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Literature summary for 3.4.24.69 extracted from

  • Fischer, A.; Nakai, Y.; Eubanks, L.M.; Clancy, C.M.; Tepp, W.H.; Pellett, S.; Dickerson, T.J.; Johnson, E.A.; Janda, K.D.; Montal, M.
    Bimodal modulation of the botulinum neurotoxin protein-conducting channel (2009), Proc. Natl. Acad. Sci. USA, 106, 1330-1335.
    View publication on PubMedView publication on EuropePMC
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Inhibitors

Inhibitors Comment Organism Structure
additional information semisynthetic strategy to identify inhibitors based on toosendanin, a traditional Chinese medicine reported to protect from BoNT intoxication, overview. No inhibition by deacetylted toosendanin and by toosendanin ketone and lactone analogues Clostridium botulinum
THF-toosendanin tetrahydrofuran analogue of toosendanin, selectively arrests the light chain translocation step of intoxication with subnanomolar potency, and increases the unoccluded heavy chain channel propensity to open with micromolar efficacy, inhibitory profile on light chain translocation, overview. The bimodal modulation by toosendanin depends on the dynamic interactions between channel and cargo, highlighting their tight interplay during the progression of LC transit across endosomes Clostridium botulinum
toosendanin i.e. TSDN, selectively arrests the light chain translocation step of intoxication with subnanomolar potency, and increases the unoccluded heavy chain channel propensity to open with micromolar efficacy, inhibitory profile on light chain translocation, overview. The bimodal modulation by toosendanin depends on the dynamic interactions between channel and cargo, highlighting their tight interplay during the progression of LC transit across endosomes. Toosendanin modulates both cargo-dependent and cargo-free activities of the BoNT/E protein-conducting channel Clostridium botulinum

Organism

Organism UniProt Comment Textmining
Clostridium botulinum
-
 BoNT serotypes A and E
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information usage of a single molecule assay of BoNT serotypes A and E light chain translocation through the heavy chain channel in neurons, and of BoNT intoxication assays, namely the mouse protection and the primary rat spinal cord cell assays Clostridium botulinum ?
-
 ?
SNAP-25 + H2O i.e. 25 kDa synaptosomal-associated protein, substrate of BoNT serotypes A and E Clostridium botulinum ?
-
 ?

Synonyms

Synonyms Comment Organism
BoNT
-
 Clostridium botulinum
BoNT serotype A
-
 Clostridium botulinum
BoNT serotype E
-
 Clostridium botulinum
Clostridium botulinum neurotoxin
-
 Clostridium botulinum

General Information

General Information Comment Organism
physiological function Clostridium botulinum neurotoxin is the causative agent of botulism, a neuroparalytic disease Clostridium botulinum