Cloned (Comment) | Organism |
---|---|
expression in Escherichia coli | Homo sapiens |
Crystallization (Comment) | Organism |
---|---|
hanging drop vapor diffusion method at 20°C, crystal structure of the catalytic kinase domain of the human CaMKKbeta isoform complexed with its selective inhibitor 7H-benzimidazo(2,1-a)benz(de)isoquinoline-7-one-3-carboxylate (i.e. STO-609). The crystal belongs to the primitive orthorhombic space group P2(1)2(1)2(1) with unit cell constants of a = 69.4 A, b = 77.2 A, c = 84.3 A | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
P274E | the P274E mutation significantly reduces the inhibitory effect of 7H-benzimidazo(2,1-a)benz(de)isoquinoline-7-one-3-carboxylate (i.e. STO-609) on the isoenzyme CaMKKbeta | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
7H-benzimidazo(2,1-a)benz(de)isoquinoline-7-one-3-carboxylate | i.e. STO-609. The CaMKKbeta residue Pro274, which replaces the conserved acidic residue of other protein kinases, is an important determinant for the selective inhibition by STO-609. ATP-competitive inhibition mechanism | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + Ca2+/calmodulin-dependent protein kinase I | Homo sapiens | the enzyme is a member of the CaMK cascade that mediates the response to intracellular Ca2+ elevation. Ca2+/calmodulin-dependent protein kinase kinase phosphorylates and activates Ca2+/calmodulin-dependent protein kinase I and Ca2+/calmodulin-dependent protein kinase IV, which directly activate transcription factors | ADP + phosphorylated Ca2+/calmodulin-dependent protein kinase I | - |
? | |
ATP + Ca2+/calmodulin-dependent protein kinase IV | Homo sapiens | the enzyme is a member of the CaMK cascade that mediates the response to intracellular Ca2+ elevation. Ca2+/calmodulin-dependent protein kinase kinase phosphorylates and activates Ca2+/calmodulin-dependent protein kinase I and Ca2+/calmodulin-dependent protein kinase IV, which directly activate transcription factors | ADP + phosphorylated Ca2+/calmodulin-dependent protein kinase IV | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | Q96RR4 | - |
- |
Purification (Comment) | Organism |
---|---|
- |
Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + Ca2+/calmodulin-dependent protein kinase I | - |
Homo sapiens | ADP + phosphorylated Ca2+/calmodulin-dependent protein kinase I | - |
? | |
ATP + Ca2+/calmodulin-dependent protein kinase I | the enzyme is a member of the CaMK cascade that mediates the response to intracellular Ca2+ elevation. Ca2+/calmodulin-dependent protein kinase kinase phosphorylates and activates Ca2+/calmodulin-dependent protein kinase I and Ca2+/calmodulin-dependent protein kinase IV, which directly activate transcription factors | Homo sapiens | ADP + phosphorylated Ca2+/calmodulin-dependent protein kinase I | - |
? | |
ATP + Ca2+/calmodulin-dependent protein kinase IV | - |
Homo sapiens | ADP + phosphorylated Ca2+/calmodulin-dependent protein kinase IV | - |
? | |
ATP + Ca2+/calmodulin-dependent protein kinase IV | the enzyme is a member of the CaMK cascade that mediates the response to intracellular Ca2+ elevation. Ca2+/calmodulin-dependent protein kinase kinase phosphorylates and activates Ca2+/calmodulin-dependent protein kinase I and Ca2+/calmodulin-dependent protein kinase IV, which directly activate transcription factors | Homo sapiens | ADP + phosphorylated Ca2+/calmodulin-dependent protein kinase IV | - |
? |
Synonyms | Comment | Organism |
---|---|---|
Ca2+/calmodulin-dependent protein kinase kinase | - |
Homo sapiens |
CaMK | - |
Homo sapiens |
CaMKK | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.02 | - |
30°C, pH 7.5, mutant enzyme P274E | Homo sapiens | 7H-benzimidazo(2,1-a)benz(de)isoquinoline-7-one-3-carboxylate | |
0.5 | - |
30°C, pH 7.5, wild-type enzyme | Homo sapiens | 7H-benzimidazo(2,1-a)benz(de)isoquinoline-7-one-3-carboxylate |
General Information | Comment | Organism |
---|---|---|
physiological function | the enzyme is a member of the CaMK cascade that mediates the response to intracellular Ca2+ elevation | Homo sapiens |