excision of 3'-terminal zidovudine 5'-monophosphate (in vitro IC50 value is about 2 microM)
capravirine
-
a nonnucleoside reverse transcriptase inhibitor, inhibits the 5' to 3' directed RNase H activity
Cl-
-
the wild-type and mutant enzymes bind the substrate considerably less tightly at higher concentrations
Dextran sulfate
-
inhibits RNase H in vitro, but is not selectively active against RNase H. Does not exhibit inhibitory activity against RNase H in the HIV-1 replication process
-
dihydroxy benzoyl naphthyl hydrazone
-
also have inhibitory activity against drug-resistant HIV-1 RT variants Y181C RT and Y188l RT. NNRTI Efavirenz shows no inhibitory effect under the same conditions
ethyl (5E)-6-[1-(4-fluorobenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoate
-
RDS 1643, good selectivity and high potency in enzyme and cell culture assay
ethyl 3-(10,12,15,16-tetrahydroxy-8-methoxy-11-methyl-1,9,14-trioxo-6,7,9,14-tetrahydrotetraceno[1,2-g]phthalazin-2(1H)-yl)propanoate
-
-
ethyl 6-hydroxy-2-methoxy-5,7-dioxo-5,6,7,8-tetrahydro-1,6-naphthyridine-8-carboxylate
-
-
GW8248
-
a nonnucleoside reverse transcriptase inhibitor, inhibits the 5' to 3' directed RNase H activity
heparin
-
inhibits RNase H in vitro, but is not selectively active against RNase H. Does not exhibit inhibitory activity against RNase H in the HIV-1 replication process
hyemaloside A
-
isolated from the evergreen tree Eugenia hyemalis
hyemaloside B
-
isolated from the evergreen tree Eugenia hyemalis
hyemaloside C
-
isolated from the evergreen tree Eugenia hyemalis
madurahydroxylactone
-
a secondary metabolite from the soil bacterium Nonomuraea rubra, belonging to the family of benzo[a]naphthacenequinone antibiotics
methyl 10,15,16-trihydroxy-8-methoxy-11-methyl-1,9,14-trioxo-2-phenyl-1,2,6,7,9,14-hexahydrotetraceno[1,2-g]phthalazin-12-yl carbonate
-
-
methyl 7-benzamido-2-hydroxy-1,3-dioxo-1,2,3,4-tetrahydroisoquinoline-4-carboxylate
-
-
N'-[(1E)-(2-methoxynaphthalen-1-yl)methylidene]-4-methylbenzohydrazide
-
N'-[(1E)-(2-methoxynaphthalen-1-yl)methylidene]-4-phenoxybenzohydrazide
-
N'-[(1E)-(2-methoxynaphthalen-1-yl)methylidene]benzohydrazide
-
N'-[(1E)-(2-methoxynaphthalen-1-yl)methylidene]biphenyl-4-carbohydrazide
-
N-(2-hydroxy-1,3-dioxo-1,2,3,4-tetrahydroisoquinolin-7-yl)-2-phenylacetamide
-
-
N-(2-hydroxy-1,3-dioxo-1,2,3,4-tetrahydroisoquinolin-7-yl)-3-nitrobenzamide
-
-
N-(2-hydroxy-1,3-dioxo-1,2,3,4-tetrahydroisoquinolin-7-yl)-4-fluorobenzamide
-
-
N-(2-hydroxy-1,3-dioxo-1,2,3,4-tetrahydroisoquinolin-7-yl)acetamide
-
-
N-(2-hydroxy-1,3-dioxo-1,2,3,4-tetrahydroisoquinolin-7-yl)benzamide
-
-
N-(2-hydroxy-1,3-dioxo-1,2,3,4-tetrahydroisoquinolin-7-yl)pentanamide
-
-
N-(4-chlorophenyl)-6-hydroxy-2-methoxy-5,7-dioxo-5,6,7,8-tetrahydro-1,6-naphthyridine-8-carboxamide
-
-
N-(4-fluorophenyl)-6-hydroxy-2-methoxy-5,7-dioxo-5,6,7,8-tetrahydro-1,6-naphthyridine-8-carboxamide
-
-
N-(4-tert-butylbenzoyl)-2-hydroxynaphthaldehyde hydrazone
BBNH, the residue Tyr501 is integral in the binding interaction, mechanism
N-[(4-fluorophenyl)methyl]-2,6-dihydroxy-5,7-dioxo-5,6,7,8-tetrahydro-1,6-naphthyridine-8-carboxamide
-
-
nootkatin
-
i.e. 2-hydroxy-5-(3-methyl-2-butenyl)-4-(1-methylethyl)-2,4,6-cycloheptatrien-1-one
Phosphonoformate
-
the inhibitor that bind in the reverse transcriptase polymerase domain inhibits also RNase H activity, IC value for the wild-type enzyme is 0.0015 mM versus substrate DNA-18-nucleotide-RNA hybrid, with the other substrates the IC50 value is above 0.025 mM
Phosphonoformic acid
-
inhibits both the polymerase and the RNase H activities
RNA-DNA duplex with bound drugs
-
two chimeric RNA-DNA duplexes mimicking intermediates of the reverse trancriptase reaction with bound 4,5-disubstituted 2-deoxystreptamine aminoglycosides, i.e. neomycin, paromomycin, and ribostamycin, inhibit specifically and competitively the RNase H cleavage reaction by 60-95% and 15-91%, respectively, overview
-
tert-butyl [7-(1-hydroxypropyl)-8-methyl-9-oxo-12-(trimethylsilyl)-9,11-dihydroindolizino[1,2-b]quinolin-2-yl]carbamate
-
mappicine analogue
TMC-125
-
a nonnucleoside reverse transcriptase inhibitor, inhibits the 5' to 3' directed RNase H activity
[(4-chlorophenyl) hydrazono] propanedioic acid
-
inhibits the RNase H of HIV-1 reverse transcriptase with potency similar to that of N-(4-tert-butylbenzoyl)-2-hydroxy-1-naphthaldehyde hydrazone. It is specific for RNase H and does not inhibit the DNA polymerase activity of reverse transcriptase. Inhibits RNase H by binding to the active site and chelating the essential Mg2+
[(4-chlorophenyl)hydrazono]propanedioic acid
-
inhibits by directly chelating Mg2+
[10,12,15,16-tetrakis(cyclohexyloxy)-8-methoxy-11-methyl-1,9,14-trioxo-6,7,9,14-tetrahydrotetraceno[1,2-g]phthalazin-2(1H)-yl]acetic acid
-
-
-
isolated from the aqueous extract of leaves of the plant Hylodendron gabunensis
1,3,4,5-tetragalloylapiitol
-
extracted from the plant Hylodendron gabunense, also inhibitory effective against HIV-2 RNase H
1,3,4,5-tetragalloylapiitol
-
isolated from the aqueous extract of leaves of the plant Hylodendron gabunensis
-
2,7-dihydroxy-4-1(methylethyl)-2,4,6-cycloheptatrien-1-one, or beta-thujaplicinol, is not candidate therapeutics because it is cytotoxic
2,7-dihydroxy-4-isopropylcyclohepta-2,4,6-trienone
-
beta-thujaplicinol, tropolone derivative. Inhibitory activity against both HIV-1 RNase H and Escherichia coli RNase H at a concentration of 0.2 microM and 50 microM respectively
-
NSC727447
2-amino-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
-
NSC727447
-
IC50 values determined by two different assay variants
2-hydroxyisoquinoline-1,3(2H,4H)-dione
-
best inhibitor with high selectivity and activity
3'-azido-3'-deoxythymidine
a nucleoside analog RT inhibitor
3'-azido-3'-deoxythymidine
a nucleoside analog RT inhibitor
-
potent inhibitor
4-[(4'-aminomethyl-1,1'-biphenyl)methyl]-1-hydroxy-1,8-naphthyridin-2-one
-
potent inhibitor
4-[(4'-aminomethyl-1,1'-biphenyl)methyl]-1-hydroxy-1,8-naphthyridin-2-one
potent inhibitor
-
5-nitrofuran-2-carboxylic acid adamantan-1-carbamoyl methyl ester
-
derivative of 5-nitrofuran-2-carboxylic acid carbamoyl methyl ester
7-(furan-2-yl)-2-hydroxy-isoquinoline-1,3(2H,4H)-dione
-
-
i.e. 2-hydroxy-3-(1-methylethyl)-2,4,6-cycloheptatrien-1-one
-
a Ardisia japonica dimeric lactone, structure determination by NMR spectrometry
ardimerin digallate
-
a Ardisia japonica dimeric lactone, structure determination by NMR spectrometry
-
i.e. 2-hydroxy-4-(1-methylethyl)-2,4,6-cycloheptatrien-1-one
-
i.e. 2,7-dihydroxy-4-(1-methylethyl)-2,4,6-cycloheptatrien-1-one
beta-thujaplicinol
able to inhibit RNase H in the presence of 200 nM HTS-1 RNA-DNA substrate. However, beta-thujaplicinol is not able to inhibit RNase H as the concentration of RNA-DNA substrate is increased
-
a nonnucleoside reverse transcriptase inhibitor, inhibits the 5' to 3' directed RNase H activity
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i.e. 2-hydroxy-5-(1-methylethyl)-2,4,6-cycloheptatrien-1-one
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inhibits RNase H in vitro, but is not selectively active against RNase H. Does not exhibit inhibitory activity against RNase H in the HIV-1 replication process
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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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tropolone derivative. Inhibitory activity against both HIV-1 RNase H and Escherichia coli RNase H at a concentration of 1.5 microM and 40 microM respectively
i.e. BBNH, highly specific, a substituted inhibitor derivative, that interacts with the nucleoside analog RT inhibitor-binding pocket, and inhibits both the polymerase and RNH activities of reverse transcriptase
N-(4-tert-butylbenzoyl)-2-hydroxy-1-naphthaldehyde hydrazone
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reasonable potency. Bifunctional inhibitor of HIV-1 reverse transcriptase, it inhibits both the reverse transcriptase DNA polymerase and RNase H activities of the enzyme with similar potency (IC50 is about 3 microM)
N-(4-tert-butylbenzoyl)-2-hydroxy-1-naphthaldehyde hydrazone
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phenylhydrazone derivative. Inhibits RNase H in vitro, but is not selectively active against RNase H. Exhibits inhibitory activity against RNase H in the HIV-1 replication process
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NSC727448
N-[3-(aminocarbonyl)-4,5-dimethyl-2-thienyl]-2-furancarboxamide
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NSC727448
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a nonnucleoside reverse transcriptase inhibitor, inhibits the 5' to 3' directed RNase H activity
i.e. NNRTIs, the association of an NNRTI with reverse transcriptase not only forms the NNRTI pocket, but also alters the relative positions of the RNase H and polymerase domains
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non-nucleoside reverse transcriptase inhibitors
i.e. NNRTIs
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NNRTI, non-competitive inhibitor that binds a hydrophobic pocket near the polymerase active site of the p66 subunit in HIV-1 reverse transcriptase
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non-nucleotide or non-nucleoside reverse transcriptase inhibitor
targets the DNA polymerasec activity of reverse transcriptase. Non-competitive inhibitor that binds a hydrophobic pocket near the polymerase active site of the p66 subunit in HIV-1 reverse transcriptase
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i.e. NRTIs, nucleoside analog RT inhibitors are non-competitive inhibitors that bind a hydrophobic pocket near the polymerase active site of the p66 subunit in HIV-1 reverse transcriptase
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nucleoside analog RT inhibitors
i.e. NRTIs, nucleoside analog RT inhibitors are non-competitive inhibitors
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NRTIs inhibit replication by competing with cellular dNTPs for incorporation into the nascent DNAchain; upon incorporation, the absence of a 3' hydroxyl group on the NRTI prevents additional synthesis and causes premature chain termination
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nucleotide or nucleoside reverse transcriptase inhibitor
targets the DNA polymerasec activity of reverse transcriptase. NRTIs inhibit replication by competing with cellular dNTPs for incorporation into the nascent DNAchain; upon incorporation, the absence of a 3' hydroxyl group on the NRTI prevents additional synthesis and causes premature chain termination
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inhibits viral RT polymerase and RNase H functions, pre-steady-state and order-of-addition kinetic analyses, ssDNA aptamer competes with primer-template for access to RT, and that addition of a nucleoside analog RT inhibitor to the in vitro reaction enhanced the overall effectiveness of both drugs, while nonnucleoside analog RT inhibitors exhibited simple additivity
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single-stranded DNA aptamer RT1t49
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inhibits viral RT polymerase and RNase H functions, pre-steady-state and order-of-addition kinetic analyses, ssDNA aptamer competes with primer-template for access to RT, and that addition of a nucleoside analog RT inhibitor to the in vitro reaction enhanced the overall effectiveness of both drugs, while nonnucleoside analog RT inhibitors exhibited simple additivity
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single-stranded DNA aptamer RT1t49
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inhibits viral RT polymerase and RNase H functions, pre-steady-state and order-of-addition kinetic analyses, ssDNA aptamer competes with primer-template for access to RT, and that addition of a nucleoside analog RT inhibitor to the in vitro reaction enhanced the overall effectiveness of both drugs, while nonnucleoside analog RT inhibitors exhibited simple additivity
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inhibits viral RT polymerase and RNase H functions, pre-steady-state and order-of-addition kinetic analyses, ssDNA aptamer competes with primer-template for access to RT, and that addition of a nucleoside analog RT inhibitor to the in vitro reaction enhanced the overall effectiveness of both drugs, while nonnucleoside analog RT inhibitors exhibited simple additivity
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single-stranded RNA aptamer RT1t49
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inhibits viral RT polymerase and RNase H functions, pre-steady-state and order-of-addition kinetic analyses, ssDNA aptamer competes with primer-template for access to RT, and that addition of a nucleoside analog RT inhibitor to the in vitro reaction enhanced the overall effectiveness of both drugs, while nonnucleoside analog RT inhibitors exhibited simple additivity
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single-stranded RNA aptamer RT1t49
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inhibits viral RT polymerase and RNase H functions, pre-steady-state and order-of-addition kinetic analyses, ssDNA aptamer competes with primer-template for access to RT, and that addition of a nucleoside analog RT inhibitor to the in vitro reaction enhanced the overall effectiveness of both drugs, while nonnucleoside analog RT inhibitors exhibited simple additivity
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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 is reported. All nine of the N-hydroxypyridinedioness inhibit HBV replication. The N-hydroxypyridinedione compound class holds potential for antiviral discovery. No inhibition by A10 and A11. 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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selectivity of tropolone derivatives for HIV-1 and HIV-2 enzymes, IC50 values, inhibition mechanism, overview
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additional information
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development of a fluorescence polarization assay for screening inhibitors against the RNase H activity of HIV-1 reverse transcriptase, two assay variants, overview
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additional information
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no inhibition by O-methylated 3,7-dihydroxytropolones and tropolones, IC50 values, overview
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additional information
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design of diverse dsDNA thioaptamers with selected thiophosphate backbone substitutions effectively inhibiting the RNase activity of the reverse transcriptase and the viral replication, i.e. thioadaptamer R12-2 or XBY-S2, overview
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additional information
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effects of reverse transcriptase polymerase domain inhibitors on RNase H activity dependent on the substrate, overview, no inhibition of RNase H by nucleoside analogue 3'-azido-3'-deoxythymidine triphosphate
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additional information
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nonnucleoside reverse transcriptase inhibitors, i.e. NNRTIs, binding to the polymerase domain of HIV-RT interferes with RNase H activity through a long-range effect, which is affected by the structure of the RNA:DNA hybrid substrate, but is independent of NNRTI compound structure and nucleic acid substrate sequence
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additional information
inhibition mechanism, overview, antiviral activity and cytotoxic effects of inhibitors, overview
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additional information
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inhibition mechanism, overview, antiviral activity and cytotoxic effects of inhibitors, overview
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additional information
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natural product extracts screening for detection of inhibitors specific for HIV-1 RNase H
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additional information
one potential class of RNase H inhibitors involves drugs that alter the interactions between the RNase H domain and substrate or that alter the alignment of substrate in the RNase H active site
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additional information
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one potential class of RNase H inhibitors involves drugs that alter the interactions between the RNase H domain and substrate or that alter the alignment of substrate in the RNase H active site
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additional information
screening of 20000 small-molecular-weight compounds for RNase H inhibitors
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additional information
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resistance to nucleoside reverse transcriptase inhibitors
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additional information
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summary of HIV-1 RNase H inhibitors. Ardimerin has no inhibitory activity against HIV-1 RNase H because of the absence of galloyl unit. Oligonucleotide with 35 base pairs based on the G-quartet inhibits the RNase H and the polymerase. Different oligonucleotides with structural characters of hairpins and dumbbells: 1R4RR4, 2R4RR4, 3R4RR4, 4D4RD4, 5R4D4R, 6R6RR6, 7R6RR6, 8nicked dumbbell, and 9ligared dumbbell. Effective, they do not inhibit the polymerase and RNase H of Mammalia
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additional information
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natural product extracts screening for detection of inhibitors specific for HIV-2 RNase H
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additional information
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one potential class of RNase H inhibitors involves drugs that alter the interactions between the RNase H domain and substrate or that alter the alignment of substrate in the RNase H active site
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additional information
one potential class of RNase H inhibitors involves drugs that alter the interactions between the RNase H domain and substrate or that alter the alignment of substrate in the RNase H active site
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