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Sekridova A.V.,Russian Cardiology Research | Sidorova M.V.,Russian Cardiology Research | Az'muko A.A.,Russian Cardiology Research | Molokoedov A.S.,Russian Cardiology Research | And 5 more authors.
Russian Journal of Bioorganic Chemistry | Year: 2010

Myosin light chain kinase (MLCK) is a key regulator of various forms of cellular mobility, in particular, endothelial and epithelial permeability. The membrane-penetrative peptide (H-RKKYKYRRK- NH2, Z-PIK) is one of the potential MLCK nhibitors for use in humans. Five analogs of Z-PIK were synthesized by the solid phase method of peptide synthesis using Fmoc echnology. According to 1H NMR, these analogs exhibited increased stability towards degradation in blood plasma. One of the ynthesized peptides, Z-[MeArg1]PIK, inhibited MLCK activity in vitro, and the inhibition efficacy of Z-[MeArg1]PIK was equal to hat of Z-PIK. The inhibitory effect of the other analogs was lower than that of Z-PIK. The Z-PIK analog that consisted of - mino acids was the least active. Thus, we demonstrated the possibility of creating an effective peptide inhibitor of MLCK with ncreased stability against biodegradation. Such a peptide inhibitor is a promising compound for further pharmacological studies. © Pleiades Publishing, Ltd., 2010.

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