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GeneE
50 sources retrieved Β· Most recent: April 2026 Β· Index updated 14 days ago
β“˜GeneE is for informational purposes only. It is not a substitute for professional medical advice, diagnosis, or treatment.
CDK4
cyclin dependent kinase 4
Chromosome 12 Β· 12q14.1
NCBI Gene: 1019Ensembl: ENSG00000135446.18HGNC: HGNC:1773UniProt: P11802
714PubMed Papers
21Diseases
18Drugs
3Pathogenic Variants
FUNCTIONAL ROLE
Hub GeneKinase
RESEARCH IMPACT
Highly StudiedTrending
CLINICAL
FDA Approved TargetOMIM Disease Gene
DATA QUALITY
βœ“ Experimental GO Evidenceβœ“ Swiss-Prot Reviewed
nucleolusprotein bindingnuclear membranecyclin-dependent protein kinase holoenzyme complexmelanoma, cutaneous malignant, susceptibility to, 3cutaneous melanomabreast carcinomabreast cancer
✦AI Summary

CDK4 is a serine/threonine kinase that forms complexes with cyclin D to regulate cell cycle progression through the G1/S transition 1. The CDK4-cyclin D complex phosphorylates retinoblastoma (RB) protein, causing its dissociation from E2F transcription factors and enabling expression of S-phase genes 2. CDK4 also phosphorylates SMAD3 to repress its transcriptional activity and integrates mitogenic and antimitogenic signals. CDK4 is critical for initiating and maintaining proliferation in hormone receptor-positive breast cancer, where it becomes a therapeutic target 1. CDK4/6 inhibitors have become standard care for advanced HR+/HER2- breast cancer, arresting sensitive cells in G1 phase 3. However, resistance mechanisms frequently emerge, including MYC-induced RB1 degradation 4 and upregulation of cyclin D1/CDK4 through PI3K/mTOR pathway activation 5. CDK4-selective inhibitors show promise in improving therapeutic efficacy while reducing hematologic toxicity compared to dual CDK4/6 inhibitors 6. Understanding CDK4's role in cell cycle control and resistance mechanisms informs development of improved treatment strategies for hormone-responsive cancers.

Sources cited
1
CDK4 mediates cellular transition into S phase and is critical for cancer initiation, growth, and survival; CDK4/6 inhibitors arrest tumor cells in G1 phase
PMID: 35304604
2
CDK4 selective inhibition improves anti-tumor efficacy and reduces neutropenia toxicity; CDK4 target coverage is a limiting factor in CDK4/6 inhibitor efficacy
PMID: 40068598
3
CDK4/6 inhibitors are approved for HR+/HER2- breast cancer; drug resistance mechanisms exist including cell cycle-specific and non-specific resistance
PMID: 36043521
4
CDK4/6 inhibition shows therapeutic effect in hormone-positive breast cancer but is limited by resistance mechanisms; combination strategies needed for broader applications
PMID: 32289274
5
CDK4/6 inhibitors interrupt cell cycle progression; three approved agents (palbociclib, ribociclib, abemaciclib) have similar mechanisms but important pharmacokinetic/pharmacodynamic differences
PMID: 33369721
6
MYC amplification confers CDK4/6 inhibitor resistance by inducing RB1 ubiquitination and degradation; MYC degradation restores RB1 and CDK4/6i sensitivity
PMID: 38424044
7
CDK4 is key in G1-to-S transition; CDK4/6 inhibitors block RB phosphorylation and restrain HR+ breast cancer cells in G1; resistance emerges through multiple mechanisms in both cancer and stromal compartments
PMID: 38943828
8
Palbociclib resistance involves upregulated cyclin D1 and CDK4 protein synthesis through PI3K/mTOR pathway activation; PI3K/mTOR inhibitors restore CDK4/6 inhibitor sensitivity
PMID: 35982377
Disease Associationsβ“˜21
melanoma, cutaneous malignant, susceptibility to, 3Open Targets
0.71Strong
cutaneous melanomaOpen Targets
0.65Moderate
breast carcinomaOpen Targets
0.64Moderate
breast cancerOpen Targets
0.63Moderate
small cell lung carcinomaOpen Targets
0.61Moderate
breast neoplasmOpen Targets
0.57Moderate
neoplasmOpen Targets
0.56Moderate
neurodegenerative diseaseOpen Targets
0.55Moderate
Alzheimer diseaseOpen Targets
0.54Moderate
Parkinson diseaseOpen Targets
0.53Moderate
lysosomal storage diseaseOpen Targets
0.53Moderate
multiple sclerosisOpen Targets
0.53Moderate
familial melanomaOpen Targets
0.49Moderate
hereditary neoplastic syndromeOpen Targets
0.48Moderate
Inherited cancer-predisposing syndromeOpen Targets
0.48Moderate
melanomaOpen Targets
0.48Moderate
cancerOpen Targets
0.44Moderate
non-small cell lung carcinomaOpen Targets
0.38Weak
head and neck squamous cell carcinomaOpen Targets
0.38Weak
Merkel cell skin cancerOpen Targets
0.38Weak
Melanoma, cutaneous malignant 3UniProt
Pathogenic Variants3
NM_000075.4(CDK4):c.70C>T (p.Arg24Cys)Pathogenic
Melanoma, cutaneous malignant, susceptibility to, 3|Familial melanoma|Hereditary cancer-predisposing syndrome|not provided
β˜…β˜…β˜†β˜†2026β†’ Residue 24
NM_000075.4(CDK4):c.71G>A (p.Arg24His)Pathogenic
Melanoma, cutaneous malignant, susceptibility to, 3|Hereditary cancer-predisposing syndrome|Familial melanoma
β˜…β˜…β˜†β˜†2024β†’ Residue 24
NM_000075.4(CDK4):c.279dup (p.Glu94Ter)Pathogenic
Gastric cancer
β˜†β˜†β˜†β˜†2021β†’ Residue 94
View on ClinVar β†—
Drug Targets18
ABEMACICLIBApproved
Cyclin-dependent kinase 6 inhibitor
breast cancer
AG-24322Phase I
Cyclin-dependent kinase 1 inhibitor
ALVOCIDIBPhase III
Cyclin-dependent kinase 4 inhibitor
chronic lymphocytic leukemia
AT-7519Phase II
Cyclin-dependent kinase inhibitor
chronic lymphocytic leukemia
AZD-5438Phase I
Cyclin-dependent kinase inhibitor
MILCICLIBPhase II
Cyclin-dependent kinase 1 inhibitor
PALBOCICLIBApproved
Cyclin-dependent kinase 4/cyclin D1 inhibitor
breast cancer
PHA-793887Phase I
Cyclin-dependent kinase inhibitor
RG-547Phase I
Cyclin-dependent kinase 1 inhibitor
RGB-286638Phase I
Cyclin-dependent kinase 1 inhibitor
RIBOCICLIBPhase III
Cyclin-dependent kinase 6 inhibitor
breast cancer
RIBOCICLIB SUCCINATEApproved
Cyclin-dependent kinase 4 inhibitor
breast cancer
RIVICICLIBPhase II
Cyclin-dependent kinase 1 inhibitor
Mantle cell lymphoma
RONICICLIBPhase II
Cyclin-dependent kinase inhibitor
small cell lung carcinoma
TRILACICLIBApproved
Cyclin-dependent kinase 6 inhibitor
small cell lung carcinoma
TRILACICLIB DIHYDROCHLORIDEApproved
Cyclin-dependent kinase 6 inhibitor
small cell lung carcinoma
UCN-01Phase II
3-phosphoinositide dependent protein kinase-1 inhibitor
non-small cell lung carcinoma
VORUCICLIBPhase I
Cyclin-dependent kinase 4 inhibitor
Related Genes
CCND2Protein interaction100%CCND3Protein interaction100%HSP90AA1Protein interaction100%HSP90AB1Protein interaction100%CDKN1BProtein interaction100%CCNA1Protein interaction100%
Tissue Expression6 tissues
Ovary
100%
Brain
90%
Heart
76%
Bone Marrow
74%
Lung
65%
Liver
45%
Gene Interaction Network
Click a node to explore
CDK4CCND2CCND3HSP90AA1HSP90AB1CDKN1BCCNA1
PROTEIN STRUCTURE
Preparing viewer…
PDB9CSK Β· 2.25 Γ… Β· X-ray
View on RCSB β†—
Constraintβ“˜
LOEUFβ“˜
0.61LoF Tolerant
pLIβ“˜
0.57Intermediate
Observed/Expected LoF0.38 [0.25–0.61]
RankingsWhere CDK4 stands among ~20K protein-coding genes
  • #297of 20,598
    Most Researched714 Β· top 5%
  • #279of 1,025
    FDA-Approved Drug Targets5
  • #3,890of 5,498
    Most Pathogenic Variants3
  • #4,228of 17,882
    Most Constrained (LOEUF)0.61 Β· top quartile
Genes detectedCDK4
Sources retrieved50 papers
Response timeβ€”
πŸ“„ Sources
50β–Ό
1
Targeting CDK4 and CDK6 in cancer.
PMID: 35304604
Nat Rev Cancer Β· 2022
1.00
2
CDK4 selective inhibition improves preclinical anti-tumor efficacy and safety.
PMID: 40068598
Cancer Cell Β· 2025
0.90
3
SLC7A11 protects luminal A breast cancer cells against ferroptosis induced by CDK4/6 inhibitors.
PMID: 39153252
Redox Biol Β· 2024
0.80
4
CDK4/6 inhibitor resistance mechanisms and treatment strategies (Review).
PMID: 36043521
Int J Mol Med Β· 2022
0.80
5
Dual targeting of CDK4/6 and CDK7 augments tumor response and antitumor immunity in breast cancer models.
PMID: 40794455
J Clin Invest Β· 2025
0.78