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.
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.
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.
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.
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.
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.
Broadly expressed or essential: HPA lists CHEK1 among essential proteins; a medicine acting on the wild-type protein would expose normal tissue too. HPA CHEK1: RNA tissue enhanced (bone marrow 25 nTPM, lymphoid tissue 20 nTPM, seminal vesicle 29 nTPM); no normal tissue stained high. Distribution: 2 cancer families in the corpus carry a prevalence row, label threshold or catalogue link for it (Prostate cancer, Lung cancer (all types)); Open Targets associates it with 0 specific cancer types at or above 0.5. (Rule 7 of scripts/fetch-target-specificity.ts.)
Sources: Human Protein Atlas CHEK1 tissue; Open Targets ENSG00000149554 associations
First described 1997. Earliest sequence paper UniProt cites for the protein: Sanchez et al, Science, 1997, "Conservation of the Chk1 checkpoint pathway in mammals: linkage of DNA damage to Cdk regulation through Cdc25". Source.
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))
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).
RNA: tissue enhanced (bone marrow 25 nTPM, lymphoid tissue 20 nTPM, seminal vesicle 29 nTPM), detected in many normal tissues.
No normal tissue stained high.
No cancer sample stained medium or high.
HPA CHEK1 tissue · HPA CHEK1 pathology · HPA protein class: Essential proteins
Human Protein Atlas version 25.1, antibody staining at reliability approved, enhanced or supported; used under CC BY-SA 3.0. Staining counts are patients per level in the atlas cohort, not population prevalence.
Query 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.
Shares Checkpoint (two meanings), CIViC.
Shares DNA damage response & homologous recombination, Prostate cancer.
Shares Checkpoint (two meanings), CIViC.
Shares Checkpoint (two meanings), CIViC.
Shares Checkpoint (two meanings), CIViC, Prostate cancer.
Shares Checkpoint (two meanings), CIViC.
Shares Checkpoint (two meanings), CIViC.