Appeal No. 2003-0395 Page 3
Application No. 09/374,704
DNA-binding can be achieved for a variety of transcription factors” (id., pages 1-2).
The present “invention relates to polyamides which bind to pre-determined sites
of the minor groove of double-stranded DNA and have an "-amino acid domain
(“positive patch”) capable of inhibiting the activity of major groove DNA-binding proteins”
(id., page 1). “[T]he positive patch comprises a rigid group joined to a positively
charged group. The rigid group positions the positively charged group such that” (id.,
page 17) “[the] positive patch [ ], upon binding of the polyamide to the minor groove of a
DNA molecule, is able to contact nucleotides in the major groove of [the] DNA molecule
. . . alter[ing] the conformation of [the] DNA molecule such that the function of a
conformation-dependent DNA binding protein is inhibited” (id., page 6).
DISCUSSION
Claim 1 is directed to a polyamide molecule comprising (1) one or more amino
acids selected from the group consisting of N-methylpyrrole, 3-hydroxy-N-methylpyrrole
and N-methylimidazole; and (2) a ”positive patch consisting of a rigid group adjacent to
a positively charged group,” wherein the rigid group comprises a first amino acid
(arginine, proline, lysine or hydroxyproline) and a second amino acid (proline, glycine,
serine, threonine, leucine, isoleucine, valine, alanine or hydroxyproline). Claim 8
specifies that the positive patch comprises the amino acid sequence Arg-Pro-Arg.
Swalley, Parks and Trauger describe various synthetic polyamides, containing N-
methylpyrrole (Py) and N-methylimidazole residues in defined sequences, which
recognize specific minor groove DNA sequences. None of the synthetic polyamides
includes the “positive patch consisting of a rigid group adjacent to a positively charged
Page: Previous 1 2 3 4 5 6 7 8 Next
Last modified: November 3, 2007