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Information on EC 3.1.26.13 - retroviral ribonuclease H and Organism(s) Human immunodeficiency virus type 1 group M subtype B and UniProt Accession P03366
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3.1.26.13 retroviral ribonuclease HSpecify your search results
Word Map
- 3.1.26.13
-
integrase
- hiv-rt
- rna-dna
-
template-primer
-
moloney
-
polypurine
- transcriptases
-
minus-strand
- 3'-azido-3'-deoxythymidine
-
nnrti
-
primer-template
-
nonnucleoside
- drug development
- medicine
- analysis
- pharmacology
The enzyme appears in selected viruses and cellular organisms
Reaction Schemes
Endohydrolysis of RNA in RNA/DNA hybrids. Three different cleavage modes: 1. sequence-specific internal cleavage of RNA. Human immunodeficiency virus type 1 and Moloney murine leukemia virus enzymes prefer to cleave the RNA strand one nucleotide away from the RNA-DNA junction. 2. RNA 5'-end directed cleavage 13-19 nucleotides from the RNA end. 3. DNA 3'-end directed cleavage 15-20 nucleotides away from the primer terminus.
Synonyms
human immunodeficiency virus reverse transcriptase, hiv-1 rnase h, rt-rnase h, reverse transcriptase-associated rnase h, hiv-1 rt-associated rnase h, retroviral ribonuclease h, hiv rt-associated rnase h, hiv-1 reverse transcriptase ribonuclease h, hiv-1 reverse transcriptase rnase h, reverse-transcriptase-associated ribonuclease h, 
more
topSYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
reverse transcriptase-associated ribonuclease H
Human immunodeficiency virus type 1 group M subtype B
-
reverse transcriptase-associated RNase H
Human immunodeficiency virus type 1 group M subtype B
-
CAS REGISTRY NUMBER
COMMENTARY
9050-76-4
-
SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
additional information
?
-
Human immunodeficiency virus type 1 group M subtype B
5' end labeled RNA-DNA heteroduplexe substrates aligned from commercial RNA and DNA oligonucleotides are used
-
-
?
additional information
?
-
Human immunodeficiency virus type 1 group M subtype B
activity of wild-type enzyme is determined with the RNA/DNA template-primer R33B/20A, comparison of HIV-1 group O subtype B ESP49 and HIV-1 group M subtype B BH10
-
-
?
additional information
?
-
Human immunodeficiency virus type 1 group M subtype B
hybrid RNA/DNA 5'-GAUCUGAGCCUGGGAGCU-fluorescin-3' and 5'-dabsyl-AGCTCCCAGGCTCAGATC-3' are used for RNase H activity assays
-
-
?
additional information
?
-
Human immunodeficiency virus type 1 group M subtype B
-
usage of DNA/RNA hybrid substrates for enzyme activity assay. The isolated RNH domain of reverse transcriptase (RT), folded by itself, is not catalytically active, due to lack of the substrate handle region, but exhibits a native-like protein fold
-
-
?
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
Mg2+
Mn2+
Human immunodeficiency virus type 1 group M subtype B
-
Mn2+ binding increased the stability of the enzyme domain RNH
Zn2+
Human immunodeficiency virus type 1 group M subtype B
-
Zn2+ binding increased the stability of the enzyme domain RNH
additional information
Human immunodeficiency virus type 1 group M subtype B
-
structural effect of divalent metal ions, i.e. Mn2+, Zn2+, and Mg2+, to the isolated ribonuclease H (RNH) of human immunodeficiency virus (HIV) using isothermal titration calorimetry and circular dichroism, overview. The binding affinity of Mg2+ is about 40 and 400 times lower than those of Mn2+ and of Zn2+, respectively. The structural analysis shows that Mg2+ binding has little effect on the thermal stability of RNH, while Zn2+ and Mn2+ binding increased the stability
Mg2+
Human immunodeficiency virus type 1 group M subtype B
-
binding thermodynamics of Mg2+ to RNH, Mg2+ binding has little effect on the thermal stability of enzyme domain RNH
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
2,6-dimethoxy-N-(3-(pyridin-2-ylcarbamoyl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophen-2-yl)nicotinamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(2,4-dichlorobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-(2-fluorophenyl)acetamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-aminobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-bromobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-chloro-4-fluorobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-chlorobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-cyclohexylacetamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-fluorobenzamido)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-fluorobenzamido)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxylic acid
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-fluorobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-methoxybenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-methylbenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-nitrobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(3,4-dihydroxybenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(3,4-dihydroxyphenyl)-3,5,6,7,8,9-hexahydro-4H-cyclohepta[4,5]thieno[2,3-d]pyrimidin-4-one
Human immunodeficiency virus type 1 group M subtype B
-
2-(3,4-dimethoxybenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(3-fluorobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(3-phenylpropanamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(4-aminobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(4-chlorobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(4-fluorobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(4-nitrobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-acetamido-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-amino-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-benzamido-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-hydroxy-6-methoxy-N-(3-(pyridin-2-ylcarbamoyl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophen-2-yl)nicotinamide
Human immunodeficiency virus type 1 group M subtype B
-
2-[(cyclohexanecarbonyl)amino]-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-[3-(4-chlorophenyl)propanamido]-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-[3-(4-fluorophenyl)propanamido]-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
4-((4'-amino-[1,1'-biphenyl]-4-yl)amino)-1-hydroxy-1,8-naphthyridin-2(1H)-one
Human immunodeficiency virus type 1 group M subtype B
-
4-([1,1'-biphenyl]-4-ylamino)-1-hydroxy-1,8-naphthyridin-2(1H)-one
Human immunodeficiency virus type 1 group M subtype B
-
5,6-dimethyl-2-(4-nitrophenyl)thieno[2,3-d]pyrimidin-4(3H)-one
Human immunodeficiency virus type 1 group M subtype B
-
ethyl 2-(2-fluorobenzamido)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxylate
Human immunodeficiency virus type 1 group M subtype B
-
ethyl 2-(4-chlorobenzamido)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxylate
Human immunodeficiency virus type 1 group M subtype B
-
methyl 4-((4'-amino-[1,1'-biphenyl]-4-yl)amino)-1-hydroxy-2-oxo-1,2-dihydro-1,8-naphthyridine-3-carboxylate
Human immunodeficiency virus type 1 group M subtype B
-
methyl 4-amino-1-hydroxy-2-oxo-1,2-dihydro-1,8-naphthyridine-3-carboxylate
Human immunodeficiency virus type 1 group M subtype B
-
N-(3-((2-fluorophenyl)carbamoyl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophen-2-yl)picolinamide
Human immunodeficiency virus type 1 group M subtype B
-
N-(pyridin-2-yl)-2-(thiophene-2-carboxamido)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
N-(pyridin-2-yl)-2-[2-(quinolin-6-yl)acetamido]-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
additional information
Human immunodeficiency virus type 1 group M subtype B
development and evaluation of inhibitors against the RNase H active site of HIV-1 reverse transcriptase. The RNase H active site of HIV-1 RT is sufficiently different from the active sites of the two cellular human enzymes, RNase H1 and RNase H2, that compounds can be developed as selective inhibitors of viral RH. Antiviral activities of compounds XZ456, XZ460, XZ462, and MK463 against wild-type enzyme and against HIV-1 vectors that carry well-known INSTI, NNRTI, and NRTI resistance mutations, overview. XZ456 and XZ460 both inhibit these NRTI mutants with efficacies similar to their antiviral activities against wild-type HIV-1. Conversely, the NRTI-resistant mutants cause a 3 to 4fold reduction in susceptibility to XZ462 and MK463. Compounds are tested in viral replication and cytotoxicity assays. For enzyme-inhibitor structural modelling, coordinates of the following retroviral RT-RT inhibitor structures are used: HIV RT-MK1 (PDB ID 3LP0) and HIV RT-MK2 (PDB ID 3LP1). The compounds target the catalytic magnesium ions in the HIV-1 RNase H
-
additional information
Human immunodeficiency virus type 1 group M subtype B
inhibitor library screening, identification and synthesis of cycloheptathiophene-3-carboxamide derivatives as allosteric HIV-1 ribonuclease H inhibitors, binding mode of compounds 2-(3,4-dihydroxyphenyl)-3,5,6,7,8,9-hexahydro-4H-cyclohepta[4,5]thieno[2,3-d]pyrimidin-4-one, 2-(3,4-dimethoxybenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide, and 2-(3,4-dihydroxybenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide, overview
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
additional information
additional information
Human immunodeficiency virus type 1 group M subtype B
-
analysis of the binding thermodynamics and structural effect of divalent metal ions, i.e. Mn2+, Zn2+, and Mg2+, to the isolated ribonuclease H (RNH) of human immunodeficiency virus (HIV) using isothermal titration calorimetry and circular dichroism, overview
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.0215
2,6-dimethoxy-N-(3-(pyridin-2-ylcarbamoyl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophen-2-yl)nicotinamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.01224
2-(2,4-dichlorobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.0099
2-(2-(2-fluorophenyl)acetamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.01488
2-(2-aminobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.00457
2-(2-bromobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.0075
2-(2-chloro-4-fluorobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.0239
2-(2-chlorobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.0671
2-(2-cyclohexylacetamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.01373
2-(2-fluorobenzamido)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.1
2-(2-fluorobenzamido)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxylic acid
Human immunodeficiency virus type 1 group M subtype B
above, pH 7.8, 37°C
0.02189
2-(2-fluorobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.01425
2-(2-methoxybenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.0183
2-(2-methylbenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.05348
2-(2-nitrobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.00084
2-(3,4-dihydroxybenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.00401
2-(3,4-dimethoxybenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.02047
2-(3-fluorobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.0146
2-(3-phenylpropanamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.02143
2-(4-aminobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.01778
2-(4-chlorobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.00472
2-(4-fluorobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.02047
2-(4-nitrobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.1
2-acetamido-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
above, pH 7.8, 37°C
0.0201
2-amino-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.0148
2-benzamido-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.001507
2-hydroxy-6-methoxy-N-(3-(pyridin-2-ylcarbamoyl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophen-2-yl)nicotinamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.0166
2-[(cyclohexanecarbonyl)amino]-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.0099
2-[3-(4-chlorophenyl)propanamido]-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.0145
2-[3-(4-fluorophenyl)propanamido]-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.0252
ethyl 2-(2-fluorobenzamido)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxylate
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.07258
ethyl 2-(4-chlorobenzamido)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxylate
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.0137
N-(3-((2-fluorophenyl)carbamoyl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophen-2-yl)picolinamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.01036
N-(pyridin-2-yl)-2-(thiophene-2-carboxamido)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
0.01644
N-(pyridin-2-yl)-2-[2-(quinolin-6-yl)acetamido]-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
pH 7.8, 37°C
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
physiological function
Human immunodeficiency virus type 1 group M subtype B
template-primer binding affinity and RNase H cleavage specificity contribute to the strand transfer efficiency of HIV-1 reverse transcriptase
additional information
additional information
Human immunodeficiency virus type 1 group M subtype B
-
enzyme domain RNH structure-function relationship analysis, overview
additional information
Human immunodeficiency virus type 1 group M subtype B
for enzyme-inhibitor structural modelling, coordinates of the following retroviral RT-RT inhibitor structures are used: HIV RT-MK1 (PDB ID 3LP0) and HIV RT-MK2 (PDB ID 3LP1)
CRYSTALLIZATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
HIV-1 reverse transcriptase mutant form RT52A in complex with rilpivirine and an RNase H inhibitor XZ462, hanging drop vapor diffusion method, the crystallization solution contains 10% PEG 8000, 50 mM imidazole, pH 6.8, 10 mM spermine, 15 mM MgSO4, and 100 mM (NH4)2SO4, crystals of the RT-rilpivirine (RPV) complex are soaked for 30 min with 2 mM compound XZ462 in the crystallization solution in presence of 15 mM MgSO4, X-ray diffraction structure determination and analysis at 1.51-2.2 A resolution, molecular replacement using the 1.51 A resolution structure of the HIV-1 RT-rilpivirine complex (PDB ID 4G1Q) as template
Human immunodeficiency virus type 1 group M subtype B
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
D443N
Human immunodeficiency virus type 1 group M subtype B
RNase H inactivating mutation, the mutant is devoid of strand transfer activity
E478Q
Human immunodeficiency virus type 1 group M subtype B
RNase H inactivating mutation, the mutant is devoid of strand transfer activity
G140S/Q148H
Human immunodeficiency virus type 1 group M subtype B
site-directed mutagenesis, mutant INSTI
K70R
Human immunodeficiency virus type 1 group M subtype B
site-directed mutagenesis, mutant NRTI
L100I/K103N
Human immunodeficiency virus type 1 group M subtype B
site-directed mutagenesis, mutant NNRTI
M184V
Human immunodeficiency virus type 1 group M subtype B
site-directed mutagenesis, mutant NRTI
V106A
Human immunodeficiency virus type 1 group M subtype B
site-directed mutagenesis, mutant NNRTI
Y181C
Human immunodeficiency virus type 1 group M subtype B
site-directed mutagenesis, mutant NNRTI
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Corona, A.; Desantis, J.; Massari, S.; Distinto, S.; Masaoka, T.; Sabatini, S.; Esposito, F.; Manfroni, G.; Maccioni, E.; Cecchetti, V.; Pannecouque, C.; Le Grice, S.; Tramontano, E.; Tabarrini, O.
Studies on cycloheptathiophene-3-carboxamide derivatives as allosteric HIV-1 ribonuclease H inhibitors
ChemMedChem
11
1709-1720
2016
Human immunodeficiency virus type 1 group M subtype B (P03366), Human immunodeficiency virus type 1 group M subtype B BH10 (P03366)
Luczkowiak, J.; Matamoros, T.; Menendez-Arias, L.
Template-primer binding affinity and RNase H cleavage specificity contribute to the strand transfer efficiency of HIV-1 reverse transcriptase
J. Biol. Chem.
293
13351-13363
2018
Human immunodeficiency virus type 1 group M subtype B (P03366), Human immunodeficiency virus type 1 group M subtype B BH10 (P03366), Human immunodeficiency virus type 1 group O subtype B, Human immunodeficiency virus type 1 group O subtype B ESP49
Oda, M.; Xi, Z.; Inaba, S.; Slack, R.; Ishima, R.
Binding thermodynamics of metal ions to HIV-1 ribonuclease H domain
J. Therm. Anal. Calorim.
135
2647-2653
2019
Human immunodeficiency virus type 1 group M subtype B, Human immunodeficiency virus type 1 group M subtype B BH10
Boyer, P.L.; Smith, S.J.; Zhao, X.Z.; Das, K.; Gruber, K.; Arnold, E.; Burke, T.R.; Hughes, S.H.
Developing and evaluating inhibitors against the RNase H active site of HIV-1 reverse transcriptase
J. Virol.
92
e02203-17
2018
Human immunodeficiency virus type 1 group M subtype B (P03366), Human immunodeficiency virus type 1 group M subtype B BH10 (P03366)
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