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Suppression of vascular endothelium hyperpermeability by cell-permeating peptide inhibitors of myosin light chain kinase

  • Molecular Biophysics
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Abstract

Novel peptides originating from the peptide inhibitor of myosin light chain kinase (MLCK), L-PIK (Arg-Lys-Lys-Tyr-Lys-Tyr-Arg-Arg-Lys), have been studied for their ability to attenuate the thrombin-induced hyperpermeability of an endothelial cell monolayer in culture. Peptides [NαMeArg1]-Lys-Lys-Tyr-Lys-Tyr-Arg-(D)Arg8-Lys and H-Arg(NO2)Lys-Lys-Tyr-Lys-Tyr-Arg-Arg-Lys-NH2 (designated PIK2 and PIK4, respectively) appeared to be the most effective inhibitors of endothelial cell monolayer hyperpermeability, and surpassed other known peptide inhibitors of MLCK derived from original L-PIK. Our results validate PIK2 and PIK4 as the leading molecules for the development of novel drugs intended to counteract pathological hyperpermeability of vascular endothelium.

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Correspondence to V. P. Shirinsky.

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Original Russian Text © A.Y. Khapchaev, M.V. Samsonov, O.A. Kazakova, E.L. Vilitkevich, M.V. Sidorova, A.A. Az’muko, A.S. Molokoedov, Zh.D. Bespalova, V.P. Shirinsky, 2012, published in Biofizika, 2012, Vol. 57, No. 5, pp. 764–770.

Translation of the text provided by the authors; redaction imposed solely for consistency and comprehensibility.

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Khapchaev, A.Y., Samsonov, M.V., Kazakova, O.A. et al. Suppression of vascular endothelium hyperpermeability by cell-permeating peptide inhibitors of myosin light chain kinase. BIOPHYSICS 57, 587–591 (2012). https://doi.org/10.1134/S0006350912050089

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  • DOI: https://doi.org/10.1134/S0006350912050089

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