AI Article Synopsis
- Botulinum neurotoxin A (BoNT/A) is the most toxic substance and poses a threat as a potential bioweapon due to the lack of approved treatments for exposure.
- Previous research showed that hydroxamic acid prodrug carbamates can help increase the cellular uptake of BoNT/A, effectively inhibiting its action.
- The current study builds on this by conducting molecular modeling of BoNT/A and creating a library of new hydroxamic acid derivatives to evaluate their effectiveness in blocking the toxin in both lab and cellular environments.
Article Abstract
Botulinum neurotoxin A (BoNT/A) is the most potent toxin known. Unfortunately, it is also a potential bioweapon in terrorism, which is without an approved therapeutic treatment once cellular intoxication takes place. Previously, we reported how hydroxamic acid prodrug carbamates increased cellular uptake, which translated to successful inhibition of this neurotoxin. Building upon this research, we detail BoNT/A protease molecular modeling studies accompanied by the construction of small library of hydroxamic acids based on 2,4-dichlorocinnamic hydroxamic acid scaffold and their carbamate prodrug derivatization along with the evaluation of these molecules in both enzymatic and cellular models.
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Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3919520 | PMC |
| http://dx.doi.org/10.1016/j.bmc.2013.11.053 | DOI Listing |
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