Id: | acc3150 |
Group: | 2sens |
Protein: | Cdk1 |
Gene Symbol: | CDK1 |
Protein Id: | P06493 |
Protein Name: | CDK1_HUMAN |
PTM: | phosphorylation |
Site: | Tyr15 |
Site Sequence: | KIEKIGEGTYGVVYKGRHKTT |
Disease Category: | Cancer |
Disease: | Hepatocellular Carcinoma |
Disease Subtype: | |
Disease Cellline: | Hep3B |
Disease Info: | |
Drug: | HKH40A |
Drug Info: | "HKH40A is a drug with potential medical applications, although specific details about it are not provided." |
Effect: | modulate |
Effect Info: | "Inhibiting the activity of Cdc25C through Chk1/2 - mediated inhibitory phosphorylation leads to the phosphorylation of downstream Cdk1 and cell cycle G2/M arrest, thereby inducing cell apoptosis." |
Note: | |
Score: | 4.0 |
Pubmed(PMID): | 19530246 |
Sentence Index: | 19530246_3-4 |
Sentence: | "We found that HKH40A activated ataxia telangiectasia mutated (ATM) kinase, which then triggered activation of the Chk1/2 signaling pathway, evidenced by Chk1/2 mediated inhibitory phosphorylation of Cdc25C protein phosphatase. This resulted in Cdk1 tyrosine phosphorylation at Tyr-15, leading to cell cycle block at G2/M phase." |
Sequence & Structure:
MEDYTKIEKIGEGTYGVVYKGRHKTTGQVVAMKKIRLESEEEGVPSTAIREISLLKELRHPNIVSLQDVLMQDSRLYLIFEFLSMDLKKYLDSIPPGQYMDSSLVKSYLYQILQGIVFCHSRRVLHRDLKPQNLLIDDKGTIKLADFGLARAFGIPIRVYTHEVVTLWYRSPEVLLGSARYSTPVDIWSIGTIFAELATKKPLFHGDSEIDQLFRIFRALGTPNNEVWPEVESLQDYKNTFPKWKPGSLASHVKNLDENGLDLLSKMLIYDPAKRISGKMALNHPYFNDLDNQIKKM
Select PDB:
Target | Drug name | MOA | Phase | Status | Disease | Source |
---|---|---|---|---|---|---|
CDK1 | DINACICLIB | Cyclin-dependent kinase 1 inhibitor | 3 | Completed | chronic lymphocytic leukemia | ClinicalTrials |
CDK1 | ALVOCIDIB | Cyclin-dependent kinase 1 inhibitor | 2 | Completed | chronic lymphocytic leukemia | ClinicalTrials ClinicalTrials |
CDK1 | AT-7519 | Cyclin-dependent kinase inhibitor | 2 | Completed | chronic lymphocytic leukemia | ClinicalTrials |
CDK1 | MILCICLIB | Cyclin-dependent kinase 1 inhibitor | 2 | Completed | hepatocellular carcinoma | ClinicalTrials |
CDK1 | ALVOCIDIB | Cyclin-dependent kinase 1 inhibitor | 2 | Terminated | chronic lymphocytic leukemia | ClinicalTrials |
CDK1 | ALVOCIDIB | Cyclin-dependent kinase 1 inhibitor | 2 | Terminated | acute myeloid leukemia | ClinicalTrials ClinicalTrials |
CDK1 | DINACICLIB | Cyclin-dependent kinase 1 inhibitor | 2 | Terminated | acute lymphoblastic leukemia | ClinicalTrials |
CDK1 | DINACICLIB | Cyclin-dependent kinase 1 inhibitor | 2 | Terminated | acute myeloid leukemia | ClinicalTrials |
CDK1 | ALVOCIDIB | Cyclin-dependent kinase 1 inhibitor | 2 | Completed | cutaneous melanoma | ClinicalTrials |
CDK1 | ALVOCIDIB | Cyclin-dependent kinase 1 inhibitor | 2 | Completed | lymphoma | ClinicalTrials ClinicalTrials |
CDK1 | RONICICLIB | Cyclin-dependent kinase inhibitor | 2 | Withdrawn | neoplasm | ClinicalTrials |
CDK1 | ALVOCIDIB | Cyclin-dependent kinase 1 inhibitor | 2 | Completed | sarcoma | ClinicalTrials |
CDK1 | RONICICLIB | Cyclin-dependent kinase inhibitor | 2 | Terminated | small cell lung carcinoma | ClinicalTrials |
CDK1 | ALVOCIDIB | Cyclin-dependent kinase 1 inhibitor | 2 | Completed | multiple myeloma | ClinicalTrials |
CDK1 | DINACICLIB | Cyclin-dependent kinase 1 inhibitor | 2 | Completed | multiple myeloma | ClinicalTrials |
CDK1 | SELICICLIB | Cyclin-dependent kinase 1 inhibitor | 2 | Terminated | non-small cell lung carcinoma | ClinicalTrials |
CDK1 | ALVOCIDIB | Cyclin-dependent kinase 1 inhibitor | 2 | Completed | pancreatic carcinoma | ClinicalTrials |
CDK1 | ALVOCIDIB | Cyclin-dependent kinase 1 inhibitor | 2 | Completed | pancreatic adenocarcinoma | ClinicalTrials |
CDK1 | MILCICLIB | Cyclin-dependent kinase 1 inhibitor | 2 | Terminated | Thymic Carcinoma | ClinicalTrials |
CDK1 | MILCICLIB | Cyclin-dependent kinase 1 inhibitor | 2 | Terminated | Thymoma | ClinicalTrials |
CDK1 | SELICICLIB | Cyclin-dependent kinase 1 inhibitor | 2 | Recruiting | pituitary-dependent Cushing's disease | ClinicalTrials |
CDK1 | SELICICLIB | Cyclin-dependent kinase 1 inhibitor | 2 | Terminated | pituitary-dependent Cushing's disease | ClinicalTrials |
CDK1 | AT-7519 | Cyclin-dependent kinase inhibitor | 2 | Completed | Mantle cell lymphoma | ClinicalTrials |
CDK1 | ALVOCIDIB | Cyclin-dependent kinase 1 inhibitor | 2 | Terminated | prolymphocytic leukemia | ClinicalTrials |
CDK1 | DINACICLIB | Cyclin-dependent kinase 1 inhibitor | 2 | Active, not recruiting | mucosal melanoma | ClinicalTrials |
Note: Only show clinically investigational or approved drugs with protein targets.
Protein Tractability:
source: Open TargetsPTM Intensity:
source: CPTACCDK1-Tyr15 | |
---|---|
Cancer | Intensity |
BRCA | -0.179 |
COAD | -0.261 |
HGSC | -0.161 |
ccRCC | 0.837 |
GBM | |
HNSC | 0.911 |
LUAD | -0.288 |
LUSC | -1.994 |
non_ccRCC | |
PDAC | |
UCEC | 1.134 |
PTM-Disease Association:
source: PTMDResidue | Position | State | Disease | Class | PMID |
---|---|---|---|---|---|
Y | 15 | U | Cancer | Phosphorylation | 24391984 |
Y | 15 | U | Vulvar cancer | Phosphorylation | 25849598 |
State Note: Based on the distinct PTM states in diseases, PTMD classified all disease-associated PTMs into six classes, including whether the up-regulation (U) or down-regulation (D) of PTM levels, the absence (A) or presence (P) of PTMs, and the creation (C) or disruption (N) of PTM sites are associated with diseases.
PTM-Drug Perturbation Response:
source: DecryptMNo data.
Function score:
source: funscoRNo data.