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Literature summary for 2.7.8.7 extracted from
- Structure, biochemistry, and inhibition of essential 4'-phosphopantetheinyl transferases from two species of Mycobacteria (2014), ACS Chem. Biol., 9, 1939-1944.
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| recombinant expression of enzyme PptT as maltose-binding-protein fusion protein | Mycobacterium tuberculosis |
| recombinant expression of enzyme PptT as maltose-binding-protein fusion protein | Mycobacterium ulcerans |
Crystallization (Commentary)
| Crystallization (Comment) | Organism |
|---|---|
| purified recombinant MBP-fusion enzyme, X-ray diffraction structure determination and analysis at 1.59 A resolution | Mycobacterium tuberculosis |
| purified recombinant MBP-fusion enzyme, X-ray diffraction structure determination and analysis at 1.65 A resolution | Mycobacterium ulcerans |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| D114N | site-directed mutagenesis, the mutation eliminates the negative charge of one of the putative Mg2+ ligands, also abolishes phosphopantetheinylation activity of PptT, inactive mutant | Mycobacterium tuberculosis |
| E109D | site-directed mutagenesis, inactive mutant, no measurable catalytic activity | Mycobacterium tuberculosis |
| E116Q | site-directed mutagenesis, the mutant shows 500fold reduced activity compared to the wild-type enzyme | Mycobacterium tuberculosis |
| E157Q | site-directed mutagenesis, removal of the negative charge associated with the putative Mg2+ ligand/general base abolishes phosphopantetheinylation activity, inactive mutant | Mycobacterium tuberculosis |
| R48A | site-directed mutagenesis, the mutation disrupts 3'-phosphate binding, the activity is reduced by 20fold compared to the wild-type enzyme | Mycobacterium tuberculosis |
| R56A | site-directed mutagenesis, the mutation disrupts 3'-phosphate binding, the activity is reduced by 100fold compared to the wild-type enzyme | Mycobacterium tuberculosis |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 2'-deoxy-adenosine-3',5'-bisphosphate | - |
Mycobacterium tuberculosis |  |
| 6-nitroso-benzopyrone | - |
Mycobacterium tuberculosis | |
| adenosine-3',5'-bisphosphate | - |
Mycobacterium tuberculosis | |
| Bay 11-7085 | - |
Mycobacterium tuberculosis | |
| Calmidazolium | - |
Mycobacterium tuberculosis | |
| CoA | - |
Mycobacterium tuberculosis | |
| guanidinyl-naltrindole | - |
Mycobacterium tuberculosis | |
| additional information | no or poor inhibition by Bay 11-7085, benserazide, (-)-ephedrine hemisulfate, and mitoxantrone | Mycobacterium tuberculosis | |
| PD 404182 | - |
Mycobacterium tuberculosis | |
| sanguinarine | - |
Mycobacterium tuberculosis | |
| SCH-202676 | - |
Mycobacterium tuberculosis | |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Mg2+ | required | Mycobacterium tuberculosis | |
| Mg2+ | required | Mycobacterium ulcerans | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| CoA-[4'-phosphopantetheine] + apo-[acyl-carrier protein] | Mycobacterium tuberculosis | - |
adenosine 3',5'-bisphosphate + holo-[acyl-carrier protein] | - |
? | |
| CoA-[4'-phosphopantetheine] + apo-[acyl-carrier protein] | Mycobacterium ulcerans | - |
adenosine 3',5'-bisphosphate + holo-[acyl-carrier protein] | - |
? | |
| CoA-[4'-phosphopantetheine] + apo-[acyl-carrier protein] | Mycobacterium tuberculosis H37Rv | - |
adenosine 3',5'-bisphosphate + holo-[acyl-carrier protein] | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Mycobacterium tuberculosis | P9WQD3 | - |
- |
| Mycobacterium tuberculosis H37Rv | P9WQD3 | - |
- |
| Mycobacterium ulcerans | A0PU93 | strain Agy99 | - |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| recombinant MBP-fusion enzyme | Mycobacterium tuberculosis |
| recombinant MBP-fusion enzyme | Mycobacterium ulcerans |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| CoA-[4'-phosphopantetheine] + apo-[acyl-carrier protein] | - |
Mycobacterium tuberculosis | adenosine 3',5'-bisphosphate + holo-[acyl-carrier protein] | - |
? | |
| CoA-[4'-phosphopantetheine] + apo-[acyl-carrier protein] | - |
Mycobacterium ulcerans | adenosine 3',5'-bisphosphate + holo-[acyl-carrier protein] | - |
? | |
| CoA-[4'-phosphopantetheine] + apo-[acyl-carrier protein] | - |
Mycobacterium tuberculosis H37Rv | adenosine 3',5'-bisphosphate + holo-[acyl-carrier protein] | - |
? | |
Subunits
| Subunits | Comment | Organism |
|---|---|---|
| More | enzyme MuPPT possesses a pseudodimeric fold characteristic of Sfp-type PPTases, three-dimensional structure comparisons, modeling, overview | Mycobacterium ulcerans |
| More | enzyme PptT possesses a pseudodimeric fold characteristic of Sfp-type PPTases, three-dimensional structure comparisons, modeling, overview | Mycobacterium tuberculosis |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| 4'-phosphopantetheinyl transferase | - |
Mycobacterium tuberculosis |
| 4'-phosphopantetheinyl transferase | - |
Mycobacterium ulcerans |
| MuPPT | - |
Mycobacterium ulcerans |
| PPTase | - |
Mycobacterium tuberculosis |
| PPTase | - |
Mycobacterium ulcerans |
| PptT | - |
Mycobacterium tuberculosis |
| Sfp-type PPTase | - |
Mycobacterium tuberculosis |
| Sfp-type PPTase | - |
Mycobacterium ulcerans |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.0005 | - |
with substrate MAS, recombinant enzyme, pH and temperature not specified in the publication | Mycobacterium tuberculosis | SCH-202676 | |
| 0.00078 | - |
with substrate VibB, recombinant enzyme, pH and temperature not specified in the publication | Mycobacterium tuberculosis | adenosine-3',5'-bisphosphate | |
| 0.0008 | - |
with substrate VibB, recombinant enzyme, pH and temperature not specified in the publication | Mycobacterium tuberculosis | SCH-202676 | |
| 0.0011 | - |
with substrate MAS, recombinant enzyme, pH and temperature not specified in the publication | Mycobacterium tuberculosis | CoA | |
| 0.0016 | - |
with substrate MAS, recombinant enzyme, pH and temperature not specified in the publication | Mycobacterium tuberculosis | adenosine-3',5'-bisphosphate | |
| 0.002 | - |
with substrate VibB, recombinant enzyme, pH and temperature not specified in the publication | Mycobacterium tuberculosis | Calmidazolium | |
| 0.0047 | - |
with substrate VibB, recombinant enzyme, pH and temperature not specified in the publication | Mycobacterium tuberculosis | CoA | |
| 0.0049 | - |
with substrate MAS, recombinant enzyme, pH and temperature not specified in the publication | Mycobacterium tuberculosis | Calmidazolium | |
| 0.0049 | - |
with substrate MAS, recombinant enzyme, pH and temperature not specified in the publication | Mycobacterium tuberculosis | sanguinarine | |
| 0.0071 | - |
with substrate VibB, recombinant enzyme, pH and temperature not specified in the publication | Mycobacterium tuberculosis | PD 404182 | |
| 0.0074 | - |
with substrate MAS, recombinant enzyme, pH and temperature not specified in the publication | Mycobacterium tuberculosis | 2'-deoxy-adenosine-3',5'-bisphosphate | |
| 0.0085 | - |
with substrate VibB, recombinant enzyme, pH and temperature not specified in the publication | Mycobacterium tuberculosis | 2'-deoxy-adenosine-3',5'-bisphosphate | |
| 0.012 | - |
with substrate MAS, recombinant enzyme, pH and temperature not specified in the publication | Mycobacterium tuberculosis | guanidinyl-naltrindole | |
| 0.017 | - |
with substrate VibB, recombinant enzyme, pH and temperature not specified in the publication | Mycobacterium tuberculosis | 6-nitroso-benzopyrone | |
| 0.019 | - |
with substrate MAS, recombinant enzyme, pH and temperature not specified in the publication | Mycobacterium tuberculosis | PD 404182 | |
| 0.019 | - |
with substrate VibB, recombinant enzyme, pH and temperature not specified in the publication | Mycobacterium tuberculosis | guanidinyl-naltrindole | |
| 0.022 | - |
with substrate VibB, recombinant enzyme, pH and temperature not specified in the publication | Mycobacterium tuberculosis | sanguinarine | |
| 0.024 | - |
with substrate MAS, recombinant enzyme, pH and temperature not specified in the publication | Mycobacterium tuberculosis | 6-nitroso-benzopyrone | |
| 0.03 | - |
with substrate MAS, recombinant enzyme, pH and temperature not specified in the publication | Mycobacterium tuberculosis | Bay 11-7085 | |
General Information
| General Information | Comment | Organism |
|---|---|---|
| additional information | analysis and comparisons of cofactor binding and active site composition, CoA binding pocket, catalytic mechanism of PptT, overview. While important for CoA binding, Arg48 and Arg56 likely play very small roles in catalysis | Mycobacterium tuberculosis |
| additional information | analysis and comparisons of cofactor binding and active site composition, CoA binding pocket, overview | Mycobacterium ulcerans |
| physiological function | 4'-phosphopantetheinyl transferase post-translationally modifies carrier proteins with a phosphopantetheine moiety, an essential reaction. In Mycobacteria, the Sfp-type PPTase activates pathways necessary for the biosynthesis of cell wall components and small molecule virulence factors | Mycobacterium tuberculosis |
| physiological function | 4'-phosphopantetheinyl transferase post-translationally modifies carrier proteins with a phosphopantetheine moiety, an essential reaction. In Mycobacteria, the Sfp-type PPTase activates pathways necessary for the biosynthesis of cell wall components and small molecule virulence factors | Mycobacterium ulcerans |
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