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Conotoxin engineering: dual pharmacophoric noradrenaline transport inhibitor/integrin binding peptide with improved

Zoltan Dekan1, Ching-I Anderson Wang, Robert K Andrews

  • 1Institute for Molecular Bioscience, The University of Queensland, St Lucia 4072, Queensland, Australia.

Organic & Biomolecular Chemistry
|May 15, 2012
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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