Table 1 FRET stabilization temperatures (ΔTm) of KRAS32R, UTR-1, UTR-2 and F21T G4s (0.2 μM) stabilized by IQc derivatives 2a, 2d and 3e (1 μM). Apparent association constants (Ka) and Hill constants (h) of the binding of 2a, 2d and 3e with the KRAS G4 (KRAS21R) and with double-stranded DNA (26ds), obtained from spectrofluorimetric titration assays

From: KRAS oncogene repression in colon cancer cell lines by G-quadruplex binding indolo[3,2-c]quinolines

 

ΔTm (°C)a

Ka × 106 (M−1)b/hc

KRAS32R

UTR-1

UTR-2

F21T

KRAS21R

26ds

2a

   

5.6

1.7/--

0.8/--

2d

10.7

5.1

2.0

17.7

4.4/2.0

2.8/1.5

3e

17.0

15.7

9.9

30.7

8.6/2.4

3.2/2.5

  1. a)SD ≤ 0.2°C;
  2. b)SD ≤ 0.2 × 106 M−1;
  3. c)SD ≤ 0.3.
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