Design, synthesis and DNA binding properties of orthogonally positioned diamino containing polyamide f-IPI

Babu B; Liu Y; Plaunt A; Riddering C; Ogilvie R; Westrate L; Davis R; Ferguson A; Mackay H; Rice T; Chavda S; Wilson D; Lin SC; Kiakos K; Hartley JA; Lee M

Biochemical and Biophysical Research Communications, Vol.404, No.3, 848-852, 2011

DOI10.1016/j.bbrc.2010.12.073 Export Citation

Design, synthesis and DNA binding properties of orthogonally positioned diamino containing polyamide f-IPI

Babu B, Liu Y, Plaunt A, Riddering C, Ogilvie R, Westrate L, Davis R, Ferguson A, Mackay H, Rice T, Chavda S, Wilson D, Lin SC, Kiakos K, Hartley JA, Lee M

An orthogonally positioned diamino/dicationic polyamide f-IPI 2 was synthesized. It has enhanced binding affinity, and it showed comparable sequence specificity to its monoamino/monocationic counterpart f-IPI 1. Results from CD and DNase I footprinting studies confirmed the minor groove binding and selectivity of polyamides 1 and 2 for the cognate sequence 5'-ACGCGT-3'. SPR studies provided their binding constants: 2.4 x 10(8) M-1 for diamino 2, which is similar to 4 times higher than 5.4 x 10(7) M-1 for its monoamino analogue 1. (C) 2010 Elsevier Inc. All rights reserved.

Keywords:Polyamides;Minor groove;Gene regulation;DNA binding;ACGCGT