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Literature summary for 2.7.11.10 extracted from
- Targeting IkB kinase for the treatment of inflammatory and other disorders (2003), Curr. Opin. Drug Discov. Devel., 6, 720-728.
Activating Compound
| Activating Compound | Comment | Organism | Structure |
|---|---|---|---|
| NEMO | - |
Homo sapiens |
Application
| Application | Comment | Organism |
|---|---|---|
| pharmacology | IKK is a target for development of therapeutics for treatment of diseases resulting from nuclear transcription factor NFkappaB pathogenesis | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 5-Aminosalicylate | weak inhibition of IKK-2 | Homo sapiens |  |
| Acetylsalicylate | weak inhibition of IKK-2 | Homo sapiens | |
| BMS-345541 | specific for IKK-2, binds at an allosteric site | Homo sapiens | |
| curcumin | weak inhibition of IKK-2 | Homo sapiens | |
| cyclopentone prostaglandines | inhibition of IKK-2 | Homo sapiens | |
| salicylate | weak inhibition of IKK-2 | Homo sapiens | |
| sulfasalazine | weak inhibition of IKK-2 | Homo sapiens | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| cytoplasm | - |
Homo sapiens | 5737 | - |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Mg2+ | - |
Homo sapiens | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + [IkappaB protein] | Homo sapiens | signalling step of IKK bound to NFkappaB for subsequent ubiquitination of IkappaB and proteolytic degradation | ADP + [IkappaB phosphoprotein] | - |
? | |
| additional information | Homo sapiens | activation of heterodimeric nuclear transcription factor NFkappaB is an essential step in inflammation, e.g. resulting in osteoarthritis, ulcerative colitis, asthma, and Crohn's disease, signalling step for phosphorylation, subsequent ubiquitination and proteolytic degradation of IkappaB, NFkappaB remains free after the reaction and is translocated to the nucleus, NFkappaB activation is also involved in development of diseases like cancer, gut ischemia-reperfusion, diabetes, or in transplant rejections, overview | ? | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + [IkappaB protein] | - |
Homo sapiens | ADP + [IkappaB phosphoprotein] | - |
? | |
| ATP + [IkappaB protein] | signalling step of IKK bound to NFkappaB for subsequent ubiquitination of IkappaB and proteolytic degradation | Homo sapiens | ADP + [IkappaB phosphoprotein] | - |
? | |
| additional information | activation of heterodimeric nuclear transcription factor NFkappaB is an essential step in inflammation, e.g. resulting in osteoarthritis, ulcerative colitis, asthma, and Crohn's disease, signalling step for phosphorylation, subsequent ubiquitination and proteolytic degradation of IkappaB, NFkappaB remains free after the reaction and is translocated to the nucleus, NFkappaB activation is also involved in development of diseases like cancer, gut ischemia-reperfusion, diabetes, or in transplant rejections, overview | Homo sapiens | ? | - |
? | |
Subunits
| Subunits | Comment | Organism |
|---|---|---|
| More | the IKK complex consists of 3 subunits: catalytic IKKalpha and IKKbeta, and noncatalytic NEMO/IKKgamma | Homo sapiens |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| IKK | - |
Homo sapiens |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Homo sapiens | |
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