Peptide nucleic acids having enhanced binding affinity, sequence specificity and solubility
OwnerOle Buchardt, deceased, by Dorte Buchardt, representative +3inventors
InventorsOle Buchardt, deceased, by Dorte Buchardt, representative, Michael Egholm, Peter Eigil Nielsen, Rolf Henrik Berg
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Abstract
A novel class of compounds, known as peptide nucleic acids, bind complementary DNA and RNA strands more strongly than a corresponding DNA strand, and exhibit increased sequence specificity and solubility. The peptide nucleic acids comprise ligands selected from a group consisting of naturally-occurring nucleobases and non-naturally-occurring nucleobases attached to a polyamide backbone, and contain C.sub.1 -C.sub.8 alkylamine side chains. Methods of enhancing the solubility, binding affinity and sequence specificity of PNAs are provided.
Claims10
A method for enhancing the solubility of a peptide nucleic acid by incorporating C.sub.1 -C.sub.8 alkylamine side chain in said peptide nucleic acid having the formula:
- ##STR3## wherein:
- each L is independently selected from a group consisting of naturally-occurring nucleobases and non-naturally-occurring nucleobases;
- each R.sup.7' is independently hydrogen or C.sub.1 -C.sub.8 alkylamine, provided that at least one R.sup.7' is C.sub.1 -C.sub.8 alkylamine;
- R.sup.h is OH, NH.sub.2 or NHLysNH.sub.2 ;
- R.sup.i is H, COCH.sub.3 or t-butoxycarbonyl;
- and
- n is an integer from 1 to 30.
Dependencies are inferred from the claim text.