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Table 1 Coherence between sensor inducibility and cellular proliferation inhibition by the vitamin D3 analogues

From: A Sleeping Beauty DNA transposon-based genetic sensor for functional screening of vitamin D3 analogues

 

Vitamin D3 compound

 

Calcitriol

Alfacalcidol

Atocalcitol

Calcipotriol

GS 1750

GS 1590

GS 1725

KH 1230

EB 1213

Relative IC50 -1 (1)

1.0

1.1

1.6

2.9

2.9

32.3

35.7

76.9

250

Relative potency (2) Clone #18

1.0

0.6

2.7

1.0

7.2

7.9

6.0

5.5

9.2

Relative potency (2) Clone #7

1.0

3.3

4.2

3.3

9.1

13.5

12.7

8.9

13.2

  1. (1) The half maximal inhibitory concentration (IC50) is a measure of the capability of the compounds to inhibit proliferation of HaCaT cells. For a direct comparison, the inverse value (IC50-1) is depicted here normalized to the response obtained during calcitriol exposure. IC50 values were measured for drug concentrations ranging from 10-11 to 10-7 M.
  2. (2) The relative capacity of each compound to induce d2eGFP expression from the sensor is shown for each of the two clones #7 and #18 (data derived from figure 4). Induction of d2eGFP was measured at a drug concentration of 10-7 M.
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BMC Biotechnology

ISSN: 1472-6750

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