Cloned (Comment) | Organism |
---|---|
recombinant expression of His-tagged enzyme in Escherichia coli BL21(DE3) | Mycoplana ramosa |
Crystallization (Comment) | Organism |
---|---|
purified enzyme in complex with 5 different inhibitors, sitting drop vapor diffusion method, mixing of 500 nl of 5-10 mg/ml of protein in 20 mM Tris, pH 8.0, 50 mM NaCl, 0.01% sodium azide, 0.5-2 mM ZnCl2, and 2.5 mM inhibitor, with 500 nl of precipitant solution containing 0.2 M LiNO3, or KNO3, or LiCL, and 20% w/v PEG 3350, and equilibration against 0.1 ml of precipitant solution reservoir, 2 days, 21°C, X-ray diffraction structure determination and analysis at 1.13-1.42 A resolution | Mycoplana ramosa |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
5-amino-N-hydroxypentanamide | - |
Mycoplana ramosa | |
5-[(3-aminopropyl)amino]pentane-1-thiol | - |
Mycoplana ramosa | |
6-amino-N-hydroxyhexanamide | - |
Mycoplana ramosa | |
6-[(3-aminopropyl)amino]-N-hydroxyhexanamide | - |
Mycoplana ramosa | |
7-amino-N-hydroxyheptanamide | - |
Mycoplana ramosa | |
7-[(3-aminopropyl)amino]-1,1,1-trifluoroheptan-2-one | AAT, an analogue of N8-acetylspermidine | Mycoplana ramosa | |
8-amino-N-hydroxyoctanamide | - |
Mycoplana ramosa | |
additional information | design, synthesis, and evaluation of polyamine deacetylase inhibitors, and high-resolution crystal structures of their complexes with acetylpolyamine amidohydrolase, overview | Mycoplana ramosa |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Mg2+ | required | Mycoplana ramosa | |
Zn2+ | dependent on | Mycoplana ramosa |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
acetylcadaverine + H2O | Mycoplana ramosa | - |
acetate + cadaverine | - |
? | |
acetylputrescine + H2O | Mycoplana ramosa | - |
acetate + putrescine | - |
? | |
N1-acetylspermidine + H2O | Mycoplana ramosa | - |
acetate + spermidine | - |
? | |
N1-acetylspermine + H2O | Mycoplana ramosa | - |
acetate + spermine | - |
? | |
N8-acetylspermidine + H2O | Mycoplana ramosa | - |
acetate + spermidine | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Mycoplana ramosa | Q48935 | - |
- |
Purification (Comment) | Organism |
---|---|
recombinant His-tagged enzyme from Escherichia coli BL21(DE3) by nickel affinity chromatography | Mycoplana ramosa |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
acetylcadaverine + H2O | - |
Mycoplana ramosa | acetate + cadaverine | - |
? | |
acetylputrescine + H2O | - |
Mycoplana ramosa | acetate + putrescine | - |
? | |
BML-KI104 + H2O | a commercial acetyllysine-fluorophore substrate. Deacetylation of the acetyllysine-fluorophore substrate is followed by cleavage of the lysine-fluorophore amide bond by a protease developer, resulting in a fluorescence shift | Mycoplana ramosa | acetate + ? | - |
? | |
additional information | the fluorophore Ac-Arg-His-Lys(Ac)-Lys(Ac)-aminomethylcoumarin is a poor substrate for APAH | Mycoplana ramosa | ? | - |
? | |
N1-acetylspermidine + H2O | - |
Mycoplana ramosa | acetate + spermidine | - |
? | |
N1-acetylspermine + H2O | - |
Mycoplana ramosa | acetate + spermine | - |
? | |
N8-acetylspermidine + H2O | - |
Mycoplana ramosa | acetate + spermidine | - |
? |
Synonyms | Comment | Organism |
---|---|---|
acetylpolyamine amidohydrolase | - |
Mycoplana ramosa |
APAH | - |
Mycoplana ramosa |
polyamine deacetylase | - |
Mycoplana ramosa |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
25 | - |
assay at | Mycoplana ramosa |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
8.2 | - |
assay at | Mycoplana ramosa |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000068 | - |
pH 8.2, 25°C | Mycoplana ramosa | 7-amino-N-hydroxyheptanamide | |
0.00013 | - |
pH 8.2, 25°C | Mycoplana ramosa | 6-amino-N-hydroxyhexanamide | |
0.00015 | - |
pH 8.2, 25°C | Mycoplana ramosa | 8-amino-N-hydroxyoctanamide | |
0.00017 | - |
pH 8.2, 25°C | Mycoplana ramosa | 5-amino-N-hydroxypentanamide | |
0.00027 | - |
pH 8.2, 25°C | Mycoplana ramosa | 7-[(3-aminopropyl)amino]-1,1,1-trifluoroheptan-2-one | |
0.00039 | - |
pH 8.2, 25°C | Mycoplana ramosa | 6-[(3-aminopropyl)amino]-N-hydroxyhexanamide | |
0.026 | - |
pH 8.2, 25°C | Mycoplana ramosa | 5-[(3-aminopropyl)amino]pentane-1-thiol |
General Information | Comment | Organism |
---|---|---|
evolution | acetylpolyamine amidohydrolase (APAH) from Mycoplana ramosa is a zinc-dependent polyamine deacetylase that shares approximately 20% amino acid sequence identity with human histone deacetylases | Mycoplana ramosa |
additional information | proposed mechanism of APAH, overview. The substrate binding mode is based on the complex of N8-acetylspermidine with the inactive mutant APAH H159A (PDB entry 3Q9C), and the binding of the tetrahedral intermediate is mimicked by the binding of trifluoromethylketone inhibitor 1 | Mycoplana ramosa |
physiological function | polyamines are essential aliphatic polycations that bind to nucleic acids and accordingly are involved in a variety of cellular processes. Polyamine function can be regulated by acetylation and deacetylation, just as histone function can be regulated by lysine acetylation and deacetylation | Mycoplana ramosa |