Identification of the ability of highly charged nanomolar inhibitors of protein kinases to cross plasma membranes and carry a protein into cells

A fluorescently labeled adenosine–oligoarginine conjugate (ARC), nanomolar bisubstrate analogue-type inhibitor of basophilic protein kinases PKA and PKC, readily enters cells of different origin and localizes into cytoplasm and nucleus. Moreover, the biotinylated derivative of ARC is able to deliver...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2002-08, Vol.12 (16), p.2117-2120
Main Authors: Uri, Asko, Raidaru, Gerda, Subbi, Juhan, Padari, Kärt, Pooga, Margus
Format: Article
Language:English
Subjects:
Adenosine - analogs & derivatives
Adenosine - chemistry
Adenosine - metabolism
Adenosine - pharmacology
Arginine - analogs & derivatives
Arginine - chemistry
Arginine - metabolism
Arginine - pharmacology
Avidin - metabolism
Biological and medical sciences
Biotinylation
Cell Membrane - metabolism
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - metabolism
Enzyme Inhibitors - pharmacology
Fluorescent Dyes
Humans
Medical sciences
Miscellaneous
Molecular Structure
Pharmacology. Drug treatments
Protein Kinase Inhibitors
Protein Transport
Temperature
Tumor Cells, Cultured
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Summary:A fluorescently labeled adenosine–oligoarginine conjugate (ARC), nanomolar bisubstrate analogue-type inhibitor of basophilic protein kinases PKA and PKC, readily enters cells of different origin and localizes into cytoplasm and nucleus. Moreover, the biotinylated derivative of ARC is able to deliver avidin, a non-covalently attached protein cargo, into cells. Graphic
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(02)00337-2