Protein Variants | Comment | Organism |
---|---|---|
additional information | an atoxic derivative of BoNT/A (BoNT/A ad) as a full-length 150 kDa molecule consisting of a 50 kDa light chain and a 100 kDa heavy chain joined by a disulfide bond and metalloprotease-inactivating point mutations (E224A/Y366A) in the light chain. Studies in neuronal cultures demonstrates that the mutant is unable to cleave SNAP25, and that it effectively competes with wild-type BoNT/A for binding to endogenous neuronal receptors. In vivo studies indicate accumulation of the mutant (BoNT/A ad) at the neuromuscular junction of the mouse diaphragm. Toxicity of the mutant BoNT/A ad is reduced by 100000fold relative to wild-type BoNT/A | Clostridium botulinum |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
GRKKRRQRRRPPQC | 90% inhibition | Clostridium botulinum | |
additional information | a tetrapeptide provides an optimum length as the most efficient peptide inhibitor that binds at the active site normally occupied by the substrate. The peptides survive within neurons for at least 40 h and inhibit BoNT/A activity within two primary neuronal cells without showing any apparent cellular toxicity | Clostridium botulinum | |
RRGC | 0.02 mM, 95% inhibition, most potent inhibitor. When assayed in the presence of dithiothreitol, the inhibitory effect is drastically reduced | Clostridium botulinum | |
RRGF | 0.02 mM, 95% inhibition | Clostridium botulinum | |
RRGI | 0.02 mM, 90% inhibition | Clostridium botulinum | |
RRGL | 0.02 mM, 95% inhibition | Clostridium botulinum | |
RRGM | 0.02 mM, 90% inhibition | Clostridium botulinum |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Clostridium botulinum | - |
- |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
SNAP-25 + H2O | - |
Clostridium botulinum | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
BoNT/A | - |
Clostridium botulinum |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.4 | - |
assay at | Clostridium botulinum |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.000096 | - |
GRKKRRQRRRPPQC | pH 7.4, 37°C | Clostridium botulinum | |
0.000158 | - |
RRGC | pH 7.4, 37°C | Clostridium botulinum | |
0.000358 | - |
RRGF | pH 7.4, 37°C | Clostridium botulinum | |
0.000664 | - |
RRGC | pH 7.4, 37°C | Clostridium botulinum | |
0.000786 | - |
RRGI | pH 7.4, 37°C | Clostridium botulinum | |
0.000845 | - |
RRGM | pH 7.4, 37°C | Clostridium botulinum |