Table 3 Kinetic parameters nucleoside analogue for P1 and P2 transporters.

From: Combining tubercidin and cordycepin scaffolds results in highly active candidates to treat late-stage sleeping sickness

Compound

P1 transporter

P2 transporter

Km or Ki

ΔG0

δ(ΔG0)

Km or Ki

ΔG0

δ(ΔG0)

Adenosine

0.12 ± 0.02

−39.4

 

0.53 ± 0.02

−35.8

 

3 Cordycepin

210 ± 48a

−21.0

18.4

0.18 ± 0.02b

−38.5

−2.7

8 7-Br-TUB

4.85 ± 0.83

−30.3

9.1

1.99 ± 0.31

−32.5

3.3

9 3′-Deoxy-TUB

99.9 ± 21.7

−22.8

16.6

0.149 ± 0.03

−38.9

−3.1

10 7-Br-3′-deoxy-TUB

9.47 ± 1.4

−28.7

10.7

0.502 ± 0.14

−35.9

−0.1

  1. Km (highlighted in bold) and Ki values are in µM; ΔG0 in kJ mol−1. Km and Ki values are mean ± SEM, derived from three independent experiments (n = 3) with three replicates. δ(ΔG0) was calculated in comparison to adenosine. Source data are provided as a Source Data file.
  2. aValue was taken from ref. 29
  3. bValue was taken from ref. 18