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Complex formation between dsDNA and oligomer of cyclic heterocycles

  • US 5,998,140 A
  • Filed: 05/08/1997
  • Issued: 12/07/1999
  • Est. Priority Date: 07/31/1996
  • Status: Expired due to Fees
First Claim
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1. A cell comprising dsDNA to which is bound in the minor groove at a target site from 1 to 2 oligomers, where the oligomers are selected to provide specific binding to said dsDNA at said target site,each of said oligomers comprising organic cyclic groups of from 5 to 6 annular members, where at least 60% of the groups are heterocycles having from 1 to 3 heteroatoms, where the heteroatoms are nitrogen, oxygen and sulfur, and wherein at least 60% of the heterocycles have at least one nitrogen atom, and said heterocycles are linked by chains of 2 atoms, wherein at least some of the chains have NH,wherein at least one of said oligomers has at least 7 of said nitrogen containing heterocycles, where at least one of said heterocycles is specific for A, G, C or T, and a pair of heterocycles refers to two heterocycles paired to a complementary pair of nucleotides in said dsDNA,each oligomer comprising at least two units of 2 consecutive heterocycles which form, at the target sites, intramolecular pairs of heterocycles with itself or intermolecular pairs of heterocycles with another oligomer,where when an oligomer forms intramolecular pairs, said oligomer comprises an internal molecule which shifts the spacing of the heterocycles or forms a hairpin turn, andwhen two oligomers form intermolecular pairs, each oligomer comprises an internal aliphatic amino acid of from 2 to 6 carbon atoms, where said internal aliphatic amino acid is paired with an A or T;

  • andeach of said oligomers comprising at at least one terminus, an aliphatic amino acid of from 2 to 6 carbon atoms or an alkyl chain comprising a polar group 2 to 4 carbon atoms from the bond linking said alkyl chain to the remainder of each oligomer,where each oligomer has one or more hydrogen atoms away from the surface of said minor groove which may be substituted, wherein the total number of carbon atoms of substituents is not more than 100 carbon atoms.

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