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Literature summary for 2.7.7.49 extracted from

  • Herman, B.D.; Schinazi, R.F.; Zhang, H.W.; Nettles, J.H.; Stanton, R.; Detorio, M.; Obikhod, A.; Pradere, U.; Coats, S.J.; Mellors, J.W.; Sluis-Cremer, N.
    Substrate mimicry: HIV-1 reverse transcriptase recognizes 6-modified-3'-azido-2',3'-dideoxyguanosine-5'-triphosphates as adenosine analogs (2012), Nucleic Acids Res., 40, 381-390.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.7.7.49

Protein Variants

Protein Variants Comment Organism
K65R site-directed mutagenesis Human immunodeficiency virus 1
L74V site-directed mutagenesis Human immunodeficiency virus 1
M184V site-directed mutagenesis Human immunodeficiency virus 1
Q151M site-directed mutagenesis Human immunodeficiency virus 1

Inhibitors

Inhibitors Comment Organism Structure
2-amino-3'-azido-2',3'-dideoxy-N,N-dimethyladenosine 5'-triphosphate
-
 Human immunodeficiency virus 1
3'-azido-2',3'-dideoxy-2,6-diaminopurine-beta-D-ribofuranosyl 5'-triphosphate
-
 Human immunodeficiency virus 1
3'-azido-2',3'-dideoxy-2-amino-6-chloropurine-beta-D-ribofuranosyl 5'-triphosphate
-
 Human immunodeficiency virus 1
3'-azido-2',3'-dideoxy-2-amino-6-methoxypurine-beta-D-ribofuranosyl 5'-triphosphate
-
 Human immunodeficiency virus 1
3'-azido-2',3'-dideoxy-2-amino-6-N-allylaminopurine-beta-D-ribofuranosyl 5'-triphosphate
-
 Human immunodeficiency virus 1
3'-azido-2',3'-dideoxyadenosine triphosphate
-
 Human immunodeficiency virus 1
3'-azido-2',3'-dideoxyguanosine triphosphate
-
 Human immunodeficiency virus 1
additional information EC50 values, molecular modeling, overview Human immunodeficiency virus 1
zidovudine triphosphate
-
 Human immunodeficiency virus 1

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
 additional information pre-steady-state incorporation of 6-modified 3'-azido-ddGTP nucleotides by HIV-1 RT, steady-state kinetics, overview Human immunodeficiency virus 1
0.00017
-
 dGTP pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1
0.00029
-
 3'-azido-2',3'-dideoxy-2,6-diaminopurine-beta-D-ribofuranosyl 5'-triphosphate pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1
0.00032
-
 3'-azido-2',3'-dideoxyadenosine triphosphate pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1
0.00033
-
 dATP pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1
0.00092
-
 3'-azido-2',3'-dideoxy-2-amino-6-chloropurine-beta-D-ribofuranosyl 5'-triphosphate pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1
0.0018
-
 3'-azido-2',3'-dideoxy-2-amino-6-chloropurine-beta-D-ribofuranosyl 5'-triphosphate pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1
0.0048
-
 3'-azido-2',3'-dideoxy-2-amino-6-N-allylaminopurine-beta-D-ribofuranosyl 5'-triphosphate pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1
0.012
-
 3'-azido-2',3'-dideoxy-2-amino-6-methoxypurine-beta-D-ribofuranosyl 5'-triphosphate pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1
0.0163
-
 3'-azido-2',3'-dideoxy-2-amino-6-methoxypurine-beta-D-ribofuranosyl 5'-triphosphate pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1
0.034
-
 3'-azido-2',3'-dideoxy-2,6-diaminopurine-beta-D-ribofuranosyl 5'-triphosphate pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ required Human immunodeficiency virus 1

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
dATP + DNAn Human immunodeficiency virus 1 RNA-dependent DNA synthesis diphosphate + DNAn+1
-
 ?
deoxynucleoside triphosphate + DNAn Human immunodeficiency virus 1 RNA-dependent DNA synthesis diphosphate + DNAn+1
-
 ?
dGTP + DNAn Human immunodeficiency virus 1 RNA-dependent DNA synthesis diphosphate + DNAn+1
-
 ?
additional information Human immunodeficiency virus 1 the enzyme performs DNA-dependent DNA synthesis and RNA-dependent DNA synthesis, see also EC 2.7.7.7 ?
-
 ?

Organism

Organism UniProt Comment Textmining
Human immunodeficiency virus 1
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3'-azido-2',3'-dideoxy-2,6-diaminopurine-beta-D-ribofuranosyl 5'-triphosphate + DNAn incorporation activity of the enzyme with the enzyme inhibitor as A analogue or G analogue Human immunodeficiency virus 1 diphosphate + ?
-
 ?
3'-azido-2',3'-dideoxy-2-amino-6-chloropurine-beta-D-ribofuranosyl 5'-triphosphate + DNAn incorporation activity of the enzyme with the enzyme inhibitor as A analogue or G analogue Human immunodeficiency virus 1 diphosphate + ?
-
 ?
3'-azido-2',3'-dideoxy-2-amino-6-methoxypurine-beta-D-ribofuranosyl 5'-triphosphate + DNAn incorporation activity of the enzyme with the enzyme inhibitor as A analogue or G analogue Human immunodeficiency virus 1 diphosphate + ?
-
 ?
3'-azido-2',3'-dideoxy-2-amino-6-N-allylaminopurine-beta-D-ribofuranosyl 5'-triphosphate + DNAn incorporation activity of the enzyme with the enzyme inhibitor as A analogue or G analogue Human immunodeficiency virus 1 diphosphate + ?
-
 ?
3'-azido-2',3'-dideoxyadenosine triphosphate + DNAn incorporation activity of the enzyme with the enzyme inhibitor as A analogue or G analogue Human immunodeficiency virus 1 diphosphate + DNAn+1
-
 ?
dATP + DNAn RNA-dependent DNA synthesis Human immunodeficiency virus 1 diphosphate + DNAn+1
-
 ?
deoxynucleoside triphosphate + DNAn RNA-dependent DNA synthesis Human immunodeficiency virus 1 diphosphate + DNAn+1
-
 ?
dGTP + DNAn RNA-dependent DNA synthesis Human immunodeficiency virus 1 diphosphate + DNAn+1
-
 ?
additional information the enzyme performs DNA-dependent DNA synthesis and RNA-dependent DNA synthesis, see also EC 2.7.7.7 Human immunodeficiency virus 1 ?
-
 ?

Synonyms

Synonyms Comment Organism
HIV-1 RT
-
 Human immunodeficiency virus 1

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Human immunodeficiency virus 1

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.16
-
 3'-azido-2',3'-dideoxy-2,6-diaminopurine-beta-D-ribofuranosyl 5'-triphosphate pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1
0.22
-
 3'-azido-2',3'-dideoxy-2-amino-6-methoxypurine-beta-D-ribofuranosyl 5'-triphosphate pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1
0.37
-
 3'-azido-2',3'-dideoxy-2-amino-6-chloropurine-beta-D-ribofuranosyl 5'-triphosphate pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1
2.1
-
 3'-azido-2',3'-dideoxy-2-amino-6-N-allylaminopurine-beta-D-ribofuranosyl 5'-triphosphate pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1
2.7
-
 3'-azido-2',3'-dideoxy-2-amino-6-chloropurine-beta-D-ribofuranosyl 5'-triphosphate pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1
2.8
-
 3'-azido-2',3'-dideoxy-2-amino-6-methoxypurine-beta-D-ribofuranosyl 5'-triphosphate pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1
14
-
 3'-azido-2',3'-dideoxy-2,6-diaminopurine-beta-D-ribofuranosyl 5'-triphosphate pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1
14
-
 3'-azido-2',3'-dideoxyadenosine triphosphate pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1
17
-
 dATP pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1
17.3
-
 dGTP pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
 assay at Human immunodeficiency virus 1

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00006
-
 pH 7.5, 37°C, mutant M184V Human immunodeficiency virus 1 3'-azido-2',3'-dideoxyguanosine triphosphate
0.00012
-
 pH 7.5, 37°C, mutant M184V Human immunodeficiency virus 1 zidovudine triphosphate
0.00013
-
 pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1 zidovudine triphosphate
0.00015
-
 pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1 3'-azido-2',3'-dideoxyguanosine triphosphate
0.00016
-
 pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1 3'-azido-2',3'-dideoxyadenosine triphosphate
0.00018
-
 pH 7.5, 37°C, mutant L74V Human immunodeficiency virus 1 zidovudine triphosphate
0.00019
-
 pH 7.5, 37°C, mutant M184V Human immunodeficiency virus 1 3'-azido-2',3'-dideoxyadenosine triphosphate
0.00025
-
 pH 7.5, 37°C, mutant L74V Human immunodeficiency virus 1 3'-azido-2',3'-dideoxyguanosine triphosphate
0.0003
-
 pH 7.5, 37°C, mutant Q151M Human immunodeficiency virus 1 3'-azido-2',3'-dideoxyguanosine triphosphate
0.00034
-
 pH 7.5, 37°C, mutant M184V Human immunodeficiency virus 1 3'-azido-2',3'-dideoxy-2,6-diaminopurine-beta-D-ribofuranosyl 5'-triphosphate
0.00036
-
 pH 7.5, 37°C, mutant K65R Human immunodeficiency virus 1 3'-azido-2',3'-dideoxyguanosine triphosphate
0.00042
-
 pH 7.5, 37°C, mutant L74V Human immunodeficiency virus 1 3'-azido-2',3'-dideoxyadenosine triphosphate
0.00066
-
 pH 7.5, 37°C, mutant K65R Human immunodeficiency virus 1 zidovudine triphosphate
0.0007
-
 pH 7.5, 37°C, mutant K65R Human immunodeficiency virus 1 3'-azido-2',3'-dideoxyadenosine triphosphate
0.0008
-
 pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1 3'-azido-2',3'-dideoxy-2,6-diaminopurine-beta-D-ribofuranosyl 5'-triphosphate
0.0013
-
 pH 7.5, 37°C, mutant L74V Human immunodeficiency virus 1 3'-azido-2',3'-dideoxy-2,6-diaminopurine-beta-D-ribofuranosyl 5'-triphosphate
0.0014
-
 pH 7.5, 37°C, mutant Q151M Human immunodeficiency virus 1 3'-azido-2',3'-dideoxyadenosine triphosphate
0.0025
-
 pH 7.5, 37°C, mutant K65R Human immunodeficiency virus 1 3'-azido-2',3'-dideoxy-2,6-diaminopurine-beta-D-ribofuranosyl 5'-triphosphate
0.0025
-
 pH 7.5, 37°C, mutant M184V Human immunodeficiency virus 1 3'-azido-2',3'-dideoxy-2-amino-6-chloropurine-beta-D-ribofuranosyl 5'-triphosphate
0.0027
-
 pH 7.5, 37°C, mutant Q151M Human immunodeficiency virus 1 zidovudine triphosphate
0.0032
-
 pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1 3'-azido-2',3'-dideoxy-2-amino-6-chloropurine-beta-D-ribofuranosyl 5'-triphosphate
0.0041
-
 pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1 3'-azido-2',3'-dideoxy-2-amino-6-N-allylaminopurine-beta-D-ribofuranosyl 5'-triphosphate
0.0042
-
 pH 7.5, 37°C, mutant Q151M Human immunodeficiency virus 1 3'-azido-2',3'-dideoxy-2,6-diaminopurine-beta-D-ribofuranosyl 5'-triphosphate
0.0048
-
 pH 7.5, 37°C, mutant M184V Human immunodeficiency virus 1 3'-azido-2',3'-dideoxy-2-amino-6-N-allylaminopurine-beta-D-ribofuranosyl 5'-triphosphate
0.0088
-
 pH 7.5, 37°C, mutant K65R Human immunodeficiency virus 1 3'-azido-2',3'-dideoxy-2-amino-6-N-allylaminopurine-beta-D-ribofuranosyl 5'-triphosphate
0.0091
-
 pH 7.5, 37°C, mutant K65R Human immunodeficiency virus 1 3'-azido-2',3'-dideoxy-2-amino-6-chloropurine-beta-D-ribofuranosyl 5'-triphosphate
0.0103
-
 pH 7.5, 37°C, mutant L74V Human immunodeficiency virus 1 3'-azido-2',3'-dideoxy-2-amino-6-N-allylaminopurine-beta-D-ribofuranosyl 5'-triphosphate
0.0118
-
 pH 7.5, 37°C, mutant L74V Human immunodeficiency virus 1 3'-azido-2',3'-dideoxy-2-amino-6-chloropurine-beta-D-ribofuranosyl 5'-triphosphate
0.0218
-
 pH 7.5, 37°C, mutant Q151M Human immunodeficiency virus 1 3'-azido-2',3'-dideoxy-2-amino-6-N-allylaminopurine-beta-D-ribofuranosyl 5'-triphosphate
0.0234
-
 pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1 2-amino-3'-azido-2',3'-dideoxy-N,N-dimethyladenosine 5'-triphosphate
0.0244
-
 pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1 3'-azido-2',3'-dideoxy-2-amino-6-methoxypurine-beta-D-ribofuranosyl 5'-triphosphate
0.0308
-
 pH 7.5, 37°C, mutant Q151M Human immunodeficiency virus 1 3'-azido-2',3'-dideoxy-2-amino-6-chloropurine-beta-D-ribofuranosyl 5'-triphosphate
0.0329
-
 pH 7.5, 37°C, mutant M184V Human immunodeficiency virus 1 3'-azido-2',3'-dideoxy-2-amino-6-methoxypurine-beta-D-ribofuranosyl 5'-triphosphate
0.05
-
 pH 7.5, 37°C, mutant K65R Human immunodeficiency virus 1 2-amino-3'-azido-2',3'-dideoxy-N,N-dimethyladenosine 5'-triphosphate
0.05
-
 pH 7.5, 37°C, mutant L74V Human immunodeficiency virus 1 2-amino-3'-azido-2',3'-dideoxy-N,N-dimethyladenosine 5'-triphosphate
0.05
-
 pH 7.5, 37°C, mutant Q151M Human immunodeficiency virus 1 2-amino-3'-azido-2',3'-dideoxy-N,N-dimethyladenosine 5'-triphosphate
0.078
-
 pH 7.5, 37°C, mutant Q151M Human immunodeficiency virus 1 3'-azido-2',3'-dideoxy-2-amino-6-methoxypurine-beta-D-ribofuranosyl 5'-triphosphate
0.08
-
 pH 7.5, 37°C, mutant K65R Human immunodeficiency virus 1 3'-azido-2',3'-dideoxy-2-amino-6-methoxypurine-beta-D-ribofuranosyl 5'-triphosphate
0.1
-
 pH 7.5, 37°C, mutant L74V Human immunodeficiency virus 1 3'-azido-2',3'-dideoxy-2-amino-6-methoxypurine-beta-D-ribofuranosyl 5'-triphosphate

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
0.000005
-
 3'-azido-2',3'-dideoxy-2,6-diaminopurine-beta-D-ribofuranosyl 5'-triphosphate pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1
0.000013
-
 3'-azido-2',3'-dideoxy-2-amino-6-methoxypurine-beta-D-ribofuranosyl 5'-triphosphate pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1
0.00023
-
 3'-azido-2',3'-dideoxy-2-amino-6-methoxypurine-beta-D-ribofuranosyl 5'-triphosphate pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1
0.000402
-
 3'-azido-2',3'-dideoxy-2-amino-6-chloropurine-beta-D-ribofuranosyl 5'-triphosphate pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1
0.00044
-
 3'-azido-2',3'-dideoxy-2-amino-6-N-allylaminopurine-beta-D-ribofuranosyl 5'-triphosphate pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1
0.00102
-
 dGTP pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1
0.0015
-
 3'-azido-2',3'-dideoxy-2-amino-6-chloropurine-beta-D-ribofuranosyl 5'-triphosphate pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1
0.044
-
 3'-azido-2',3'-dideoxyadenosine triphosphate pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1
0.048
-
 3'-azido-2',3'-dideoxy-2,6-diaminopurine-beta-D-ribofuranosyl 5'-triphosphate pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1
0.052
-
 dATP pH 7.5, 37°C, wild-type enzyme Human immunodeficiency virus 1