CHEK2
CHEK2 (Serine/threonine-protein kinase Chk2) is a protein kinase, an enzyme that switches other proteins on by adding phosphate groups. The public catalogues list it as a drug target, an oncogene driver, a biomarker and a DNA repair gene, and clinical evidence ties its variants to diagnosis, prognosis or drug response. Tied to Breast cancer, Prostate cancer, Sarcomas and 5 more. This dossier gathers the 0 products (0 approved), 0 trials, 0 pathways and 0 resistance routes in the corpus that involve it, with external identifiers so it can be joined to UniProt, ChEMBL, Open Targets and the rest of biology.
Biology
Serine/threonine-protein kinase which is required for checkpoint-mediated cell cycle arrest, activation of DNA repair and apoptosis in response to the presence of DNA double-strand breaks. May also negatively regulate cell cycle progression during unperturbed cell cycles. Following activation, phosphorylates numerous effectors preferentially at the consensus sequence [L-X-R-X-X-S/T]. Regulates cell cycle checkpoint arrest through phosphorylation of CDC25A, CDC25B and CDC25C, inhibiting their activity. Inhibition of CDC25 phosphatase activity leads to increased inhibitory tyrosine phosphorylation of CDK-cyclin complexes and blocks cell cycle progression. May also phosphorylate NEK6 which is involved in G2/M cell cycle arrest. Location: Nucleus; Nucleus, PML body; Nucleus, nucleoplasm (UniProt). Locus 22q12.1 (HGNC).
- Breast cancer: Open Targets association 0.87 with breast cancer (MONDO_0007254); CIViC evidence names this disease
- Prostate cancer: Open Targets association 0.80 with prostate cancer (MONDO_0008315); CIViC evidence names this disease
- Sarcomas: Open Targets association 0.75 with sarcoma (MONDO_0005089)
- Colorectal cancer: Open Targets association 0.74 with colorectal cancer (MONDO_0005575)
- Ovarian cancer: Open Targets association 0.73 with ovarian cancer (MONDO_0008170)
- Lung cancer: Open Targets association 0.69 with lung cancer (MONDO_0008903)
External identifiers
Built from HGNC, Ensembl, UniProt and ChEMBL idsProducts by modality and phase
Browse products →No product in the corpus is aimed at this target yet.
Trials
Evidence ranking →No trial in the corpus names this target or one of its products.
Resistance routes
Unaddressed routes →The resistance atlas has no route that names this target.
Pathways
Pathway-to-drug matrix →No pathway diagram carries this target as a node.
Companion diagnostics
Assay registry →No companion diagnostic in the registry measures this target.
Preclinical models
All models →No model entry for this target yet; check the cancer entries on the models page.
Open questions
All open questions →No open questions recorded for this target yet. Suggest one.
Literature
Preprints →Query for this target: (TITLE:"CHEK2" OR ABSTRACT:"CHEK2" OR TITLE:"checkpoint kinase 2" OR ABSTRACT:"checkpoint kinase 2" OR TITLE:"Serine/threonine-protein kinase Chk2" OR ABSTRACT:"Serine/threonine-protein kinase Chk2" OR TITLE:"CDS1" OR ABSTRACT:"CDS1" OR TITLE:"CHK2" OR ABSTRACT:"CHK2" OR TITLE:"HuCds1" OR ABSTRACT:"HuCds1") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about CHEK2, not a curated reading list.
Export
The dossier as machine-readable JSON: identifiers from HGNC, Ensembl, UniProt and ChEMBL, products with status, trials, pathways, hotspots, open questions and assays. The full entity record is in the open API at /api/v1/entities/chek2.json. Licence CC BY-NC 4.0.