Table 3.

Fold change in expression of genes downregulated by ≥2.4-fold by JQ1 in CCA2 tumors, compared with CCA1 tumors

CCA2CCA1
GeneAccession #JQ1VCFold changeJQ1VCFold change
FASNM_000043.313.2331.45−2.3832.4182.71−2.55
BRCA2NM_000059.341.73102.2−2.451.971.971
WEE1NM_003390.27.1317.69−2.48508.96467.081.09
CDK6NM_001259.5132.33334.13−2.53115.55189.77−1.64
MYBL2NM_002466.2115.02294.82−2.56Not included
CHEK1NM_001274.291.61237.82−2.6498.43414.431.20
FGRNM_001042729.14.0710.81−2.65Not included
CDK4NM_000075.266.16192.61−2.91572.19560.11.02
MYCL1NM_001033082.17.1321.62−3.03Not included
CTGFNM_001901.2492.661505.53−3.06Not included
CDH11NM_001797.2224.95691.84−3.08Not included
MMP9NM_004994.227.4885.5−3.116.659.87−1.48
FGF2NM_002006.427.4888.45−3.2245.29144.14−3.18
FLT3NM_004119.13.059.83−3.221.1711.17
PPARGNM_138711.3160.83518.88−3.23501.94512.72−1.02
E2F1NM_005225.137.66122.84−3.26215.07248.57−1.16
MSH2NM_000251.163.11213.25−3.38704.5579.411.22
TP53NM_000546.2131.31479.57−3.65127.25107.281.19
FGFR2NM_000141.4111.97410.78−3.67123.74133.61−1.08
TEKNM_000459.216.2962.89−3.86Not included
LCKNM_001042771.117.371.74−4.15Not included
MYCNNM_005378.425.45130.7−5.1465.259.022.25
MYCNM_002467.3238.191375.81−5.78448.08578.53−1.29
TIMP3NM_000362.4352.192565.89−7.29Not included
  • NOTE: Exposure to JQ1 in vivo downregulated expression of 24 genes by ≥2.4-fold in the relatively sensitive CCA2 tumors. In contrast, JQ1 downregulated only 2 genes to this extent (FAS and FGF2) in a subset of 16 of these 24 genes in CCA1 tumors. These data indicate inhibition of expression of FAS and FGF2 are likely not associated with sensitivity to JQ1 and that expression of BRCA2, WEE1, CDK6, CHEK1, CDK4, MMP9, LFT3, PPARG, E2F1, MSH2, TP53, FGFR2, MYCN, and MYC may be BET dependent in CCA tumors.