CHEK1
CHEK1 (Serine/threonine-protein kinase Chk1) is a protein kinase, an enzyme that switches other proteins on by adding phosphate groups. The public catalogues list it as a drug target, a biomarker and a DNA repair gene, and clinical evidence ties its variants to diagnosis, prognosis or drug response. Tied to Prostate cancer and Small-cell lung cancer.
Overview
Serine/threonine-protein kinase which is required for checkpoint-mediated cell cycle arrest and activation of DNA repair in response to the presence of DNA damage or unreplicated DNA. May also negatively regulate cell cycle progression during unperturbed cell cycles. This regulation is achieved by a number of mechanisms that together help to preserve the integrity of the genome.
CIViC holds 2 clinical evidence items and 0 assertions across 2 variants, naming Olaparib, Cisplatin and Prexasertib.
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · CHEK1 (Serine/threonine-protein kinase Chk1) is a protein kinase, an enzyme that switches other proteins on by adding phosphate groups. The public catalogues list it as a drug target, a biomarker and a DNA repair gene, and clinical evidence ties its variants to diagnosis, prognosis or drug response. Tied to Prostate cancer and Small-cell lung cancer.
- 1 · What it is
CHEK1 (Serine/threonine-protein kinase Chk1) is a protein kinase, an enzyme that switches other proteins on by adding phosphate groups. The public catalogues list it as a drug target, a biomarker and a DNA repair gene, and clinical evidence ties its variants to diagnosis, prognosis or drug response. Tied to Prostate cancer and Small-cell lung cancer.
- 2 · What goes wrong in cancer
Serine/threonine-protein kinase which is required for checkpoint-mediated cell cycle arrest and activation of DNA repair in response to the presence of DNA damage or unreplicated DNA.
- 3 · How drugs use it
No product in this corpus aims at CHEK1 yet. Kinases are switched on by binding ATP inside the cell, so most drugs are small molecules shaped to plug that ATP pocket.
External identifiers
Sources: HGNC HGNC:1925 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt O14757 (protein name, function text, keywords and locations (REST API)); CIViC gene CHEK1 (2 evidence items, 0 assertions, 2 variants; diseases: Lung Small Cell Carcinoma, Castration-resistant Prostate Carcinoma (GraphQL API, CC0))
Biology
Serine/threonine-protein kinase which is required for checkpoint-mediated cell cycle arrest and activation of DNA repair in response to the presence of DNA damage or unreplicated DNA. May also negatively regulate cell cycle progression during unperturbed cell cycles. This regulation is achieved by a number of mechanisms that together help to preserve the integrity of the genome. Recognises the substrate consensus sequence [R-X-X-S/T]. Binds to and phosphorylates CDC25A, CDC25B and CDC25C. Phosphorylation of CDC25A at 'Ser-178' and 'Thr-507' and phosphorylation of CDC25C at 'Ser-216' creates binding sites for 14-3-3 proteins which inhibit CDC25A and CDC25C. Location: Nucleus; Chromosome; Cytoplasm; Cytoplasm, cytoskeleton, microtubule organizing center, centrosome (UniProt). Locus 11q24.2 (HGNC).
- Prostate cancer: CIViC evidence names this disease
- Small-cell lung cancer: CIViC evidence names this disease
Notes
top- Written by scripts/fetch-cancer-genes.ts from CIViC, Open Targets, IntOGen, HGNC and UniProt; the function text is UniProt's, condensed and in UK spelling. Roles: CIViC lists 3 therapies; CIViC holds 2 clinical evidence items on its variants; UniProt keyword "DNA repair". Evidence tier "clinical-evidence" is the strongest of those signals.
- Prevalence not recorded: none of the sources gives a positivity rate.
Latest papers
topQuery for this target: (TITLE:"CHEK1" OR ABSTRACT:"CHEK1" OR TITLE:"checkpoint kinase 1" OR ABSTRACT:"checkpoint kinase 1" OR TITLE:"Serine/threonine-protein kinase Chk1" OR ABSTRACT:"Serine/threonine-protein kinase Chk1" OR TITLE:"CHK1" OR ABSTRACT:"CHK1") 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 CHEK1, not a curated reading list.
Similar pages
not linked directly; found by shared links- TargetPOLK
Shares DNA damage response & homologous recombination, Prostate cancer.
- PairingPARP inhibitor + AR pathway inhibitor (prostate)
Shares DNA damage response & homologous recombination, Prostate cancer.
- IdeaWhich patients' blood clones will become leukaemia after treatment?
Shares DNA damage response & homologous recombination, Prostate cancer.
- TermEnabling characteristic: genome instability and mutation
Shares DNA replication stress, DNA damage response & homologous recombination.
- TargetWEE1
Shares DNA replication stress, DNA damage response & homologous recombination.
- TargetMYC
Shares DNA replication stress, CIViC, Prostate cancer.
- PathwayBase excision repair, PARP & alkylation damage
Shares DNA replication stress, DNA damage response & homologous recombination, Prostate cancer.
- TargetATR
Shares DNA replication stress, DNA damage response & homologous recombination, Small-cell lung cancer.