Id: acc2495
Group: 2sens
Protein: Cdc2
Gene Symbol: CDK1
Protein Id: P06493
Protein Name: CDK1_HUMAN
PTM: phosphorylation
Site: Thr14
Site Sequence: TKIEKIGEGTYGVVYKGRHKT
Disease Category: Cancer
Disease: Colorectal Cancer
Disease Subtype: "Colon Cancer, p53 mut"
Disease Cellline: HT29
Disease Info:
Drug: radiation
Drug Info: -
Effect: inhibit
Effect Info: "PD0166285 can significantly inhibit the phosphorylation of Cdc2 at Tyr - 15 and Thr - 14 induced by irradiation, suppress cancer cells, and enhance the efficacy of radiotherapy."
Note: Non-conventional drugs
Score: 4.5
Pubmed(PMID): 11719452
Sentence Index:
Sentence:

Sequence & Structure:

MEDYTKIEKIGEGTYGVVYKGRHKTTGQVVAMKKIRLESEEEGVPSTAIREISLLKELRHPNIVSLQDVLMQDSRLYLIFEFLSMDLKKYLDSIPPGQYMDSSLVKSYLYQILQGIVFCHSRRVLHRDLKPQNLLIDDKGTIKLADFGLARAFGIPIRVYTHEVVTLWYRSPEVLLGSARYSTPVDIWSIGTIFAELATKKPLFHGDSEIDQLFRIFRALGTPNNEVWPEVESLQDYKNTFPKWKPGSLASHVKNLDENGLDLLSKMLIYDPAKRISGKMALNHPYFNDLDNQIKKM

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

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CDK1 RONICICLIB Cyclin-dependent kinase inhibitor 2 Withdrawn neoplasm ClinicalTrials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 Targets
Small molecule
Antibody
PROTAC
Other modalities
Approved Drug
Advanced Clinical
Phase 1 Clinical
Structure with Ligand
High-Quality Ligand
High-Quality Pocket
Med-Quality Pocket
Druggable Family
Approved Drug
Advanced Clinical
Phase 1 Clinical
UniProt loc high conf
GO CC high conf
UniProt loc med conf
UniProt SigP or TMHMM
GO CC med conf
Human Protein Atlas loc
Approved Drug
Advanced Clinical
Phase 1 Clinical
Literature
UniProt Ubiquitination
Database Ubiquitination
Half-life Data
Small Molecule Binder
Approved Drug
Advanced Clinical
Phase 1 Clinical

PTM Intensity:

source: CPTAC
CDK1-Thr14
Cancer Intensity
BRCA 0.255
COAD -0.114
HGSC -1.7
ccRCC 0.829
GBM
HNSC 0.883
LUAD 0.018
LUSC -1.214
non_ccRCC
PDAC
UCEC 1.044

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
T 161 U Vulvar cancer Phosphorylation 25849598
Y 15 U Cancer Phosphorylation 24391984
Y 15 U Vulvar cancer Phosphorylation 25849598
- - U Breast cancer Ubiquitination 36604147

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: DecryptM

No data.

Function score:

source: funscoR

No data.

Cross Links: