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Identification of a botulinum neurotoxin A protease inhibitor displaying efficacy in a cellular model

Grant E Boldt1, Lisa M Eubanks, Kim D Janda

  • 1Department of Chemistry and Immunology, Skaggs Institute for Chemical Biology, Worm Institute for Research Medicine (WIRM), Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.

Chemical Communications (Cambridge, England)
|July 21, 2006
PubMed

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Directly acting muscle relaxants like dantrolene and botulinum toxin (BoNT) have distinct mechanisms and applications. Dantrolene, a hydantoin derivative, acts on the ryanodine receptor (RYR1) in skeletal muscle cells. RYR1 are calcium channels present at the sarcoplasmic reticulum membrane. In response to excitation, they release calcium ions from the sarcoplasmic reticulum to the cytosol. Calcium promotes actin-myosin-mediated contraction of muscles.
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