Conjugated peptide nucleic acids having enhanced cellular uptake
AssigneePeter E. Neilsen
InventorsPeter E. Neilsen, Helle Knudsen
Life of this patent
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Abstract
Peptide nucleic acids conjugated to lipophilic groups and incorporated into liposomes exhibit enhanced cellular uptake and distribution. Cellular uptake and distribution of peptide nucleic acids also increases with the introduction of an amino acid side chain into the backbone of peptide nucleic acids. Methods of modulating cellular uptake and methods for treating animals are provided. The peptide nucleic acids of the invention comprise naturally-occurring nucleobases and non-naturally-occurring nucleobases attached to a polyamide backbone.
Claims14
A peptide nucleic acid having formula:
- wherein:
- each L is, independently, a naturally-occurring nucleobase or a non-naturally-occurring nucleobase;
- each R7′ hydrogen or the side chain of a naturally-occurring or non-naturally-occurring amino acid, at least one R7′ being the side chain of a naturally-occurring or non-naturally-occurring amino acid;
- Rh is OH, NH2, or NHLysNH2;
- each of Ri and Rj is, independently, an adamantoyl group or an amino acid labeled with a fluorescent group;
- or Ri and Rj, together, are an adamantoyl group;
- and
- n is an integer from 1 to 30.
A composition comprising a peptide nucleic acid incorporated into a liposome, said peptide nucleic acid having formula:
- wherein:
- each L is, independently, a naturally-occurring nucleobase or a non-naturally-occurring nucleobase;
- each R7′ is hydrogen or the side chain of a naturally-occurring or non-naturally-occurring amino acid, at least one R7′ being the side chain of a naturally-occurring or non-naturally-occurring amino acid;
- Rh is OH, NH2, or NHLysNH2;
- each of Ri and Rj is, independently, an adamantoyl group or an amino acid labeled with a fluorescent group;
- or Ri and Rj, together, are an adamantoyl group;
- and
- n is an integer from 1 to 30.
Dependencies are inferred from the claim text.