title: [Suppression of vascular endothelium hyperpermeability by cell-permeating peptide inhibitors of myosin light chain kinase].
abstract: Novel peptides originating from the peptide inhibitor of myosin light chain kinase, L-PIK (Arg-Lys-Lys-Tyr-Lys-Tyr-Arg-Arg-Lys), have been studied for ability to attenuate the thrombin-induced hyperpermeability of endothelial cell monolayer in culture. Peptides [NalphaMeArg1]-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 hyperpermebility, and surpassed other known peptide inhibitors of myosin light chain kinase 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.
authors.forename: A Iu
authors.initials: AIu
authors.lastname: Khapchaev
authors.forename: M V
authors.initials: MV
authors.lastname: Samsonov
authors.forename: O A
authors.initials: OA
authors.lastname: Kazakova
authors.forename: E L
authors.initials: EL
authors.lastname: Vilitkevich
authors.forename: M V
authors.initials: MV
authors.lastname: Sidorova
authors.forename: A A
authors.initials: AA
authors.lastname: Az'muko
authors.forename: A S
authors.initials: AS
authors.lastname: Molokoedov
authors.forename: Zh D
authors.initials: ZhD
authors.lastname: Bespalova
authors.forename: V P
authors.initials: VP
authors.lastname: Shirinskiĭ
mesh_terms: D000595:Amino Acid Sequence; D002199:Capillary Permeability / Q000187:drug effects*; D002460:Cell Line; D015194:Diffusion Chambers, Culture; D017097:Electric Impedance; D042783:Endothelial Cells / Q000166:cytology / Q000187:drug effects* / Q000201:enzymology; D004730:Endothelium, Vascular / Q000166:cytology / Q000187:drug effects* / Q000201:enzymology; D016650:Fluorescein-5-isothiocyanate / Q000031:analogs & derivatives; D006801:Humans; D007700:Kinetics; D008969:Molecular Sequence Data; D009219:Myosin-Light-Chain Kinase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D010455:Peptides / Q000138:chemical synthesis / Q000494:pharmacology*; D012709:Serum Albumin; D013050:Spectrometry, Fluorescence; D013329:Structure-Activity Relationship; D013917:Thrombin / Q000494:pharmacology
chemical_list: C518288:FITC-albumin; D010455:Peptides; D012709:Serum Albumin; D009219:Myosin-Light-Chain Kinase; D013917:Thrombin; D016650:Fluorescein-5-isothiocyanate