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

Asko Uri; Gerda Raidaru; Juhan Subbi; Kärt Padari; Margus Pooga

doi:10.1016/s0960-894x(02)00337-2

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

Bioorg Med Chem Lett. 2002 Aug 19;12(16):2117-20. doi: 10.1016/s0960-894x(02)00337-2.

Authors

Asko Uri¹, Gerda Raidaru, Juhan Subbi, Kärt Padari, Margus Pooga

Affiliation

¹ Institute of Organic and Bioorganic Chemistry, University of Tartu, 2 Jakobi St., 51014, Tartu, Estonia. [email protected]

PMID: 12127517
DOI: 10.1016/s0960-894x(02)00337-2

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Adenosine / analogs & derivatives*
Adenosine / chemistry*
Adenosine / metabolism*
Adenosine / pharmacology
Arginine / analogs & derivatives*
Arginine / chemistry
Arginine / metabolism*
Arginine / pharmacology
Avidin / metabolism*
Biotinylation
Cell Membrane / metabolism*
Enzyme Inhibitors / chemistry*
Enzyme Inhibitors / metabolism*
Enzyme Inhibitors / pharmacology
Fluorescent Dyes
Humans
Molecular Structure
Protein Kinase Inhibitors*
Protein Transport
Temperature
Tumor Cells, Cultured

Substances

Enzyme Inhibitors
Fluorescent Dyes
Protein Kinase Inhibitors
Avidin
Arginine
Adenosine