Oligonucleotides conjugated to protein-binding drugs
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United States of America Patent
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Dec 2, 2003
Grant Date -
N/A
app pub date -
Jun 15, 1999
filing date -
Jun 15, 1999
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Abstract
Ligand-conjugated oligomeric compounds are described wherein ligands are conjugated to one or more sites on an oligomeric compound including the 2'-, 3'-, 5'-, nucleobase and internucleotide linkage sites. The ligand can be attached via an optional linking group. Ligands are selected for conjugation that bind to one or more cellular, serum or vascular proteins imparting enhanced pharmacokinetic properties to the resulting ligand-conjugated oligomeric compounds. Also provided are methods for increasing the concentration of an oligonucleotide in serum and methods for increasing the capacity of serum for an oligonucleotide. Further, methods for increasing the binding of an oligonucleotide to a portion of the vascular system is described. Also provided are methods for promoting cellular uptake of an oligonucleotide in cells.
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