Uncharged polynucleotide-binding polymers

• US 5,142,047 A
• Filed: 09/23/1987
• Issued: 08/25/1992
• Est. Priority Date: 03/15/1985
• Status: Expired due to Term

• Current Assignee: AntiVirals, Inc. (Sarepta Therapeutics, Inc.)
• Original Assignee: Anti-Gene Development Group
• Inventors: Summerton, James, Weller, Dwight, Stirchak, Eugene
• Primary Examiner(s): Lee, Mary C.
• Assistant Examiner(s): McKane, Joseph K.
• Application Number:
  US07/100,033
• Time in Patent Office: 1,798 Days
• Field of Search: 544/118, 544/122, 544/123
• US Class Current: 544/118
• CPC Class Codes: A61K 47/545 Heterocyclic compounds A61K47/558 takes precedence
• CPC Class Codes: A61K 47/548 Phosphates or phosphonates, e.g. bone-seeking phospholipids A61K47/544
• CPC Class Codes: A61K 47/58 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. poly[meth]acrylate, polyacrylamide, polystyrene, polyvinylpyrrolidone, polyvinylalcohol or polystyrene sulfonic acid resin
• CPC Class Codes: A61K 47/59 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
• CPC Class Codes: B01J 2219/0072 Organic compounds
• CPC Class Codes: C07H 21/00 Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
• CPC Class Codes: C07K 14/003 Peptide-nucleic acids (PNAs)
• CPC Class Codes: C12Q 1/6813 Hybridisation assays
• CPC Class Codes: C12Q 1/682 Signal amplification
• CPC Class Codes: C12Q 1/6839 Triple helix formation or other higher order conformations in hybridisation assays
• CPC Class Codes: Y02P 20/55 Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Abstract

A composition of polymer molecules effective to bind, with substantially uniform binding affinity, to a single-stranded polynucleotide containing a target sequence of bases. The polymer molecules are composed of a sequence of base-pairing moieties effective to hydrogen bond to corresponding, complementary bases in the target sequence, under selected binding conditions, and a predominantly uncharged, achiral backbone supporting the base-pairing moieties at positions and in orientations which allow hydrogen bonding between the pairing moieties of the polymer and the corresponding complementary bases in the target sequence. The composition has diagnostic uses, in a solid-support assay system, and therapeutic uses involving inhibition or inactivation of target polynucleotides.

Claims

1. A morpholino subunit of the form:

##STR4## where P is a base-pairing moiety capable of binding by Watson/Crick pairing to complementary bases in a polynucleotide, and where P is selected from the group consisting of;

##STR5## where X=F, Cl, Br, I, H, or CH₃, and ##STR6## T is H or an N-protective group.

2. A morpholino subunit of the form:

##STR7## where P is a base-pairing moiety capable of binding by Watson/Crick pairing to complementary bases in a polynucleotide, and where P is selected from the group consisting of;

##STR8## where X=F, Cl, Br, I, H, or CH₃, and ##STR9## T₁ and T₂ are each either H or an N-protective group.