An adenosine-oligoarginine conjugate (ARC) was assembled in a stepwise manner on a poly(ethylene glycol) carrier. The pegylated conjugate inhibited cAMP-dependent protein kinase with IC(50)=460 nM and the cellular uptake of its BODIPY FL derivative was demonstrated and compared to that of free ARC with fluorescence microscopy.
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Therapeutic potential of adenosine analogues and conjugates.
Pharmacol Rep
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Department of Organic Chemistry, Gdansk University of Technology, G. Narutowicza 11/12, PL 80-952 Gdańsk, Poland.
This review summarizes current knowledge of adenosine analogues and conjugates with promising therapeutic properties. Adenosine is a signaling molecule that triggers numerous physiological responses. It acts through the adenosine receptors (ARs), belonging to the family of G-protein-coupled receptors and widely distributed throughout the body.
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FEBS J
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Institute of Molecular and Cell Biology, University of Tartu, and Estonian Biocentre, Tartu, Estonia.
Aberrant regulation of protein kinases impairs normal cellular functioning and may lead to disease. The protein kinase involved in the regulation of the dynamics of the actin cytoskeleton, Rho-kinase (ROCK), phosphorylates various substrates (e.g.
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Anal Biochem
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Institute of Organic and Bioorganic Chemistry, University of Tartu, 51014 Tartu, Estonia.
Interactions between adenosine-oligoarginine conjugates (ARC), bisubstrate analog inhibitors of protein kinases, and catalytic subunits of cAMP-dependent protein kinase (cAPK Calpha) were characterized with surface-plasmon-resonance-based biosensors. ARC-704 bound to the immobilized kinase with subnanomolar affinity. The immobilization of ARC-704 to the chip surface via streptavidin-biotin complex yielded a high-affinity surface (K(D)=16nM).
View Article and Find Full Text PDFLiquid-phase synthesis of a pegylated adenosine-oligoarginine conjugate, cell-permeable inhibitor of cAMP-dependent protein kinase.
Bioorg Med Chem Lett
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Institute of Organic and Bioorganic Chemistry, University of Tartu, 2 Jakobi St., 51014, Tartu, Estonia.
An adenosine-oligoarginine conjugate (ARC) was assembled in a stepwise manner on a poly(ethylene glycol) carrier. The pegylated conjugate inhibited cAMP-dependent protein kinase with IC(50)=460 nM and the cellular uptake of its BODIPY FL derivative was demonstrated and compared to that of free ARC with fluorescence microscopy.
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Bioorg Med Chem Lett
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Institute of Organic and Bioorganic Chemistry, University of Tartu, 2 Jakobi St., 51014, Tartu, Estonia.
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.
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