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Literature summary for 2.7.7.49 extracted from
- Pre-steady state kinetic analysis of cyclobutyl derivatives of 2-deoxyadenosine 5-triphosphate as inhibitors of HIV-1 reverse transcriptase (2012), Bioorg. Med. Chem. Lett., 22, 4064-4067.
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| K65R | site-directed mutagenesis | Human immunodeficiency virus 1 |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| ((1s,3s)-3-(7-amino-2H-2,3,5,6-tetraazabenzo[cd]azulen-2-yl)cyclobutyl)methyl tetrahydrogen triphosphate | - |
Human immunodeficiency virus 1 |  |
| 2'-fluoro-N-cyclobutyladenosine triphosphate | - |
Human immunodeficiency virus 1 | |
| additional information | N-cyclobutyladenosine analogues can act as substrates for incorporation by HIV-1 RT and be a potential scaffold for HIV inhibitors, cyclobutyl derivatives of 2-deoxyadenosine 5-triphosphate as inhibitors of HIV-1 reverse transcriptase, overview | Human immunodeficiency virus 1 | |
| N-cyclobutyladenosine triphosphate | - |
Human immunodeficiency virus 1 | |
| N-cyclobutyladenosine-phosphonyl diphosphate | - |
Human immunodeficiency virus 1 | |
| tenofovir diphosphate | - |
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 kinetic analysis of 2-deoxyadenosine 5-triphosphate compounds with wild-type and mutant K65R enzymes, overview | Human immunodeficiency virus 1 | |
| 0.0047 | - |
N-cyclobutyladenosine-phosphonyl diphosphate | pH and temperature not specified in the publication, wild-type enzyme | Human immunodeficiency virus 1 | |
| 0.0066 | - |
tenofovir diphosphate | pH and temperature not specified in the publication, wild-type enzyme | Human immunodeficiency virus 1 | |
| 0.0291 | - |
dATP | pH and temperature not specified in the publication, wild-type enzyme | 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 | - |
diphosphate + DNAn+1 | - |
? | |
| deoxynucleoside triphosphate + DNAn | Human immunodeficiency virus 1 | - |
diphosphate + DNAn+1 | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Human immunodeficiency virus 1 | - |
- |
- |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ((1s,3s)-3-(7-amino-2H-2,3,5,6-tetraazabenzo[cd]azulen-2-yl)cyclobutyl)methyl tetrahydrogen triphosphate + DNAn | - |
Human immunodeficiency virus 1 | diphosphate + DNAn+1 | - |
? | |
| 2'-fluoro-N-cyclobutyladenosine triphosphate + DNAn | - |
Human immunodeficiency virus 1 | diphosphate + DNAn+1 | - |
? | |
| dATP + DNAn | - |
Human immunodeficiency virus 1 | diphosphate + DNAn+1 | - |
? | |
| deoxynucleoside triphosphate + DNAn | - |
Human immunodeficiency virus 1 | diphosphate + DNAn+1 | - |
? | |
| additional information | N-cyclobutyladenosine analogues can act as substrates for incorporation by HIV-1 RT and be a potential scaffold for HIV inhibitors, overview | Human immunodeficiency virus 1 | ? | - |
? | |
| N-cyclobutyladenosine triphosphate + DNAn | - |
Human immunodeficiency virus 1 | diphosphate + DNAn+1 | - |
? | |
| N-cyclobutyladenosine-phosphonyl diphosphate + DNAn | - |
Human immunodeficiency virus 1 | diphosphate + DNAn+1 | - |
? | |
| tenofovir diphosphate + DNAn | - |
Human immunodeficiency virus 1 | diphosphate + DNAn+1 | - |
? | |
Turnover Number [1/s]
| Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.07 | - |
N-cyclobutyladenosine-phosphonyl diphosphate | pH and temperature not specified in the publication, wild-type enzyme | Human immunodeficiency virus 1 | |
| 0.15 | - |
tenofovir diphosphate | pH and temperature not specified in the publication, wild-type enzyme | Human immunodeficiency virus 1 | |
| 0.4 | - |
dATP | pH and temperature not specified in the publication, wild-type enzyme | Human immunodeficiency virus 1 | |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | inhibition kinetic analysis of 2-deoxyadenosine 5-triphosphate compounds with wild-type and mutant K65R enzymes, overview | Human immunodeficiency virus 1 |
kcat/KM [mM/s]
| kcat/KM Value [1/mMs-1] | kcat/KM Value Maximum [1/mMs-1] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 5.15 | - |
dATP | pH and temperature not specified in the publication, wild-type enzyme | Human immunodeficiency virus 1 | |
| 14.89 | - |
N-cyclobutyladenosine-phosphonyl diphosphate | pH and temperature not specified in the publication, wild-type enzyme | Human immunodeficiency virus 1 | |
| 60.6 | - |
tenofovir diphosphate | pH and temperature not specified in the publication, wild-type enzyme | Human immunodeficiency virus 1 | |
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