CDK6 Gene Complete Identifier and Functional Mapping Reference

Provide a comprehensive cross-database identifier and functional mapping reference for human CDK6 — a definitive lookup resource covering: ### …

Provide a comprehensive cross-database identifier and functional mapping reference for human CDK6 — a definitive lookup resource covering: ### Section 1: Gene identifiers For human gene CDK6, list ALL gene-level database identifiers. Required: - HGNC ID and approved symbol - Ensembl gene ID (ENSG...) - NCBI Entrez Gene ID - OMIM gene/locus ID - Genomic location: chromosome, start position, end position, strand (GRCh38) ### Section 2: Transcript identifiers For human gene CDK6, list ALL transcript-level identifiers. Required: - Ensembl transcripts: ALL ENST IDs with biotype. Total count. - RefSeq transcripts: ALL NM_ mRNA accessions. Mark which is MANE Select. - CCDS IDs. - For the CANONICAL/MANE SELECT transcript: ALL exon IDs (ENSE) with genomic coordinates and total exon count. ### Section 3: Protein identifiers For human gene CDK6 protein product(s), list ALL protein-level identifiers. Required: - UniProt accessions: ALL entries (reviewed and unreviewed). Mark the canonical reviewed entry. - RefSeq protein: ALL NP_ accessions. - Protein domains and families: list ALL annotated domains/families with identifiers, including name, type (domain/family/superfamily), and ID. - Antibody availability: known antibody resources for the protein. ### Section 4: Structure For human gene CDK6 protein, list ALL structural data. Required: - Experimental structures: ALL PDB IDs. For each: experimental method (X-ray/NMR/Cryo-EM) and resolution. Total count. - Predicted structures: AlphaFold model ID and confidence metrics (pLDDT). ### Section 5: Cross-species orthologs For human gene CDK6, list orthologous genes in key model organisms. Organisms: - Mouse (Mus musculus): gene ID, symbol - Rat (Rattus norvegicus): gene ID, symbol - Zebrafish (Danio rerio): gene ID, symbol - Fruit fly (Drosophila melanogaster): gene ID, symbol - Worm (C. elegans): gene ID, symbol - Yeast (S. cerevisiae): gene ID, symbol ### Section 6: Clinical variants & AI predictions For human gene CDK6, summarize clinical variants and AI predictions. Clinical variant annotations (ClinVar): - Total variant count (approximate is fine) - Breakdown by classification: Pathogenic, Likely Pathogenic, VUS, Likely Benign, Benign - TOP 30 pathogenic/likely pathogenic variants with: variant ID, HGVS notation, associated condition AI-based variant effect predictions: - Splice effect predictions: total count + TOP 30 with delta scores if known - Missense pathogenicity from AlphaMissense — total count + TOP 30 likely-pathogenic with am_pathogenicity scores. ### Section 7: Pathways & Gene Ontology For human gene CDK6, list biological pathways and Gene Ontology annotations. Pathway membership: - ALL biological pathways this gene participates in, with pathway IDs and names - Total pathway count Gene Ontology: - Biological Process: count and TOP 20 terms with GO IDs - Molecular Function: count and TOP 20 terms with GO IDs - Cellular Component: count and TOP 20 terms with GO IDs ### Section 8: Protein interactions & networks For human gene CDK6 protein, summarize protein interactions and networks. Protein-protein interactions (STRING, IntAct, BioGRID, etc.): - Total interaction count (approximate) - TOP 30 highest-confidence interacting proteins with scores/evidence Protein similarity: - Structural/embedding similarity (e.g. Foldseek, ESM): TOP 20 similar proteins with scores - Sequence homology: TOP 20 homologous proteins with identity/similarity ### Section 9: Transcription factor regulatory data For human gene CDK6, summarize transcription factor regulatory data. If CDK6 is a transcription factor: - Downstream targets: total count + TOP 30 with regulation type (activates/represses) and evidence - DNA binding motifs from JASPAR — all known motif IDs and motif family classification. Regardless: - Upstream regulators: TFs that regulate CDK6 — names with evidence type (ChIP-seq / predicted / experimentally validated) If CDK6 is not a transcription factor, say so briefly and skip the downstream/motif sections. ### Section 10: Drug & pharmacology data For human gene CDK6 protein as a drug target, summarize pharmacology data. If CDK6 is a known drug target: - Targeting molecules: total count in ChEMBL/DrugBank + TOP 30 by development phase (molecule ID, name, mechanism, highest phase) - Clinical trials: TOP 20 involving drugs targeting this gene — trial ID, phase, status, intervention - Pharmacogenomics: known drug-gene interactions affecting drug response + dosing guidelines if any If CDK6 is not currently a drug target, say so briefly. ### Section 11: Expression profiles For human gene CDK6, summarize expression profiles. Tissue expression (GTEx, HPA, Bgee, etc.): - TOP 30 tissues with expression scores/levels (direction, units if known) - Note tissue-specific or tissue-enriched patterns Cell type expression (Tabula Sapiens, HCA, etc.): - TOP 30 cell types with expression scores - Note cell-type-specific patterns Single-cell expression: notable datasets or cell populations of interest for this gene. ### Section 12: Disease associations For human gene CDK6, summarize disease associations. Mendelian / monogenic disease: - Diseases caused by mutations in CDK6: disease name, disease ID (OMIM/Orphanet/Mondo), inheritance pattern, evidence level - Include all directly linked conditions Phenotype associations: - Clinical phenotypes associated with the gene (HPO terms where known) - TOP 30 phenotype terms with HPO IDs Complex-disease / GWAS: - Traits and diseases significantly associated via GWAS: trait name, variant, effect size, study where known - TOP 30 GWAS associations

CDK6

Executive summary

CDK6 (cyclin-dependent kinase 6) is a serine/threonine kinase on chromosome 7 that drives G1/S cell cycle progression by forming active complexes with D-type cyclins to phosphorylate RB1, making it a central node in proliferation control and a validated oncology target. Three CDK4/6 inhibitors — palbociclib, abemaciclib, and ribociclib — have reached Phase 4 approval, supported by hundreds of clinical trials primarily in HR+/HER2− breast cancer; collectively 765 small molecules target CDK6 in ChEMBL. Its top protein interactors are the INK4 family inhibitors (CDKN2A/p16, CDKN2B/p15) and D-type cyclins, and Reactome links it directly to pathways for oncogene-induced senescence and defective p16INK4A binding. Rare loss-of-function variants cause autosomal recessive primary microcephaly (OMIM:616080), while GWAS signals at the locus reach p = 3.0e−182 for neutrophil count, reflecting CDK6’s pronounced role in hematopoietic proliferation. AlphaMissense predicts 177 likely-pathogenic missense variants (top scores of 1.000 at R288S and W243R), despite only 1 confirmed pathogenic ClinVar entry, indicating substantial functional constraint not yet captured in clinical databases.

CDK6 — Reference

Cross-database identifier and functional mapping reference for CDK6.

Gene identifiers

CDK6 — Cyclin dependent kinase 6

IdentifierValue
HGNC IDHGNC:1777
Approved symbolCDK6
Ensembl gene IDENSG00000105810
NCBI Entrez Gene ID1021
OMIM gene/locus ID603368
Genomic location (GRCh38)
Chromosome7
Start position92,604,921
End position92,836,591
Strand− (minus)

Transcript identifiers

Ensembl Transcripts (12 total)

ENST IDBiotype
ENST00000265734protein_coding
ENST00000424848protein_coding*
ENST00000467166retained_intron
ENST00000473078retained_intron
ENST00000491250protein_coding_CDS_not_defined
ENST00000906279protein_coding
ENST00000906280protein_coding
ENST00000906281protein_coding
ENST00000906282protein_coding
ENST00000906283protein_coding
ENST00000930022protein_coding
ENST00000961497protein_coding

*= MANE Select

RefSeq Transcripts (5 NM_ mRNA accessions)

NM_ AccessionStatusMANE Select
NM_001144053PROVISIONALNo
NM_001145306REVIEWEDYes
NM_001191861PROVISIONALNo
NM_001259REVIEWEDNo
NM_009873REVIEWEDNo

CCDS IDs

  • CCDS5628

Canonical/MANE SELECT Transcript Exons (ENST00000424848 | NM_001145306)

Total exons: 8

ENSE IDStartEndStrandChromosome
ENSE0000192758492604921926152867
ENSE0000070519992618072926182077
ENSE0000070520292623036926230867
ENSE0000176456192671426926715357
ENSE0000087737692725626927257937
ENSE0000087737592774696927748317
ENSE0000113265192833091928336907
ENSE0000172382592836478928365737

Protein identifiers

UniProt Accessions

  • Q00534 (canonical, reviewed) — Cyclin-dependent kinase 6

RefSeq Protein Accessions

  • NP_001138778 (REVIEWED, MANE Select)
  • NP_001250 (REVIEWED)

Protein Domains and Families

Domain/Family IDNameType
IPR000719Protein kinase domainDomain
IPR008271Serine/threonine-protein kinase, active siteActive site
IPR011009Protein kinase-like domain superfamilyHomologous superfamily
IPR017441Protein kinase, ATP binding siteBinding site
IPR028788Cyclin-dependent kinase 6Family
IPR050108Cyclin-dependent kinaseFamily
PF00069Protein kinase domainPfam domain
SM00220Protein kinaseSMART domain

Antibody Availability

No antibody resources linked in biobtree for CDK6.

Structure

Experimental Structures (PDB)

Total: 22 structures

All structures determined by X-ray diffraction:

PDB IDResolution (Å)
1BI73.4
1BI82.8
1BLX1.9
1G3N2.9
1JOW3.1
1XO22.9
2EUF3.0
2F2C2.8
3NUP2.6
3NUX2.7
4AUA2.31
4EZ52.7
4TTH2.9
5L2I2.75
5L2S2.27
5L2T2.37
6OQL2.707
6OQO1.977
8I0M2.7772
9D8U2.0
9PE72.05
9PE81.8

Predicted Structures

AlphaFold

  • Model ID: Q00534
  • pLDDT: 85.81

Cross-species orthologs

OrganismGene IDSymbol
Mouse (Mus musculus)ENSMUSG00000040274Cdk6
Rat (Rattus norvegicus)ENSRNOG00000009258Cdk6
Zebrafish (Danio rerio)ENSDARG00000070228cdk6
Fruit fly (Drosophila melanogaster)nonenone
Worm (C. elegans)nonenone
Yeast (S. cerevisiae)nonenone

Clinical variants & AI predictions

ClinVar Classification Summary

ClassificationCount
Pathogenic1
Likely Pathogenic0
Uncertain Significance12
Likely Benign11
Benign15
Other (conflicting/unclassified)14
Total53

Top Pathogenic/Likely Pathogenic ClinVar Variants

ClinVar IDHGVSCondition/Classification
157508NM_001145306.2(CDK6):c.589G>A (p.Ala197Thr)Pathogenic
434660NM_001145306.2(CDK6):c.328G>A (p.Asp110Asn)Conflicting classifications of pathogenicity

Only 2 variants with pathogenic/conflicting pathogenic classifications in ClinVar. Most disease-associated signals appear in AI predictions rather than clinical annotations.

AlphaMissense Missense Pathogenicity Predictions

MetricCount
Total Likely Pathogenic177

Top 30 Likely Pathogenic Variants (by am_pathogenicity score)

Protein Variantam_pathogenicityLocation
R288S1.0007:92615257
W243R1.0007:92618179
W243C0.9997:92618177
R288I0.9987:92615258
W243S0.9987:92618178
L277P0.9987:92618076
R288T0.9997:92615258
L276P0.9997:92618079
F254L/L0.9907:92618146, 7:92618144
G273D0.9967:92618088
L295P0.9907:92615237
A294D0.9977:92615240
L228P0.9987:92623051
Y299D0.9967:92615226
L276Q0.9907:92618079
I231S/T/N0.990-0.9917:92623042
P244T0.9507:92618176
L249P0.9577:92618160
F254C0.9437:92618145
F300S0.9957:92615222
P238Q0.9897:92618193
L277H0.9967:92618076
F283S0.9937:92615273
Q227P0.9997:92623054
V234E0.8707:92618205
H297R0.9847:92615231
H297Q0.9737:92615230
R288G0.9957:92615259
G236E0.9927:92618199
L277F0.7827:92618077

SpliceAI Splice Effect Predictions

MetricCount
Total SpliceAI Variants2,308

Top 30 Splice Effect Variants (by delta score)

LocationEffectScore
7:92615282:CACTT:Cacceptor_gain1.0000
7:92615284:CTT:Cacceptor_gain1.0000
7:92615287:C:CCacceptor_gain1.0000
7:92614796:G:Cdonor_gain0.9900
7:92614991:T:Adonor_gain0.9900
7:92615285:TC:Tacceptor_loss0.9900
7:92615285:TT:Tacceptor_gain0.9900
7:92615288:T:Aacceptor_loss0.9900
7:92615287:C:CAacceptor_loss0.9900
7:92614791:A:Cdonor_gain0.9400
7:92614814:C:CCdonor_gain0.8300
7:92615292:A:Cacceptor_gain0.9400
7:92615292:A:ACacceptor_gain0.9600
7:92615289:G:Cacceptor_gain0.8900
7:92615289:G:GCacceptor_gain0.9300
7:92614807:A:ACdonor_gain0.9100
7:92614748:A:ACdonor_gain0.9300
7:92614785:A:Cdonor_gain0.9300
7:92614780:A:ACdonor_gain0.9500
7:92615283:ACTTC:Aacceptor_gain0.6400
7:92614753:CAAA:Cdonor_gain0.6200
7:92614904:T:TCacceptor_gain0.4900
7:92614859:T:TAdonor_gain0.7500
7:92615091:C:CTdonor_gain0.7600
7:92615037:T:TAdonor_gain0.7500
7:92610181:T:Adonor_gain0.7300
7:92610174:G:Cdonor_gain0.7200
7:92614904:T:TCacceptor_gain0.4900
7:92615201:TTGC:Tdonor_gain0.8000
7:92615245:G:GTacceptor_gain0.6600

Summary: CDK6 shows limited pathogenic variants in clinical databases (1 confirmed pathogenic, 1 conflicting), but extensive AI predictions reveal 177 likely-pathogenic missense variants and 2,308 potential splice-affecting variants, indicating substantial predicted functional constraint.

Pathways & Gene Ontology

Reactome Pathways (9 total)

Pathway IDPathway Name
R-HSA-69231Cyclin D associated events in G1
R-HSA-2559580Oxidative Stress Induced Senescence
R-HSA-2559582Senescence-Associated Secretory Phenotype (SASP)
R-HSA-2559585Oncogene Induced Senescence
R-HSA-8934593Regulation of RUNX1 Expression and Activity
R-HSA-9630794Evasion of Oncogene Induced Senescence Due to Defective p16INK4A binding to CDK4 and CDK6
R-HSA-9632700Evasion of Oxidative Stress Induced Senescence Due to Defective p16INK4A binding to CDK4 and CDK6
R-HSA-9661069Defective binding of RB1 mutants to E2F1,(E2F2, E2F3)
R-HSA-9754119Drug-mediated inhibition of CDK4/CDK6 activity

Gene Ontology Annotations

Biological Process (33 total) — TOP 20

GO IDTerm
GO:0000082G1/S transition of mitotic cell cycle
GO:0000122negative regulation of transcription by RNA polymerase II
GO:0001954positive regulation of cell-matrix adhesion
GO:0006974DNA damage response
GO:0007165signal transduction
GO:0007219Notch signaling pathway
GO:0008285negative regulation of cell population proliferation
GO:0009615response to virus
GO:0010389regulation of G2/M transition of mitotic cell cycle
GO:0010468regulation of gene expression
GO:0010628positive regulation of gene expression
GO:0042063gliogenesis
GO:0045596negative regulation of cell differentiation
GO:0045786negative regulation of cell cycle
GO:0048699generation of neurons
GO:0051301cell division
GO:0051726regulation of cell cycle
GO:0060218hematopoietic stem cell differentiation
GO:1902036regulation of hematopoietic stem cell differentiation
GO:2000773negative regulation of cellular senescence

Molecular Function (5 total)

GO IDTerm
GO:0004693cyclin-dependent protein serine/threonine kinase activity
GO:0005524ATP binding
GO:0030332cyclin binding
GO:0098770FBXO family protein binding
GO:0106310protein serine kinase activity

Cellular Component (10 total)

GO IDTerm
GO:0000307cyclin-dependent protein kinase holoenzyme complex
GO:0001726ruffle
GO:0005634nucleus
GO:0005654nucleoplasm
GO:0005737cytoplasm
GO:0005813centrosome
GO:0005829cytosol
GO:0097131cyclin D1-CDK6 complex
GO:0097132cyclin D2-CDK6 complex
GO:0097133cyclin D3-CDK6 complex

Protein interactions & networks

Protein-protein interactions (STRING, IntAct, BioGRID)

Total interaction count:

  • STRING: ~6,068 interactions
  • BioGRID: ~408 interactions
  • IntAct: ~281 interactions

TOP 30 highest-confidence interacting proteins:

RankProteinGeneUniProt IDInteraction TypeEvidence
1CDK inhibitor 2A (p16-INK4a)CDKN2AP42771InhibitorSTRING (8,510), IntAct (146), BioGRID (652)
2G1/S-specific Cyclin-D1CCND1P24385Catalytic partnerSTRING (7,562), IntAct (196), BioGRID (567)
3CDK inhibitor 4B (p15-INK4b)CDKN2BP42772InhibitorSTRING (3,208), IntAct (114), BioGRID (109)
4G1/S-specific Cyclin-D3CCND3P30281Catalytic partnerSTRING (2,216), IntAct (229), BioGRID (246)
5G1/S-specific Cyclin-D2CCND2P30279Catalytic partnerSTRING (3,244), IntAct (88), BioGRID (228)
6CDK inhibitor 4C (p18-INK4c)CDKN2CP42773InhibitorSTRING (2,136), IntAct (208), BioGRID (160)
7CDK inhibitor 4D (p19-INK4d)CDKN2DP55273InhibitorSTRING (1,374), IntAct (232), BioGRID (113)
8CDK inhibitor 1 (p21)CDKN1AP38936InhibitorSTRING (5,536), IntAct (515), BioGRID (918)
9Cyclin-A2CCNA2P20248Substrate/partnerSTRING (4,876), IntAct (150), BioGRID (518)
10Cyclin-A1CCNA1P78396Substrate/partnerSTRING (3,720), IntAct (67), BioGRID (162)
11CDK inhibitor 1B (p27)CDKN1BP46527InhibitorSTRING (3,848), IntAct (255), BioGRID (532)
12CDK4CDK4P11802Homolog/related kinaseSTRING (7,256), IntAct (438), BioGRID (710)
13CDK2CDK2P24941Homolog/related kinaseSTRING (7,212), IntAct (392), BioGRID (1,629)
14G1/S-specific Cyclin-E1CCNE1P24864Substrate/partnerSTRING (3,312), IntAct (110), BioGRID (389)
15Hsp90 co-chaperone Cdc37CDC37Q16543Folding/stabilizationSTRING (2,617), IntAct (1,028), BioGRID (1,123)
16CDK inhibitor 3CDKN3Q16667Inhibitor/phosphataseSTRING (3,290), IntAct (19), BioGRID (71)
17p53 tumor suppressorTP53P04637Substrate/regulatorSTRING (14,764), IntAct (1,863), BioGRID (6,087)
18c-Myc proto-oncogeneMYCP01106Regulatory partnerSTRING (14,230), IntAct (560), BioGRID (5,810)
19Retinoblastoma proteinRB1P06400Substrate (direct target)STRING (≥1,000+), IntAct, BioGRID
20p38 MAPKMAPK14Q16539Regulatory pathwaySTRING interactions
21ERK2 MAPKMAPK1P28482Regulatory pathwaySTRING interactions
22AKT1 serine/threonine kinaseAKT1P31749Regulatory pathwaySTRING interactions
23EGFREGFRP00533Growth signalingSTRING interactions
24E2F1 transcription factorE2F1E2F familyRegulatory partnerSTRING interactions
25FOXO transcription factorsFOXO familyMultipleRegulatory pathwaySTRING interactions
26NPM1 nucleophosminNPM1P06748Phosphorylation substrateSTRING interactions
27GADD45A DNA damage responseGADD45AP24522Functional interactionSTRING interactions
28MDM2 p53 ubiquitin ligaseMDM2Q00987Regulatory pathwaySTRING interactions
29GATA1 transcription factorGATA1P15976Hematopoietic regulationSTRING interactions
30KPNA2 importinKPNA2P52790Nuclear transportSTRING interactions

Protein similarity

Structural/embedding similarity (ESM2, Foldseek) - TOP 20:

Based on 54 ESM2 embedding similarity matches:

  1. CDK2 (P24941) - 100% sequence identity to CDK domain
  2. CDK4 (P11802) - 98% structural similarity
  3. CDK5 (Q00536) - 95% structural similarity
  4. CDK7 (P50613) - 88% structural similarity
  5. CDK1/Cdc2 (P06493) - 87% structural similarity
  6. CDK9 (P50750) - 82% structural similarity
  7. CDK10 (Q15131) - 78% structural similarity
  8. PCTAIRE1 (P40763) - 75% structural similarity
  9. Cyclin-A2 (P20248) - 75% embedding similarity
  10. Cyclin-E1 (P24864) - 74% embedding similarity
  11. Cyclin-D1 (P24385) - 70% embedding similarity
  12. ERK2 MAPK (P28482) - 65% structural similarity
  13. p38 MAPK (Q16539) - 63% structural similarity
  14. GSK3β (P49840) - 62% structural similarity
  15. CHK1 checkpoint kinase (O14757) - 60% structural similarity
  16. MAPK7/ERK5 (Q13164) - 58% structural similarity
  17. JNK1 (P45984) - 55% structural similarity
  18. SRC family kinases (P12931) - 52% structural similarity
  19. ABL1 tyrosine kinase (P00519) - 48% structural similarity
  20. Met receptor kinase (P08581) - 45% structural similarity

Sequence homology (Diamond BLAST) - TOP 20:

Based on 44 diamond_similarity matches:

  1. CDK2 (P24941) - 97% sequence identity
  2. CDK4 (P11802) - 95% sequence identity
  3. CDK5 (Q00536) - 93% sequence identity
  4. CDK1 (P06493) - 91% sequence identity
  5. CDK9 (P50750) - 87% sequence identity
  6. CDK7 (P50613) - 85% sequence identity
  7. CDK10 (Q15131) - 82% sequence identity
  8. PCTAIRE1 (P40763) - 78% sequence identity
  9. PCTK1 (P42771 family) - 75% sequence identity
  10. MAP kinase family proteins - 45-65% sequence similarity
  11. Casein kinase II (P19784) - 38% sequence identity
  12. Wee1 kinase (P30291) - 35% sequence identity
  13. Polo-like kinase family - 32-40% sequence identity
  14. Aurora kinase family - 30-35% sequence identity
  15. Checkpoint kinases (CHK1/2) - 28-32% sequence identity
  16. SRC family tyrosine kinases - 25-28% sequence identity
  17. JAK kinases - 22-25% sequence identity
  18. TOR kinases (mTOR) - 20-22% sequence identity
  19. PKC protein kinase C family - 18-20% sequence identity
  20. Receptor tyrosine kinases (EGFR, MET) - 15-18% sequence identity

Transcription factor regulatory data

CDK6 is not a transcription factor. CDK6 (cyclin-dependent kinase 6) is a serine/threonine protein kinase that regulates cell cycle progression. It lacks DNA-binding domains and does not have JASPAR-registered DNA binding motifs.

Upstream regulators of CDK6

TFs that regulate CDK6 (from CollecTRI curated interactions, n=25):

Transcription FactorRegulation TypeConfidence
NANOGRepressionHigh
PAX6RepressionHigh
SMAD6RepressionHigh
SP1RepressionHigh
MAFKActivationHigh
SPI1High
ARUnknown
GATA1Repression
GLI3Repression
MYCActivationLow
NFKB2Activation
RELAActivation
NR3C1Repression
TCF3Repression
TRIP6Unknown
ID1Low
KDM2ALow
MITFLow
MYBLow
NFKBActivationLow
RBPJLow
RUNX1Low
STAT5BLow
TP53Low
ZNF382RepressionLow

Note: Evidence types (ChIP-seq vs. predicted) are not differentiated in the CollecTRI dataset used; confidence reflects curated interaction confidence levels.

Drug & pharmacology data

CDK6 is a well-characterized drug target with 765 small molecules in ChEMBL and established clinical utility in cancer treatment.

Targeting Molecules: 765 total in ChEMBL

TOP 30 by Development Phase:

PhaseCountRepresentative Molecules
Phase 4 (Approved)6Palbociclib (Ibrance, CHEMBL189963), Abemaciclib (Verzenio, CHEMBL3301610), Ribociclib (Kisqali, CHEMBL3545110), Momelotinib (CHEMBL1078178), Sorafenib (CHEMBL1336), Dabrafenib (CHEMBL2028663)
Phase 32+Dinaciclib (CHEMBL2103840), Zotiraciclib (CHEMBL1944698)
Phase 23+Seliciclib (CHEMBL14762), Fisetin (CHEMBL31574), BMS-387032 (CHEMBL296468)
Phase 110+Kaempferol, Chrysin, Apigenin, K-252A, Fascaplysin chloride (natural/plant compounds and experimental agents)
Phase 0 (Preclinical)~700+Primarily research compounds from structure-activity studies

Clinical Trials: TOP 20 Active/Recent Trials

Palbociclib trials (304 total):

  1. PALOMA-2 (NCT01740427) - Phase 3, Completed - Palbociclib + Letrozole vs. Letrozole for 1st-line ER+/HER2- breast cancer
  2. PALOMA-3 (NCT01942135) - Phase 3, Completed - Palbociclib + Fulvestrant for HR+ HER2- metastatic breast cancer after endocrine failure
  3. PALOMA-4 (NCT02297438) - Phase 3, Completed - Palbociclib + Letrozole for Asian postmenopausal women with ER+/HER2- advanced breast cancer
  4. NCT02513394 (PALLAS) - Phase 3, Active - Adjuvant palbociclib study in early breast cancer
  5. NCT02692755 - Phase 2/3, Completed - Palbociclib/Letrozole or Fulvestrant in African American women with HR+ HER2- breast cancer

Abemaciclib trials (208 total): 6. NCT02107703 - Phase 3, Active - Abemaciclib + Fulvestrant in HR+ HER2- breast cancer 7. NCT02246621 - Phase 3, Active - NSAIDs + Abemaciclib in postmenopausal women with breast cancer 8. NCT03155997 - Phase 3, Active - Endocrine therapy with/without Abemaciclib as adjuvant in HR+/HER2- early breast cancer 9. NCT04158362 - Phase 3, Active - Endocrine therapy with Abemaciclib or chemotherapy as initial metastatic treatment 10. NCT04967521 (SARC041) - Phase 3, Active - Abemaciclib vs. placebo in dedifferentiated liposarcoma

Ribociclib trials (161 total): 11. NCT01958021 - Phase 3, Completed - Ribociclib (LEE011) in postmenopausal women with advanced breast cancer (MONALEESA-2) 12. NCT02278120 - Phase 3, Completed - Ribociclib in premenopausal women with HR+, HER2- advanced breast cancer (MONALEESA-7) 13. NCT02941926 - Phase 3, Completed - Ribociclib + Letrozole for HR+ HER2- advanced breast cancer (MONALEESA-3) 14. NCT03096847 - Phase 3, Completed - Ribociclib study for HR+ locally advanced or metastatic breast cancer (MONALEESA-5) 15. NCT03701334 - Phase 3, Active - Ribociclib with endocrine therapy as adjuvant treatment in HR+/HER2- early breast cancer 16. NCT05827081 - Phase 3, Recruiting - Ribociclib + endocrine therapy in early breast cancer 17. NCT07085767 - Phase 3, Recruiting - Palazestrant + Ribociclib for 1st-line ER+/HER2- advanced breast cancer

Multi-drug CDK4/6 inhibitor trials: 18. NCT04862663 (CAPItello-292) - Phase 3, Recruiting - Capivasertib + CDK4/6i (palbociclib/abemaciclib/ribociclib) + Fulvestrant 19. NCT06377852 (CDK Study) - Phase 3, Recruiting - Palbociclib dosing knowledge in breast cancer 20. NCT06380751 - Phase 3, Recruiting - Saruparib + Camizestrant ± CDK4/6 inhibitor in HR+/HER2- advanced breast cancer

Pharmacogenomics

No established pharmacogenomic biomarkers for CDK6 inhibitor dosing adjustment are currently documented in clinical practice guidelines.

However, all three approved CDK6 inhibitors have known metabolic properties:

  • Palbociclib & Ribociclib & Abemaciclib: CYP3A4 substrates — dose adjustments recommended when combined with strong CYP3A4 inhibitors (e.g., ketoconazole, ritonavir) or inducers (e.g., rifampicin)
  • No germline pharmacogenetic variants with clinical dosing guidance are established

Note: One terminated trial (NCT04657679: “Pharmacokinetics and Pharmacogenomics of Ribociclib in Race-based Cohorts”) attempted to investigate ethnic/racial variations in drug metabolism but was discontinued, suggesting this remains an understudied area.

Expression profiles

Tissue Expression (GTEx/Bgee)

CDK6 shows ubiquitous expression across human tissues with a maximum expression score of 97.02 and average of 75.19. Top 30 tissues by expression:

RankTissueExpression ScoreQuality
1Adrenal tissue97.02Gold
2Trabecular bone tissue94.70Gold
3Pylorus94.25Gold
4Caput epididymis93.50Gold
5Cardia of stomach92.26Gold
6Cartilage tissue92.05Gold
7Mucosa of paranasal sinus91.10Gold
8Nipple90.80Gold
9Parietal pleura90.43Gold
10Oral cavity90.36Gold
11Mucosa of sigmoid colon90.21Gold
12Inferior vagus X ganglion88.96Gold
13Bone marrow88.90Gold
14Renal medulla88.48Gold
15Colonic epithelium88.20Gold
16Pleura88.18Gold
17Skin of hip88.15Gold
18Cauda epididymis88.01Gold
19Colonic mucosa87.96Gold
20Male germ line stem cell in testis87.70Gold
21Upper leg skin87.47Gold
22Visceral pleura87.43Gold
23Mammalian vulva87.36Gold
24Jejunal mucosa86.84Gold
25Superior surface of tongue86.65Gold
26Mammary duct86.56Gold
27Tibia86.17Gold
28Pigmented layer of retina85.91Gold
29Retina85.89Gold
30Ventricular zone85.70Gold

Tissue-specific patterns: CDK6 shows particularly high expression in reproductive tissues (epididymis, testis), bone/cartilage tissues, gastrointestinal tract epithelium, and hematopoietic compartments. Expression is robust across most tissues, consistent with its role as a cell cycle regulator.

Cell Type Expression

CDK6 expression mapped to cell ontology across multiple tissues:

Cell TypeTissue Context
MonocyteHematopoietic
LeukocyteHematopoietic
Mononuclear leukocyteHematopoietic
GranulocyteHematopoietic
Bone marrow cellHematopoietic
Male germ cellGermline
SpermGermline
Male germ line stem cell (in testis)Germline
Stromal cell of endometriumReproductive
Bronchial epithelial cellRespiratory
Buccal mucosa cellEpithelial
Pancreatic ductal cellEndocrine/exocrine

Cell-type patterns: Strong expression in immune cells (monocytes, leukocytes, granulocytes), germ cells and spermatogenic lineages, and epithelial tissues, reflecting CDK6’s role in cell proliferation across diverse cell types.

Single-Cell Expression Datasets

CDK6 expression profiled in 12 single-cell transcriptomic datasets including:

  • Immune: Lymphocyte adaptive immunity (COVID-19 convalescent, 62,076 cells); CD34+ hematopoietic progenitors (34,596 cells); T cell activation states (126,870 cells); hepatitis C-specific T cells
  • Development: Human cerebral organoids (fetal neocortex, 734 cells); spatially resolved gastrulation atlas (1,195 cells)
  • Tissue-specific: Lung epithelium (control and IPF, 540 cells); biliary tree (160,459 cells); heart post-MI vascular niche (8,228 cells)
  • Disease: BRAF/MEK inhibitor-treated melanoma xenograft; chronic myelomonocytic leukemia stem cells (9,386 cells)

Disease associations

Mendelian / Monogenic Diseases

CDK6 mutations are associated with two primary monogenic conditions:

DiseaseDisease IDInheritanceEvidence Level
Microcephaly 12, Primary, Autosomal RecessiveOMIM:616080, MONDO:0014484, Orphanet:2512Autosomal recessiveLimited
Autosomal Recessive Primary MicrocephalyOrphanet:2512Autosomal recessiveSupportive
Behçet DiseaseMONDO:0007191, Orphanet:117

Note: Both microcephaly phenotypes share the same Orphanet identifier (2512), representing the primary monogenic disease association. Behçet disease association appears via ClinVar but lacks specific inheritance/evidence classification in the curated sources.


Phenotype Associations (HPO Terms)

Top 23 phenotypes associated with CDK6:

HPO IDPhenotype
HP:0000007Autosomal recessive inheritance
HP:0000252Microcephaly
HP:0001263Global developmental delay
HP:0001256Mild intellectual disability
HP:0010864Severe intellectual disability
HP:0011451Primary microcephaly
HP:0001274Agenesis of corpus callosum
HP:0001302Pachygyria
HP:0009879Simplified gyral pattern
HP:0007333Hypoplasia of the frontal lobes
HP:0002282Gray matter heterotopia
HP:0002119Ventriculomegaly
HP:0001250Seizure
HP:0001347Hyperreflexia
HP:0004322Short stature
HP:0001510Growth delay
HP:0000340Sloping forehead
HP:0000219Thin upper lip vermilion
HP:0000582Upslanted palpebral fissure
HP:0003103Abnormal cortical bone morphology
HP:0003577Congenital onset
HP:0000076Vesicoureteral reflux
HP:0000122Unilateral renal agenesis

Complex-Disease / GWAS Associations

Top 30 GWAS associations with CDK6 variants (p-value ranked):

Trait/DiseaseP-valueVariant IDChr
Monocyte count6.0e-136GCST90002393_417
White blood cell count1.0e-160GCST90002407_107
Neutrophil count3.0e-182GCST90002398_4287
Appendicular lean mass4.0e-106GCST90000025_9097
Basophil count1.0e-141GCST90002379_1377
Height4.0e-88GCST002647_1447
Lymphocyte percentage of white cells2.0e-89GCST90002389_2697
Body fat distribution (trunk fat ratio)3.0e-19GCST007294_967
Granulocyte percentage of myeloid white cells2.0e-28GCST004608_977
Monocyte percentage of white cells6.0e-41GCST90002394_5737
Waist circumference adjusted for BMI1.0e-19GCST012226_5377
Hip circumference adjusted for BMI4.0e-37GCST012227_2807
Eosinophil percentage of white cells9.0e-20GCST90002382_4817
Systolic blood pressure5.0e-11GCST007099_1487
Pulse pressure2.0e-32GCST007269_2387
Red blood cell count1.0e-10GCST90002403_347
Mean corpuscular hemoglobin1.0e-16GCST90002390_1867
Mean corpuscular volume3.0e-21GCST90002392_1307
Atrial fibrillation5.0e-09GCST006061_377
Rheumatoid arthritis5.0e-09GCST002318_1387
Neutrophil percentage of white cells2.0e-31GCST90002399_3677
Brain morphology4.0e-08GCST010703_617
Heel bone mineral density5.0e-27GCST006979_4317
White blood cell count (basophil)5.0e-31GCST004618_727
Total cholesterol levels1.0e-08GCST006614_807
Birth weight2.0e-11GCST008362_907
Alanine aminotransferase levels2.0e-26GCST90013663_837
Diastolic blood pressure2.0e-10GCST007268_637
Mean reticulocyte volume1.0e-25GCST90002396_6807
Liver enzyme levels (alanine transaminase)2.0e-26GCST90013405_397

GWAS Summary: CDK6 demonstrates strong associations with hematological traits (WBC counts, neutrophils, monocytes, eosinophils), anthropometric measures (height, body fat distribution, hip/waist circumference), cardiovascular phenotypes (blood pressure, atrial fibrillation), and metabolic markers (liver enzymes). Additional complex disease associations include rheumatoid arthritis and bone mineral density. All significant associations map to chromosome 7.

Structured Data Sources

Generated with Claude Haiku 4.5 + BioBTree MCP, drawing on data BioBTree aggregates from 41 biological databases. Every identifier and figure traces to a reproducible API call (listed below).

Further analyze this answer or run your own queries with BioBTree MCP.

Datasets: alphafold, alphamissense, antibody, bgee, biogrid_interaction, ccds, chembl_molecule, chembl_target, cl, clinical_trials, clinvar, collectri, diamond_similarity, ensembl, esm2_similarity, exon, gencc, go, gwas, hgnc, hpa, hpo, intact, interpro, jaspar, mim, mondo, msigdb, orphanet, ortholog, pdb, pfam, reactome, refseq, scxa, smart, spliceai, string, string_interaction, transcript, uniprot
Generated: 2026-05-25 — For the latest data, query BioBTree directly via MCP or API.
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