Id: | acc1201 |
Group: | 2sens |
Protein: | CDK2 |
Gene Symbol: | CDK2 |
Protein Id: | P24941 |
Protein Name: | CDK2_HUMAN |
PTM: | phosphorylation |
Site: | Thr160 |
Site Sequence: | AFGVPVRTYTHEVVTLWYRAP |
Disease Category: | Cancer |
Disease: | Colorectal Cancer |
Disease Subtype: | |
Disease Cellline: | LoVo |
Disease Info: | |
Drug: | adapalene |
Drug Info: | "Adapalene is a topical retinoid medication primarily used for the treatment of mild to moderate acne vulgaris, including comedones, papules, and pustules, by modulating keratinocyte differentiation and reducing inflammation. " |
Effect: | modulate |
Effect Info: | Adapalene (ADA) can significantly increase the phosphorylation of CDK2 (at Thr-160) and Rb (at Ser-795) and inhibit tumors. |
Note: | |
Score: | 4.0 |
Pubmed(PMID): | 26398439 |
Sentence Index: | 26398439_4-5 |
Sentence: | "Among them, adapalene (ADA; CD271,6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphtoic acid) exhibited the highest anti-proliferative effects in LOVO and DLD1 human colon cancer cell lines. Consistent with the expected properties of CDK2 inhibitors, the present study demonstrated that ADA significantly increased the G1-phase population and decreased the expression of CDK2, cyclin E and retinoblastoma protein (Rb), as well as the phosphorylation of CDK2 (on Thr-160) and Rb (on Ser-795)." |
Sequence & Structure:
MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNHPNIVKLLDVIHTENKLYLVFEFLHQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHSHRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYYSTAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSFPKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
Select PDB:
Target | Drug name | MOA | Phase | Status | Disease | Source |
---|---|---|---|---|---|---|
CDK2 | DINACICLIB | Cyclin-dependent kinase 2 inhibitor | 3 | Completed | chronic lymphocytic leukemia | ClinicalTrials |
CDK2 | ALVOCIDIB | Cyclin-dependent kinase 2 inhibitor | 2 | Completed | chronic lymphocytic leukemia | ClinicalTrials ClinicalTrials |
CDK2 | MILCICLIB | Cyclin-dependent kinase 2 inhibitor | 2 | Completed | hepatocellular carcinoma | ClinicalTrials |
CDK2 | ALVOCIDIB | Cyclin-dependent kinase 2 inhibitor | 2 | Terminated | chronic lymphocytic leukemia | ClinicalTrials |
CDK2 | AT-7519 | Cyclin-dependent kinase inhibitor | 2 | Completed | chronic lymphocytic leukemia | ClinicalTrials |
CDK2 | ALVOCIDIB | Cyclin-dependent kinase 2 inhibitor | 2 | Terminated | acute myeloid leukemia | ClinicalTrials ClinicalTrials |
CDK2 | DINACICLIB | Cyclin-dependent kinase 2 inhibitor | 2 | Terminated | acute lymphoblastic leukemia | ClinicalTrials |
CDK2 | DINACICLIB | Cyclin-dependent kinase 2 inhibitor | 2 | Terminated | acute myeloid leukemia | ClinicalTrials |
CDK2 | ALVOCIDIB | Cyclin-dependent kinase 2 inhibitor | 2 | Completed | cutaneous melanoma | ClinicalTrials |
CDK2 | ALVOCIDIB | Cyclin-dependent kinase 2 inhibitor | 2 | Completed | lymphoma | ClinicalTrials ClinicalTrials |
CDK2 | UCN-01 | Cyclin-dependent kinase 2 inhibitor | 2 | Terminated | lymphoma | ClinicalTrials |
CDK2 | RONICICLIB | Cyclin-dependent kinase inhibitor | 2 | Withdrawn | neoplasm | ClinicalTrials |
CDK2 | RONICICLIB | Cyclin-dependent kinase inhibitor | 2 | Terminated | small cell lung carcinoma | ClinicalTrials |
CDK2 | UCN-01 | Cyclin-dependent kinase 2 inhibitor | 2 | Completed | small cell lung carcinoma | ClinicalTrials |
CDK2 | ALVOCIDIB | Cyclin-dependent kinase 2 inhibitor | 2 | Completed | sarcoma | ClinicalTrials |
CDK2 | UCN-01 | Cyclin-dependent kinase 2 inhibitor | 2 | Terminated | melanoma | ClinicalTrials |
CDK2 | ALVOCIDIB | Cyclin-dependent kinase 2 inhibitor | 2 | Completed | multiple myeloma | ClinicalTrials |
CDK2 | DINACICLIB | Cyclin-dependent kinase 2 inhibitor | 2 | Completed | multiple myeloma | ClinicalTrials |
CDK2 | UCN-01 | Cyclin-dependent kinase 2 inhibitor | 2 | Completed | pancreatic carcinoma | ClinicalTrials |
CDK2 | SELICICLIB | Cyclin-dependent kinase 2 inhibitor | 2 | Terminated | non-small cell lung carcinoma | ClinicalTrials |
CDK2 | ALVOCIDIB | Cyclin-dependent kinase 2 inhibitor | 2 | Completed | pancreatic carcinoma | ClinicalTrials |
CDK2 | ALVOCIDIB | Cyclin-dependent kinase 2 inhibitor | 2 | Completed | pancreatic adenocarcinoma | ClinicalTrials |
CDK2 | MILCICLIB | Cyclin-dependent kinase 2 inhibitor | 2 | Terminated | Thymoma | ClinicalTrials |
CDK2 | MILCICLIB | Cyclin-dependent kinase 2 inhibitor | 2 | Terminated | Thymic Carcinoma | ClinicalTrials |
CDK2 | SELICICLIB | Cyclin-dependent kinase 2 inhibitor | 2 | Recruiting | pituitary-dependent Cushing's disease | ClinicalTrials |
Note: Only show clinically investigational or approved drugs with protein targets.
Protein Tractability:
source: Open TargetsPTM Intensity:
source: CPTACCDK2-Thr160 | |
---|---|
Cancer | Intensity |
BRCA | |
COAD | |
HGSC | |
ccRCC | |
GBM | |
HNSC | |
LUAD | |
LUSC | |
non_ccRCC | |
PDAC | |
UCEC |
PTM-Disease Association:
source: PTMDResidue | Position | State | Disease | Class | PMID |
---|---|---|---|---|---|
- | - | P | Hepatocellular carcinoma | Ubiquitination | 29497124 |
- | - | U | T-cell acute lymphoblastic leukemia | Acetylation | 34407842 |
Y | 15 | U | Neuroblastoma | Phosphorylation | 24349301 |
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.