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Literature summary for 1.14.14.18 extracted from
- Isocyanides inhibit human heme oxygenases at the verdoheme stage (2009), Biochemistry, 48, 8920-8928.
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expressed in Escherichia coli | Candida albicans |
| truncated HO-1 lacking the 23 C-terminal residues, truncated HO-2 lacking the 23 C-terminal residues in the pBAce expression vector construct transformed into Escherichia coli DH5alpha | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| benzyl isocyanide | most potent uncompetitive inhibitor with respect to heme, is the strongest ligand to ferrous heme | Candida albicans |  |
| benzyl isocyanide | most potent uncompetitive inhibitor with respect to heme, is the strongest ligand to ferrous heme with an almost 42fold greater binding affinity for HO-1 than isopropyl isocyanide. HO-2 displays a similar trend. Ferric verdoheme-HO-1 shows a 2fold higher affinity for the inhibitor than ferric heme-HO-1 | Homo sapiens | |
| isopropyl isocyanide | - |
Candida albicans | |
| isopropyl isocyanide | binding affinity is the weakest for HO-1. HO-2 displays a similar trend | Homo sapiens | |
| additional information | whereas equilibrium binding of the isocyanides to ferric human heme oxygenases is rapid, binding to ferric Hmx1 is much slower | Candida albicans | |
| n-butyl isocyanide | - |
Candida albicans | |
| n-butyl isocyanide | displays a 9fold higher affinity than isopropyl isocyanide for HO-1. HO-2 displays a similar trend. Ferric verdoheme-HO-1 shows a 2fold higher affinity for the inhibitor than ferric heme-HO-1 | Homo sapiens | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.005 | - |
heme | HO-1 | Homo sapiens | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Candida albicans | - |
- |
- |
| Homo sapiens | - |
- |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| to apparent homogeneity | Candida albicans |
| truncated HO-1 and HO-2 lacking the 23 C-terminal residues, by gel filtration | Homo sapiens |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| heme + electron donor + O2 | - |
Homo sapiens | biliverdin + Fe2+ + CO + oxidized electron donor + H2O | - |
? | |
| heme + electron donor + O2 | - |
Candida albicans | biliverdin + Fe2+ + CO + oxidized electron donor + H2O | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| heme oxygenase | - |
Candida albicans |
| heme oxygenase-1 | - |
Homo sapiens |
| Hmx1 | - |
Candida albicans |
| HO-1 | - |
Homo sapiens |
| HO-2 | - |
Homo sapiens |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| heme | - |
Candida albicans | |
| additional information | CO as a ferrous heme ligand or ferricyanide as an oxidant have no effect | Homo sapiens | |
| NADPH | - |
Homo sapiens | |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0015 | - |
benzyl isocyanide | HO-1 | Homo sapiens | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.0001 | - |
HO-2, inhibition of conversion of heme | Homo sapiens | benzyl isocyanide | |
| 0.00013 | - |
HO-1, inhibition of conversion of heme | Homo sapiens | benzyl isocyanide | |
| 0.00025 | - |
HO-1, inhibition of conversion of heme | Homo sapiens | n-butyl isocyanide | |
| 0.00034 | - |
HO-2, inhibition of conversion of heme | Homo sapiens | n-butyl isocyanide | |
| 0.00072 | - |
HO-1, inhibition of conversion of heme | Homo sapiens | isopropyl isocyanide | |
| 0.00117 | - |
HO-2, inhibition of conversion of heme | Homo sapiens | isopropyl isocyanide | |
| 0.005 | - |
HO-1, inhibition of conversion of verdoheme | Homo sapiens | benzyl isocyanide | |
| 0.045 | - |
HO-1, inhibition of conversion of verdoheme | Homo sapiens | n-butyl isocyanide | |
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