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Literature summary for 3.4.24.69 extracted from

  • Hale, M.; Oyler, G.; Swaminathan, S.; Ahmed, S.A.
    Basic tetrapeptides as potent intracellular inhibitors of type A botulinum neurotoxin protease activity (2011), J. Biol. Chem., 286, 1802-1811.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.24.69

Protein Variants

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

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

Organism UniProt Comment Textmining
Clostridium botulinum
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
SNAP-25 + H2O
-
 Clostridium botulinum ?
-
 ?

Synonyms

Synonyms Comment Organism
BoNT/A
-
 Clostridium botulinum

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
 assay at Clostridium botulinum

Ki Value [mM]

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