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26 sources retrieved · Most recent: April 2026 · Index updated 15 days ago
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WEE1
WEE1 G2 checkpoint kinase
Chromosome 11 · 11p15.4
NCBI Gene: 7465Ensembl: ENSG00000166483.13HGNC: HGNC:12761UniProt: P30291
242PubMed Papers
20Diseases
2Drugs
0Pathogenic Variants
FUNCTIONAL ROLE
Kinase
RESEARCH IMPACT
Trending
CLINICAL
Clinical Trials
DATA QUALITY
✓ Experimental GO Evidence✓ Swiss-Prot Reviewed
protein bindingnegative regulation of G2/M transition of mitotic cell cyclenucleusnucleolusneurodegenerative diseaseactinic keratosiscutaneous squamous cell carcinomasquamous cell carcinoma
✦AI Summary

WEE1 is a crucial cell cycle checkpoint kinase that acts as a negative regulator of mitotic entry by controlling the G2/M transition 1. The primary function involves phosphorylating and inactivating cyclin B1-complexed CDK1 on tyrosine-15, preventing premature mitosis and maintaining genomic stability 2. WEE1 activity peaks during S and G2 phases and decreases at M phase through hyperphosphorylation and protein degradation. Mechanistically, WEE1 functions within the ATR-CHK1-WEE1 pathway that controls S and G2/M checkpoints, particularly important when the G1 checkpoint is compromised in cancer 1. In cancer contexts, WEE1 exhibits dual roles as both tumor suppressor in normal cells and pseudo-oncogene in malignant cells 3. Disease relevance is significant in cancers with TP53 mutations, where WEE1 inhibition enhances apoptosis through mitotic catastrophe by promoting uncontrolled G2/M transition and reducing DNA damage response proteins like CHK2 and Rad51 4. Clinical significance includes the development of WEE1 inhibitors as cancer therapeutics, showing particular promise in TP53-mutated tumors and when combined with chemotherapy or other targeted agents, though optimal biomarkers and treatment combinations are still being defined 5 6.

Sources cited
1
WEE1 functions in the ATR-CHK1-WEE1 pathway controlling S and G2/M checkpoints
PMID: 32508294
2
WEE1 regulates CDK1 activation and mitotic entry through complex signaling networks
PMID: 31602636
3
WEE1 has dual roles as tumor suppressor in normal cells and pseudo-oncogene in cancer cells
PMID: 32958072
4
WEE1 inhibition enhances apoptosis in KRAS-mutant NSCLC with TP53 mutations through mitotic catastrophe
PMID: 38776912
5
Clinical development of WEE1 inhibitors shows promise but faces challenges with toxicity and biomarker identification
PMID: 34269904
6
Cyclin E1 overexpression serves as a potential biomarker for WEE1 inhibitor sensitivity in ovarian cancer
PMID: 39994376
Disease Associationsⓘ20
neurodegenerative diseaseOpen Targets
0.52Moderate
actinic keratosisOpen Targets
0.44Moderate
cutaneous squamous cell carcinomaOpen Targets
0.41Moderate
squamous cell carcinomaOpen Targets
0.41Moderate
neuroinflammatory disorderOpen Targets
0.38Weak
skin neoplasmOpen Targets
0.33Weak
skin diseaseOpen Targets
0.33Weak
skin cancerOpen Targets
0.33Weak
Alzheimer diseaseOpen Targets
0.26Weak
Parkinson diseaseOpen Targets
0.19Weak
multiple sclerosisOpen Targets
0.19Weak
lysosomal storage diseaseOpen Targets
0.18Weak
neoplasmOpen Targets
0.13Weak
small cell lung carcinomaOpen Targets
0.12Weak
ovarian cancerOpen Targets
0.12Weak
glioblastoma multiformeOpen Targets
0.11Weak
Endometrial Serous AdenocarcinomaOpen Targets
0.10Weak
triple-negative breast cancerOpen Targets
0.10Suggestive
acute myeloid leukemiaOpen Targets
0.10Suggestive
gastric cancerOpen Targets
0.09Suggestive
Pathogenic Variants
No pathogenic variants reported on ClinVar for this gene.
View on ClinVar ↗
Drug Targets2
ADAVOSERTIBPhase II
Serine/threonine-protein kinase WEE1 inhibitor
ovarian cancer
AZENOSERTIBPhase II
Serine/threonine-protein kinase WEE1 inhibitor
Endometrial Serous Adenocarcinoma
Related Genes
CCNA2Protein interaction100%CCNA1Protein interaction99%CCNB1Protein interaction99%CCNB2Protein interaction96%CDCA3Protein interaction94%CABLES1Protein interaction94%
Tissue Expression6 tissues
Heart
100%
Bone Marrow
59%
Liver
32%
Brain
29%
Ovary
26%
Lung
22%
Gene Interaction Network
Click a node to explore
WEE1CCNA2CCNA1CCNB1CCNB2CDCA3CABLES1
PROTEIN STRUCTURE
Preparing viewer…
PDB8BJU · 1.53 Å · X-ray
View on RCSB ↗
Constraintⓘ
LOEUFⓘ
0.41Moderately Constrained
pLIⓘ
1.00Intolerant
Observed/Expected LoF0.25 [0.17–0.41]
RankingsWhere WEE1 stands among ~20K protein-coding genes
  • #1,623of 20,598
    Most Researched242 · top 10%
  • #2,055of 17,882
    Most Constrained (LOEUF)0.41 · top quartile
Genes detectedWEE1
Sources retrieved26 papers
Response time—
📄 Sources
26▼
1
DNA damage checkpoint kinases in cancer.
PMID: 32508294
Expert Rev Mol Med · 2020
1.00
2
A WEE1 family business: regulation of mitosis, cancer progression, and therapeutic target.
PMID: 32958072
J Hematol Oncol · 2020
0.90
3
Macrophage WEE1 Directly Binds to and Phosphorylates NF-κB p65 Subunit to Induce Inflammatory Response and Drive Atherosclerosis.
PMID: 40202104
Adv Sci (Weinh) · 2025
0.84
4
Discovery of CRBN-Dependent WEE1 Molecular Glue Degraders from a Multicomponent Combinatorial Library.
PMID: 39499896
J Am Chem Soc · 2024
0.80
5
Checkpoint kinase Wee1 activation drives inflammation and hypertrophy through the protein kinase B/phosphoinositide 3-kinases-nuclear factor κB pathway in cardiomyocytes.
PMID: 40396291
Eur Heart J · 2026
0.76