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Functional implications of modifying RyR-activating peptides for membrane permeability

Dulhunty, Angela; Cengia, Louise; Young, Jaqui; Pace, Suzy M; Lamb, Graham; Harvey, Peta; Chan, Yao-ban; Wimmer, Norbert; Toth, Istvan; Casarotto, Marco


Our aim was to determine whether lipoamino acid conjugation of peptides that are high-affinity activators of ryanodine receptor (RyR) channels would (a) render the peptides membrane permeable, (b) alter their structure or (a) reduce their activity. The peptides correspond to the A region of the II-III loop of the skeletal dihydropyridine receptor. The lipoamino acid conjugation increased the apparent permeability of the peptide across the Caco-2 cell monolayer by up to ∼20-fold. Nuclear...[Show more]

CollectionsANU Research Publications
Date published: 2005
Type: Journal article
Source: British Journal of Pharmacology
DOI: 10.1038/sj.bjp.0705981


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