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Literature summary for 2.3.1.B43 extracted from
- Role of the substrate specificity-defining residues of human SIRT5 in modulating the structural stability and inhibitory features of the enzyme (2016), PLoS ONE, 11, e0152467.
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expressed in Escherichia coli BL21(DE3) cells | Homo sapiens |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| R105L | the mutant enzyme favores the deacetylase reaction over the desuccinylation reaction | Homo sapiens |
| Y102A | the mutant enzyme catalyzes both deacetylation and desuccinylation reactions with comparable efficiencies | Homo sapiens |
| Y102A/R105I | the mutant enzyme favores the deacetylase reaction over the desuccinylation reaction | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| Isonicotinamide | - |
Homo sapiens |  |
| additional information | not inhibited by EX527 (i.e. 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide) | Homo sapiens | |
| nicotinamide | competitive inhibition | Homo sapiens | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.069 | - |
NAD+ | wild type enzyme, with [protein]-N6-succinyl-L-lysine as cosubstrate, at 8.0 pH and 25°C | Homo sapiens | |
| 0.29 | - |
[protein]-N6-succinyl-L-lysine | wild type enzyme, at 8.0 pH and 25°C | Homo sapiens | |
| 0.321 | - |
NAD+ | mutant enzyme Y102A, with [protein]-N6-succinyl-L-lysine as cosubstrate, at 8.0 pH and 25°C | Homo sapiens | |
| 0.388 | - |
[protein]-N6-succinyl-L-lysine | mutant enzyme Y102A/R105I, at 8.0 pH and 25°C | Homo sapiens | |
| 0.609 | - |
NAD+ | mutant enzyme R105I, with [protein]-N6-acetyl-L-lysine as cosubstrate, at 8.0 pH and 25°C | Homo sapiens | |
| 0.72 | - |
[protein]-N6-acetyl-L-lysine | mutant enzyme Y102A, at 8.0 pH and 25°C | Homo sapiens | |
| 1.194 | - |
NAD+ | mutant enzyme Y102A/R105I, with [protein]-N6-acetyl-L-lysine as cosubstrate, at 8.0 pH and 25°C | Homo sapiens | |
| 1.605 | - |
NAD+ | mutant enzyme Y102A, with [protein]-N6-acetyl-L-lysine as cosubstrate, at 8.0 pH and 25°C | Homo sapiens | |
| 1.658 | - |
[protein]-N6-succinyl-L-lysine | mutant enzyme R105I, at 8.0 pH and 25°C | Homo sapiens | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| NAD+ + [protein]-N6-acetyl-L-lysine | Homo sapiens | weak deacetylase activity | nicotinamide + [protein]-L-lysine + 2'-O-acetyl-ADP-ribose | - |
? | |
| NAD+ + [protein]-N6-succinyl-L-lysine | Homo sapiens | strong succinylase activity | nicotinamide + [protein]-L-lysine + 2'-O-succinyl-ADP-ribose | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | Q9NXA8 | - |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| HisTrap column chromatography and Hitrap column chromatography | Homo sapiens |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| NAD+ + Ac-Suc-L-Lys-7-amido-4-methylcoumarin | - |
Homo sapiens | nicotinamide + ? | - |
? | |
| NAD+ + Fluor-de-Lys | - |
Homo sapiens | nicotinamide + ? | - |
? | |
| NAD+ + [protein]-N6-acetyl-L-lysine | weak deacetylase activity | Homo sapiens | nicotinamide + [protein]-L-lysine + 2'-O-acetyl-ADP-ribose | - |
? | |
| NAD+ + [protein]-N6-succinyl-L-lysine | strong succinylase activity | Homo sapiens | nicotinamide + [protein]-L-lysine + 2'-O-succinyl-ADP-ribose | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| SIRT5 | - |
Homo sapiens |
Temperature Stability [°C]
| Temperature Stability Minimum [°C] | Temperature Stability Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 52.9 | - |
melting temperature | Homo sapiens |
Turnover Number [1/s]
| Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.000026 | - |
[protein]-N6-succinyl-L-lysine | mutant enzyme Y102A/R105I, at 8.0 pH and 25°C | Homo sapiens | |
| 0.000026 | - |
NAD+ | mutant enzyme Y102A/R105I, with [protein]-N6-acetyl-L-lysine as cosubstrate, at 8.0 pH and 25°C | Homo sapiens | |
| 0.000066 | - |
[protein]-N6-acetyl-L-lysine | mutant enzyme Y102A, at 8.0 pH and 25°C | Homo sapiens | |
| 0.000122 | - |
NAD+ | mutant enzyme R105I, with [protein]-N6-acetyl-L-lysine as cosubstrate, at 8.0 pH and 25°C | Homo sapiens | |
| 0.000274 | - |
[protein]-N6-succinyl-L-lysine | mutant enzyme R105I, at 8.0 pH and 25°C | Homo sapiens | |
| 0.000274 | - |
NAD+ | mutant enzyme Y102A, with [protein]-N6-succinyl-L-lysine as cosubstrate, at 8.0 pH and 25°C | Homo sapiens | |
| 0.04 | - |
[protein]-N6-succinyl-L-lysine | wild type enzyme, at 8.0 pH and 25°C | Homo sapiens | |
| 0.04 | - |
NAD+ | wild type enzyme, with [protein]-N6-succinyl-L-lysine as cosubstrate, at 8.0 pH and 25°C | Homo sapiens | |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0175 | - |
nicotinamide | wild type enzyme, at pH 8.0 and 25°C | Homo sapiens | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.0111 | - |
wild type enzyme, with 0.05 mM NAD+, at 8.0 pH and 25°C | Homo sapiens | Isonicotinamide | |
| 0.0347 | - |
wild type enzyme, at 8.0 pH and 25°C | Homo sapiens | Isonicotinamide | |
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