Abstract
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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Adenosine / chemistry
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Cell Membrane Permeability
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Cyclic AMP-Dependent Protein Kinases / antagonists & inhibitors*
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Drug Carriers / chemical synthesis*
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Drug Carriers / pharmacokinetics
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Drug Design
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Drug Stability
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / pharmacokinetics
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HeLa Cells
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Humans
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Inhibitory Concentration 50
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Microscopy, Fluorescence
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Molecular Structure
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Peptides / chemistry*
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Polyethylene Glycols / chemistry*
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Structure-Activity Relationship
Substances
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Drug Carriers
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Enzyme Inhibitors
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Peptides
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polyarginine
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Polyethylene Glycols
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Cyclic AMP-Dependent Protein Kinases
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Adenosine