Activating Compound | Comment | Organism | Structure |
---|---|---|---|
Cdc25A | - |
Homo sapiens | |
cyclin E | enhances Cdk activity, overexpression activates the DNA damage response in U2-OS osteogenic sarcoma cells | Homo sapiens | |
E2F1 | - |
Homo sapiens | |
additional information | Chk1 inhibition augments Cdk activity | Homo sapiens |
Application | Comment | Organism |
---|---|---|
medicine | Cdk dysregulation in the generation of genomic instability, increased Cdk activity may critically reduce licensing of origins of DNA replication, drive re-replication, or mediate overexpression of checkpoint proteins, inducing deleterious cell cycle delay. These effects may fuel tumorigenesis | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
additional information | dominant negative mutant of CDK2, induction delays S phase progression in many cell types, is not relieved by treatment with potent checkpoint inhibitor caffeine | Homo sapiens |
additional information | yeast cells deficient in S phase Cdk activity acquire DNA damage, cdc7 mutants are unable to initiate DNA replication but have normal Cdk activity, induced double-strand break is promptly repaired | Saccharomyces cerevisiae |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
Cdk2DN | inhibition of Cdk2, induces phosphorylation of ataxia-telangiectasia mutated substrates | Homo sapiens | |
additional information | inhibition of Cdk2 by inactivation of Cdc25 phosphatases | Homo sapiens | |
p21 | induction of p21 by p53 leads to inhibition of Cdk2 and Cdk1 complexes | Homo sapiens | |
Sic1 | Cdk inhibitor, double-strand break is not efficiently repaired | Saccharomyces cerevisiae | |
siRNA | inhibition of Cdk2, induces phosphorylation of ataxia-telangiectasia mutated substrates | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + BRCA2 | Homo sapiens | phosphorylates at Ser3291, phosphorylation reaches maximal levels in G2/M | ADP + phosphorylated BRCA2 | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Saccharomyces cerevisiae | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
fibroblast | primary diploid fibroblast | Homo sapiens | - |
ovary cancer cell line | - |
Homo sapiens | - |
U2-OS cell | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + BRCA2 | phosphorylates at Ser3291, phosphorylation reaches maximal levels in G2/M | Homo sapiens | ADP + phosphorylated BRCA2 | - |
? | |
ATP + BRCA2 | phosphorylates at Ser3291, an event that disrupts association with RAD51 | Homo sapiens | ADP + phosphorylated BRCA2 | - |
? | |
ATP + Cdc6 | - |
Homo sapiens | ADP + phosphorylated Cdc6 | - |
? | |
ATP + DNA polymerase alpha | - |
Homo sapiens | ADP + phosphorylated DNA polymerase alpha | - |
? | |
ATP + DNA polymerase sigma | - |
Homo sapiens | ADP + phosphorylated DNA polymerase sigma | - |
? | |
ATP + histone H1 | - |
Homo sapiens | ADP + phosphorylated histone H1 | - |
? | |
ATP + Mcm3 | - |
Homo sapiens | ADP + phosphorylated Mcm3 | - |
? | |
ATP + Mcm4 | - |
Homo sapiens | ADP + phosphorylated Mcm4 | - |
? | |
ATP + Orc2 | - |
Homo sapiens | ADP + phosphorylated Orc2 | - |
? | |
ATP + Orc6 | - |
Homo sapiens | ADP + phosphorylated Orc6 | - |
? | |
ATP + replication factor C | - |
Homo sapiens | ADP + phosphorylated replication factor C | - |
? | |
ATP + retinoblastoma protein | - |
Homo sapiens | ADP + phosphorylated retinoblastoma protein | - |
? | |
additional information | Cdk activity is required to fire origins of DNA replication and to prevent 'licensing' (establishing the competence) of additional origins after replication initiation | Saccharomyces cerevisiae | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
CDK | - |
Saccharomyces cerevisiae |
Cdk 2 | - |
Homo sapiens |
cdk7 | - |
Saccharomyces cerevisiae |
cyclin-dependent kinase | - |
Homo sapiens |
cyclin-dependent kinase | - |
Saccharomyces cerevisiae |