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Table 1 On and off target profile of pentacyclic acridinium salts 1, 2 and 3

From: On and off-target effects of telomere uncapping G-quadruplex selective ligands based on pentacyclic acridinium salts

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

  1. aBuffer solution: 10 mM HEPES, 200 mM KCl, 3 mM EDTA and 0.01% P20 surfactant with the final pH adjusted to 7.4.
  2. bHuman telomeric sequence 5′-d[AGGG(TTAGGG)3]-3′.
  3. c5′-d[CGA3T3C(CT)2GA3T3CG]-3′ hairpin sequence.
  4. dThermal stability data for h-Tel (anti-parallel) determined by CD in the absence and presence of compounds.
  5. eTm for unaligned h-Tel = 70 ± 3.
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