Oligonucleotide having enhanced binding affinity

Details Oligonucleotide having enhanced binding affinity Oligonucleotide having enhanced binding affinity

1992-06-22

1996-01-23

Fleisher, Mindy B.

Organic compounds -- part of the class 532-570 series

Organic compounds

Carbohydrates or derivatives

536 231, 536 245, 552506, 552515, 552544, 552557, 552586, 552588, 552574, 552604, 552607, 552625, 552638, C07H 1512, C07H 1700, C07J 4100, C07J 3100

Patent

active

054866030

ABSTRACT:
The present invention relates to an oligonucleotide or analog thereof conjugated to a molecule comprising a structure, which structure (a) is of substantially fixed conformation; (b) contains, is directly attached to, or is attached to a carbon atom that is directly attached to, an first amine; and (c) contains, is directly attached to, or is attached to an atom that is directly attached to a phosphate, a second amine, or a cationic sulfur. In a preferred embodiment, the structure consists of at least a nonaromatic cyclic portion or substituted derivative thereof. In a specific embodiment, the structure is a nonaromatic cyclic compound. In another embodiment, the molecule is a steroid. In yet another particular aspect, the structure is an aromatic compound. In another embodiment, the structure can bind to a nucleic acid sequence in a nonintercalative manner. The invention also relates to a conjugate comprising a steroid or substituted derivative thereof containing, or attached directly or through a carbon atom to, an amine, which steroid or substituted derivative is conjugated to at least one hydrogen-phosphonate and a cation; such a conjugate may be used as an intermediate in synthesis. The oligonucleotide conjugates of the invention can have a number of uses. For example, the conjugates may be used for diagnostic purposes by detecting a nucleic acid sequence.

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