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Literature summary for 2.1.1.37 extracted from
- Tea polyphenol (-)-epigallocatechin-3-gallate inhibits DNA methyltransferase and reactivates methylation-silenced genes in cancer cell lines (2003), Cancer Res., 63, 7563-7570.
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| (-)-epigallocatechin-3-gallate | competitive, the inhibitor can form hydrogen bonds with Pro1223, Glu1265, Cys1225, Ser1229 and Arg1309. Hypermethylation of CpG islands in the promoter regions is an important mechanism to silence the expression of many important genes in cancer. (-)-Epigallocatechin-3-gallate can inhibit DNMT activity and reactivate methylation-silenced genes in cancer cells | Homo sapiens |  |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| S-adenosyl-L-methionine + DNA | Homo sapiens | hypermethylation of CpG islands in the promoter regions is an important mechanism to silence the expression of many important genes in cancer | S-adenosyl-L-homocysteine + DNA containing 5-methylcytosine | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| HT-29 cell | colon cancer | Homo sapiens | - |
| KYSE-150 cell | esophageal cancer | Homo sapiens | - |
| PC-3 cell | prostate cancer | Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| S-adenosyl-L-methionine + DNA | hypermethylation of CpG islands in the promoter regions is an important mechanism to silence the expression of many important genes in cancer | Homo sapiens | S-adenosyl-L-homocysteine + DNA containing 5-methylcytosine | - |
? | |
| S-adenosyl-L-methionine + poly(dI-dC)/poly(dI-dC) | - |
Homo sapiens | S-adenosyl-L-homocysteine + poly(dI-dC)/poly(dI-dC) containing 5-methylcytosine | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| 5-cytosine DNA methyltransferase | - |
Homo sapiens |
| DNMT | - |
Homo sapiens |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.00689 | - |
(-)-epigallocatechin-3-gallate | substrate: poly(dI-dC)/poly(dI-dC) | Homo sapiens | |
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