Table 1. Equilibrium binding constants of polyamides to the E2-DNA binding site.
Molecule | Kd (nM) | Kia (nM) | Linkerb | Comment |
---|---|---|---|---|
PA4 | 1000 | 1000 | One | Tandem hairpin |
PA1 | 1 | 2 | Two | Tandem hairpin |
PA3 | 100 | >10 000 | NA | Single hairpin |
PA2 | 1000 | 2000 | NA | Single hairpin |
PA5 | 1 | 16 | Six | Tandem hairpin |
PA6 | 3 | 3.2 | Four | Tandem hairpin |
Netropsin | 100 | >10 000 | NA | Natural product |
NA, not applicable.
aKi is the concentration of polyamide required to reduce the amount of shifted (E2–DNA) complex by half in the presence of a fixed amount of E2dbd protein under equilibrium conditions.
bNumber of ethylene repeats in the flexible linker of a tandem hairpin polyamide.