Table 1.
ET-770 (the Compound 1a) |
ET-770 Derivative (the Compound 3) |
RM (the Compound 2a) |
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---|---|---|---|---|---|---|---|---|---|---|---|
Downregulated Genes (n = 426) |
Downregulated Genes (n = 417) |
Downregulated Genes (n = 274) |
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Rank | Gene Symbol | Gene Name | Fold Change | Rank | Gene Symbol | Gene Name | Fold Change | Rank | Gene Symbol | Gene Name | Fold Change |
1 |
SSBP2 |
single-stranded DNA binding protein 2 |
0.040 |
1 |
PTPRZ1 |
protein tyrosine phosphatase, receptor-type, Z polypeptide 1 |
0.043 |
1 |
PSD3 |
pleckstrin and Sec7 domain containing 3 |
0.068 |
2 |
ELMO1 |
engulfment and cell motility 1 |
0.049 |
2 |
SSBP2 |
single-stranded DNA binding protein 2 |
0.053 |
2 |
MST131 |
MSTP131 |
0.099 |
3 |
ODZ2 |
odz, odd Oz/ten-m homolog 2 (Drosophila) |
0.053 |
3 |
NLGN1 |
neuroligin 1 |
0.055 |
3 |
PLCB1 |
phospholipase C, beta 1 (phosphoinositide-specific) |
0.106 |
4 |
PRKD1 |
protein kinase D1 |
0.068 |
4 |
CD180 |
CD180 molecule |
0.068 |
4 |
EXOC6B |
exocyst complex component 6B |
0.114 |
5 |
NLGN1 |
neuroligin 1 |
0.072 |
5 |
EPHA3 |
EPH receptor A3 |
0.073 |
5 |
ELMO1 |
engulfment and cell motility 1 |
0.125 |
6 |
MLLT3 |
myeloid/lymphoid or mixed-lineage leukemia (trithorax homolog, Drosophila); translocated to, 3 |
0.072 |
6 |
PRKD1 |
protein kinase D1 |
0.075 |
6 |
DPYD |
dihydropyrimidine dehydrogenase |
0.125 |
7 |
SBF2 |
SET binding factor 2 |
0.088 |
7 |
PSD3 |
pleckstrin and Sec7 domain containing 3 |
0.080 |
7 |
DIAPH2 |
diaphanous homolog 2 (Drosophila) |
0.128 |
8 |
EPHA3 |
EPH receptor A3 |
0.089 |
8 |
ELMO1 |
engulfment and cell motility 1 |
0.084 |
8 |
PDE1C |
phosphodiesterase 1 C, calmodulin-dependent 70 kDa |
0.133 |
9 |
PSD3 |
pleckstrin and Sec7 domain containing 3 |
0.089 |
9 |
ODZ2 |
odz, odd Oz/ten-m homolog 2 (Drosophila) |
0.084 |
9 |
FAM172A |
family with sequence similarity 172, member A |
0.138 |
10 |
ERC1 |
ELKS/RAB6-interacting/CAST family member 1 |
0.094 |
10 |
CASK |
calcium/calmodulin-dependent serine protein kinase (MAGUK family) |
0.094 |
10 |
FRMD5 |
FERM domain containing 5 |
0.139 |
Upregulated Genes (n = 45) |
Upregulated Genes (n = 84) |
Upregulated Genes (n = 9) |
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Rank |
Gene Symbol |
Gene Name |
Fold Change |
Rank |
Gene Symbol |
Gene Name |
Fold Change |
Rank |
Gene Symbol |
Gene Name |
Fold Change |
1 |
OSR2 |
odd-skipped related 2 (Drosophila) |
6.10 |
1 |
AKAP5 |
A kinase (PRKA) anchor protein 5 |
6.42 |
1 |
DENND2C |
DENN/MADD domain containing 2 C |
4.28 |
2 |
HBEGF |
heparin-binding EGF-like growth factor |
5.12 |
2 |
SLC25A19 |
solute carrier family 25 (mitochondrial thiamine pyrophosphate carrier), member 19 |
4.90 |
2 |
ZNF844 |
zinc finger protein 844 |
4.07 |
3 |
AKAP5 |
A kinase (PRKA) anchor protein 5 |
4.89 |
3 |
OSR2 |
odd-skipped related 2 (Drosophila) |
4.86 |
3 |
HBEGF |
heparin-binding EGF-like growth factor |
4.02 |
4 |
CSNK1G1 |
casein kinase 1, gamma 1 |
4.69 |
4 |
ZNF844 |
zinc finger protein 844 |
4.79 |
4 |
OSR2 |
odd-skipped related 2 (Drosophila) |
3.52 |
5 |
IL1A |
interleukin 1, alpha |
4.66 |
5 |
HBEGF |
heparin-binding EGF-like growth factor |
4.63 |
5 |
LRRTM2 |
leucine rich repeat transmembrane neuronal 2 |
3.44 |
6 |
GABRQ |
gamma-aminobutyric acid (GABA) receptor, theta |
4.28 |
6 |
CDC25A |
cell division cycle 25 homolog A (S. pombe) |
4.38 |
6 |
TSPYL2 |
TSPY-like 2 |
3.28 |
7 |
ZNF844 |
zinc finger protein844 |
4.03 |
7 |
ZNF684 |
zinc finger protein 684 |
4.24 |
7 |
TLCD1 |
TLC domain containing 1 |
3.10 |
8 |
E2F2 |
E2F transcription factor 2 |
3.82 |
8 |
TLCD1 |
TLC domain containing 1 |
4.10 |
8 |
RHEBL1 |
Ras homolog enriched in brain like 1 |
3.08 |
9 |
IL17RB |
interleukin 17 receptor B |
3.79 |
9 |
GPATCH4 |
G patch domain containing 4 |
4.06 |
9 |
GABRQ |
gamma-aminobutyric acid (GABA) receptor, theta |
3.00 |
10 | B7H6 | B7 homolog 6 | 3.75 | 10 | CHAC2 | ChaC, cation transport regulator homolog 2 (E. coli) | 4.01 |
The genome-wide gene expression profile was studied on Human Gene 1.0 ST array in U373MG cells following a 24 hour-exposure to the vehicle (DMSO) or to the three chemical compounds (Figure 1) individually at the concentration of IC50. The fold changes greater than 3 or smaller than 0.3333, calculated by the expression levels in the compound-treated cells divided by those in the vehicle-treated cells, were considered as substantial upregulation or downregulation. Top ten of them are listed with gene symbol, gene name, and fold change.