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 avidin, a non-covalently attached protein cargo, into cells.
Institute of Organic and Bioorganic Chemistry, University of Tartu, 2 Jakobi St., 51014, Tartu, Estonia. asko@chem.ut.ee
Asko
A
Uri
Gerda
G
Raidaru
Juhan
J
Subbi
Kärt
K
Padari
Margus
M
Pooga
D000241:Adenosine / Q000031:analogs & derivatives* / Q000737:chemistry* / Q000378:metabolism* / Q000494:pharmacology; D001120:Arginine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D001360:Avidin / Q000378:metabolism*; D019921:Biotinylation; D002462:Cell Membrane / Q000378:metabolism*; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000378:metabolism* / Q000494:pharmacology; D005456:Fluorescent Dyes; D006801:Humans; D015394:Molecular Structure; D047428:Protein Kinase Inhibitors; D021381:Protein Transport; D013696:Temperature; D014407:Tumor Cells, Cultured
D004791:Enzyme Inhibitors; D005456:Fluorescent Dyes; D047428:Protein Kinase Inhibitors; D001360:Avidin; D001120:Arginine; D000241:Adenosine