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Table 1 Up-Regulated Human Peripheral Blood Biomarkers of LXR-623 Activity

From: Discovery and implementation of transcriptional biomarkers of synthetic LXR agonists in peripheral blood cells

Gene Symbol

Gene Title

Fold Change

p-Value

ABCG1

ATP-binding cassette, sub-family G (WHITE), member 1

43.83

7.9E-08

SCD

stearoyl-CoA desaturase (delta-9-desaturase)

24.59

1.4E-07

ABCA1

ATP-binding cassette, sub-family A (ABC1), member 1

19.54

7.0E-08

APOC1

apolipoprotein C-I

13.37

2.5E-07

SREBF1

sterol regulatory element binding transcription factor 1

6.60

2.7E-03

PLTP

phospholipid transfer protein

5.81

9.0E-05

APOC2

apolipoprotein C-II

4.17

4.2E-06

LDLR

low density lipoprotein receptor (familial hypercholesterolemia)

3.91

2.4E-04

NR1H3

nuclear receptor subfamily 1, group H, member 3

3.85

1.0E-03

FADS1

fatty acid desaturase 1

3.01

3.9E-05

APOE

apolipoprotein E

2.85

1.6E-02

  1. Selected genes changed significantly in human PBMC following ex vivo treatment with LXR-623. Peripheral blood mononuclear cells were purified from normal human donors (n = 4) and treated in culture with either vehicle (0.1% DMSO) or 2 uM LXR-623 for 18 hours. RNA purified from these PBMC cultures was profiled using Affymetrix HG U133 Plus 2.0 arrays to evaluate the genes that are regulated in peripheral blood cells by LXR-623. Shown is a list of genes associated with reverse cholesterol transport and lipoprotein metabolism that were significantly changed in human PBMC by treatment with LXR-623, along with fold-change and statistical significance.