Any feedback?
Literature summary for 2.1.1.357 extracted from
- H3K36 methyltransferases as cancer drug targets Rationale and perspectives for inhibitor development (2016), Future Med. Chem., 8, 1589-1607 .
No PubMed abstract available
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| A-893 | inhibitor of SMYD2 | Homo sapiens |  |
| AZ505 | inhibitor of SMYD2 | Homo sapiens | |
| LLY-507 | inhibitor of SMYD2 | Homo sapiens | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 2 S-adenosyl-L-methionine + a [histone H3]-L-lysine36 | Homo sapiens | overall reaction | 2 S-adenosyl-L-homocysteine + a [histone H3]-N6,N6-dimethyl-L-lysine36 | - |
? | |
| S-adenosyl-L-homocysteine + nuclear factor-kappaB | Homo sapiens | NSD1 also methylates nonhistone proteins, including the p65 subunit of nuclear factor-kappaB at Lys218 and Lys221 | ? | - |
? | |
| S-adenosyl-L-methionine + a [histone H3]-L-lysine36 | Homo sapiens | - |
S-adenosyl-L-homocysteine + a [histone H3]-N6-methyl-L-lysine36 | - |
? | |
| S-adenosyl-L-methionine + a [histone H3]-N6-methyl-L-lysine36 | Homo sapiens | - |
S-adenosyl-L-homocysteine + a [histone H3]-N6,N6-dimethyl-L-lysine36 | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
| Homo sapiens | Q96L73 | - |
- |
| Homo sapiens | Q9NR48 | - |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| bladder transitional cell carcinoma cell | - |
Homo sapiens | - |
| breast cancer cell | - |
Homo sapiens | - |
| chronic lymphocytic leukemia cell | - |
Homo sapiens | - |
| colonic cancer cell | - |
Homo sapiens | - |
| esophageal squamous cell carcinoma cell line | - |
Homo sapiens | - |
| gastric cancer cell | - |
Homo sapiens | - |
| head and neck squamous cell carcinoma cell | - |
Homo sapiens | - |
| lung cancer cell | - |
Homo sapiens | - |
| lung squamous cell carcinoma cell | - |
Homo sapiens | - |
| lymphoblastic leukemia cell | - |
Homo sapiens | - |
| MCF-10A cell | - |
Homo sapiens | - |
| myeloma cell | - |
Homo sapiens | - |
| prostate gland cancer cell | - |
Homo sapiens | - |
| thyroid cancer cell | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 2 S-adenosyl-L-methionine + a [histone H3]-L-lysine36 | overall reaction | Homo sapiens | 2 S-adenosyl-L-homocysteine + a [histone H3]-N6,N6-dimethyl-L-lysine36 | - |
? | |
| S-adenosyl-L-homocysteine + nuclear factor-kappaB | NSD1 also methylates nonhistone proteins, including the p65 subunit of nuclear factor-kappaB at Lys218 and Lys221 | Homo sapiens | ? | - |
? | |
| S-adenosyl-L-methionine + a [histone H3]-L-lysine36 | - |
Homo sapiens | S-adenosyl-L-homocysteine + a [histone H3]-N6-methyl-L-lysine36 | - |
? | |
| S-adenosyl-L-methionine + a [histone H3]-N6-methyl-L-lysine36 | - |
Homo sapiens | S-adenosyl-L-homocysteine + a [histone H3]-N6,N6-dimethyl-L-lysine36 | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| Ash1L | - |
Homo sapiens |
| H3K36 KMTase | - |
Homo sapiens |
| H3K36 methyltransferase | - |
Homo sapiens |
| MMSET | - |
Homo sapiens |
| NSD1 | - |
Homo sapiens |
| NSD2 | - |
Homo sapiens |
| NSD3 | - |
Homo sapiens |
| SET | catalytic domain | Homo sapiens |
| SETMAR | - |
Homo sapiens |
| Smyd2 | - |
Homo sapiens |
| Whsc1 | - |
Homo sapiens |
| WHSC1L1 | - |
Homo sapiens |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.0000028 | - |
pH and temperature not specified in the publication | Homo sapiens | A-893 | |
| 0.000015 | - |
pH and temperature not specified in the publication | Homo sapiens | LLY-507 | |
General Information
| General Information | Comment | Organism |
|---|---|---|
| malfunction | germline deletion of NSD2 causes Wolf-Hirschhorn syndrome, a developmental disorder characterized by craniofacial defects, growth retardation and microcephaly | Homo sapiens |
| malfunction | mutations in NSD1 cause Sotos syndrome, a condition of childhood overgrowth and intellectual disability | Homo sapiens |
| physiological function | ASH1L is a HOX gene activator and important transcriptional regulator during development | Homo sapiens |
| physiological function | NSD2 is an important developmental regulator and oncogene. ASH1L is a HOX gene activator and important transcriptional regulator during development. SMYD2 promotes cancer cell proliferation in head and neck squamous cell carcinoma and esophageal squamous-cell carcinoma. SETMAR protein is linked to cancer via its role in DNA repair. The tumor suppressor SETD3 is implicated in DNA replication and repair due to its interaction with proliferating cell nuclear antigen | Homo sapiens |
| physiological function | NSD2 is an important developmental regulator and oncogene. SMYD2 promotes cancer cell proliferation in head and neck squamous cell carcinoma and esophageal squamous-cell carcinoma. SETMAR protein is linked to cancer via its role in DNA repair. The tumor suppressor SETD3 is implicated in DNA replication and repair due to its interaction with proliferating cell nuclear antigen | Homo sapiens |
Use of this online version of BRENDA is free under the CC BY 4.0 license. See terms of use for full details.
Release 2023.1 (January 2023)
Legal
Curated at
Member of
