abstract |
This invention relates to novel oligonucleotide-polyamide conjugates preferably having a free 3' hydroxyl moiety, and wherein the polyamide is coupled to the oligonucleotide through its carboxyl terminus. A nucleotide polymer conjugate of the formula (I): Nu-NUC-C=C-X?1-NH-X2-X3¿ where X1 is an unsubstituted or substituted C¿1?-C10 alkylene group, in which one or more carbons may optionally be replaced by -NH-, -O- or -S-; X?2¿ is a bond, or an unsubstituted or substituted C¿1?-C20 alkylene group, in which one or more carbons may optionally be replaced by -NH-, -O- or -S-; the optional substituents in X?1 or X2¿ selected from a variety of groups; X3 is an amino acid, or a polyamide linked via its carboxy terminus; NUC is a nucleoside group of any one of formulas (a), (b), (c), (d) where ← indicates the bond to the -C=C- group in formula (I), and X4 is a sugar group of formula (e) where the 5' oxygen is linked to Nu, and X?5 and X6¿ are each independently H or OR, where R is H, a protecting group, or a solid phase matrix, and Nu is an oligonucleotide. Methods of preparing these compounds, and various uses, for example, as PCR primers, or as a substrate for DNA or RNA polymerase, are also disclosed. |