|
Compound
|
Off-target effects: cardiac receptor inhibition
|
On-target effects: ligand-quadruplex interaction
|
|---|
|
hERG % inhib. (10 μM)
|
B2 adrenergic % inhib. (10 μM)
|
Surface plasmon resonancea(K x 107 M-1)
|
CD study thermal stabilityd
|
|---|
|
Quadruplex (Q) DNAb
|
Duplex (D) DNAc
|
Ratio Q/D
|
Tm/°C
|
∆Tme
|
|---|
|
1
|
100
|
100
|
0.83
|
0.06
|
13.8
|
86 ± 3
|
16
|
|
2
|
42.5
|
24
|
1.5
|
0.04
|
37.5
|
89 ± 3
|
19
|
|
3
|
21
|
29
|
0.8
|
0.07
|
11.4
|
85 ± 3
|
15
|
- aBuffer solution: 10 mM HEPES, 200 mM KCl, 3 mM EDTA and 0.01% P20 surfactant with the final pH adjusted to 7.4.
- bHuman telomeric sequence 5′-d[AGGG(TTAGGG)3]-3′.
- c5′-d[CGA3T3C(CT)2GA3T3CG]-3′ hairpin sequence.
- dThermal stability data for h-Tel (anti-parallel) determined by CD in the absence and presence of compounds.
- eTm for unaligned h-Tel = 70 ± 3.
