Design, synthesis and use of specific polyamide dna-binding...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 207/34 (2006.01) A61K 31/415 (2006.01) A61K 31/785 (2006.01) A61K 38/00 (2006.01) A61K 38/04 (2006.01) A61K 49/00 (2006.01) A61P 43/00 (2006.01) C07D 233/90 (2006.01) C07D 403/12 (2006.01) C07D 403/14 (2006.01) C07K 7/02 (2006.01) C08G 69/00 (2006.01) C08G 69/08 (2006.01) C12Q 1/68 (2006.01) C12N 15/09 (2006.01)

Patent

CA 2281930

The invention encompasses improved selective polyamides for binding to specific nucleotide sequences of double stranded DNA as well as methods for designing and synthesizing polyamide DNA binding ligands that are selective for an identified specific nucleotide sequence. The 3-hydroxy-N- methylpyrrole/N-methylpyrrole carboxamide pair specifically recognizes the T.A base pair, while the N-methylpyrrole/3-hydroxy-N-methylpyrrole pair recognizes A.T nucleotide pairs. Similarly, an N-methylimidizole/N-methylpyrrole carboxamide pair specifically recognizes the G.C nucleotide pair, and the N- methylpyrrole/N-methylimidizole carboxamide pair recognizes the C.G nucleotide pair.

L'invention concerne des polyamides sélectifs améliorés destinés à se lier à des séquences nucléotidiques spécifiques d'ADN à double brin, ainsi que des procédés pour concevoir et synthétiser des ligands à base de polyamide pour liaison à l'ADN, qui sont sélectifs vis-à-vis d'une séquence nucléotidique spécifique identifiée. La paire de carboxamides 3-hydroxy-N-méthylpyrrole/N-méthylpyrrole reconnaît la paire de bases T.A, tandis que la paire N-méthylpyrrole/3-hydroxy-N-méthylpyrrole reconnaît les paires nucléotidiques A.T. De façon similaire, une paire de carboxamides N-méthylimidizole/N-méthylpyrrole reconnaît spécifiquement la paire nucléotidique G.C, et la paire de carboxamides de N-méthylpyrrole/N-méthylimidizole reconnaît la paire nucléotidique C.G.

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