Author/Authors :
Nahoum G Anthony، نويسنده , , Keith R Fox، نويسنده , , Blair F Johnston، نويسنده , , Abedawn I Khalaf، نويسنده , , Simon P. MacKay، نويسنده , , Iain S McGroarty، نويسنده , , John A Parkinson، نويسنده , , Graham G Skellern، نويسنده , , Colin J. Suckling، نويسنده , , Roger D. Waigh، نويسنده ,
Abstract :
Footprinting, capillary electrophoresis, molecular modelling and NMR studies have been used to examine the binding of a short polyamide to DNA. This molecule, which contains an isopropyl-substituted thiazole in place of one of the N-methylpyrroles, is selective for the sequence 5′-ACTAGT-3′ to which it binds with high affinity. Two molecules bind side-by-side in the minor groove, but their binding is staggered so that the molecule reads six base pairs, unlike the related natural products, which tend to bind to four-base-pair sequences. The result suggests that high affinity and selectivity may be gained without resort to very large molecules, which may be difficult to deliver to the site of action.
