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Cancer epigenetics is the study of epigenetic changes to the DNA of cancer cells. These changes provide a way for cells to control and regulate gene activity without changing the genes permanently. Epigenetic control relies on small, reversible, changes to the DNA and proteins such as: DNA methylation, changes in the structure of histone proteins or gene regulation by small noncoding microRNAs. Controlling epigenetic changes may provide us with helpful tools for cancer prevention, detection, and therapy.
Library of Cancer Epigenetics Related Ligands contains 954 small ligands, some representative molecules are given below: TMP269, HDAC inhibitor; XD14, BDR inhibitor; KDM5-IN-1, KDM5 inhibitor; Progesterone, Progesterone receptor agonist.
Related terms: poly(ADP-ribose) polymerase, histone deacetylase, tankyrase, aurora kinase, bromodomain, nuclear receptor coactivator
Epigenetic process in cancer(Created by BioRender.com)
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NoteAll the compounds with solubility below 10 mM are shipped as 2 mM solutions.
Histone deacetylases (HDACs)
154
154
Number of compounds
154
Aurora kinase (Aur) family
113
113
Number of compounds
113
Poly ADP-ribose polymerases
107
107
Number of compounds
107
Bromodomain kinase (BRDK) family
80
80
Number of compounds
80
Protein arginine N-methyltransferases
50
50
Number of compounds
50
Trace amine receptor
50
50
Number of compounds
50
Non-enzymatic BRD containing proteins
34
34
Number of compounds
34
Others
33
33
Number of compounds
33
Histone acetyltransferases (HATs)
31
31
Number of compounds
31
Janus kinase (JakA) family
30
30
Number of compounds
30
Opioid receptors
28
28
Number of compounds
28
Histone demethylases
27
27
Number of compounds
27
Melatonin receptors
19
19
Number of compounds
19
Receptor tyrosine phosphatase (RTP) family
16
16
Number of compounds
16
ABCG subfamily
15
15
Number of compounds
15
CDK1 subfamily
13
13
Number of compounds
13
ABCC subfamily
12
12
Number of compounds
12
Tachykinin receptors
12
12
Number of compounds
12
ABCB subfamily
12
12
Number of compounds
12
Histone-lysine methyltransferase
12
12
Number of compounds
12
Type I RTKs: ErbB (epidermal growth factor) receptor family
9
9
Number of compounds
9
Histamine receptors
9
9
Number of compounds
9
C13: Legumain
8
8
Number of compounds
8
C1: Papain
8
8
Number of compounds
8
Lipid phosphate phosphatases
7
7
Number of compounds
7
Methyltransferases
7
7
Number of compounds
7
Inwardly rectifying potassium channels (KIR)
7
7
Number of compounds
7
SLC18 family of vesicular amine transporters
5
5
Number of compounds
5
S9: Prolyl oligopeptidase
5
5
Number of compounds
5
Orexin receptors
5
5
Number of compounds
5
Glycine receptors
5
5
Number of compounds
5
Two-pore domain potassium channels (K2P)
4
4
Number of compounds
4
C14: Caspase
3
3
Number of compounds
3
Ionotropic glutamate receptors
3
3
Number of compounds
3
NuaK subfamily
2
2
Number of compounds
2
Tau tubulin kinase (TTBK) family
2
2
Number of compounds
2
SLC7 family
2
2
Number of compounds
2
Organic anion transporters (OATs)
2
2
Number of compounds
2
Lanosterol biosynthesis pathway
2
2
Number of compounds
2
Protein tyrosine phosphatases non-receptor type (PTPN)
1
1
Number of compounds
1
1H. Liver X receptor-like receptors
1
1
Number of compounds
1
Tousled-like kinase (TLK) family
1
1
Number of compounds
1
RIO3 subfamily
1
1
Number of compounds
1
CDK4 subfamily
1
1
Number of compounds
1
M12: Astacin/Adamalysin
1
1
Number of compounds
1
Phospholipase A2
1
1
Number of compounds
1
Cyclic nucleotide-regulated channels (CNG)
1
1
Number of compounds
1
S8: Subtilisin
1
1
Number of compounds
1
Methyllysine reader proteins
1
1
Number of compounds
1
Lysophospholipid (LPA) receptors
1
1
Number of compounds
1
4A. Nerve growth factor IB-like receptors
1
1
Number of compounds
1
ClC family
1
1
Number of compounds
1
SLC19 family of vitamin transporters
1
1
Number of compounds
1
PITSLRE subfamily
1
1
Number of compounds
1
Polo-like kinase (PLK) family
1
1
Number of compounds
1
Death-associated kinase (DAPK) family
1
1
Number of compounds
1
Ryanodine receptors (RyR)
1
1
Number of compounds
1
Voltage-gated calcium channels (CaV)
1
1
Number of compounds
1
IL-6 receptor family
1
1
Number of compounds
1
EBCL-0015