YAP1
YAP1 (Transcriptional coactivator YAP1) is a protein that switches other genes on and off. The public catalogues list it as a drug target and a biomarker, and clinical evidence ties its variants to diagnosis, prognosis or drug response. Tied to Oesophageal cancer and Breast cancer.
Overview
Transcriptional regulator with dual roles as a coactivator and corepressor. Critical downstream regulatory target in the Hippo signalling pathway, crucial for organ size control and tumour suppression by restricting proliferation and promoting apoptosis. The Hippo signalling pathway core involves a kinase cascade featuring STK3/MST2 and STK4/MST1, along with its regulatory partner SAV1, which phosphorylates and activates LATS1/2 in complex with their regulatory protein, MOB1.
CIViC holds 3 clinical evidence items and 0 assertions across 2 variants, naming Docetaxel, Verteporfin and Fluorouracil. Open Targets scores its association with cancer at 0.65 (direct and indirect evidence; datatypes affected pathway 0.27, literature 1.00, genetic association 0.00, somatic mutation 0.97, animal model 0.53).
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · YAP1 (Transcriptional coactivator YAP1) is a protein that switches other genes on and off. The public catalogues list it as a drug target and a biomarker, and clinical evidence ties its variants to diagnosis, prognosis or drug response. Tied to Oesophageal cancer and Breast cancer.
- 1 · What it is
YAP1 (Transcriptional coactivator YAP1) is a protein that switches other genes on and off. The public catalogues list it as a drug target and a biomarker, and clinical evidence ties its variants to diagnosis, prognosis or drug response. Tied to Oesophageal cancer and Breast cancer.
- 2 · What goes wrong in cancer
Transcriptional regulator with dual roles as a coactivator and corepressor.
- 3 · How drugs use it
No product in this corpus aims at YAP1 yet. Transcription factors have no pocket to plug, so drugs either degrade them or block the partner protein they need to dock on DNA.
External identifiers
Sources: HGNC HGNC:16262 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt P46937 (protein name, function text, keywords and locations (REST API)); CIViC gene YAP1 (3 evidence items, 0 assertions, 2 variants; diseases: Oesophageal Cancer (GraphQL API, CC0)); Open Targets ENSG00000137693 (association with cancer (MONDO_0004992) 0.65; per-cancer scores at or above 0.5: breast cancer 0.54 (GraphQL API, CC0))
Biology
Transcriptional regulator with dual roles as a coactivator and corepressor. Critical downstream regulatory target in the Hippo signalling pathway, crucial for organ size control and tumour suppression by restricting proliferation and promoting apoptosis. The Hippo signalling pathway core involves a kinase cascade featuring STK3/MST2 and STK4/MST1, along with its regulatory partner SAV1, which phosphorylates and activates LATS1/2 in complex with their regulatory protein, MOB1. This activation leads to the phosphorylation and inactivation of the YAP1 oncoprotein and WWTR1/TAZ. Phosphorylation of YAP1 by LATS1/2 prevents its nuclear translocation, thereby regulating the expression of its target genes. The transcriptional regulation of gene expression requires TEAD transcription factors and modulates cell growth, anchorage-independent growth, and induction of epithelial-mesenchymal transition (EMT). Location: Cytoplasm; Nucleus; Cell junction, tight junction; Cell membrane (UniProt). Locus 11q22.1 (HGNC).
- Oesophageal cancer: CIViC evidence names this disease
- Breast cancer: Open Targets association 0.54 with breast cancer (MONDO_0007254)
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 3 clinical evidence items on its variants. 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:"YAP1" OR ABSTRACT:"YAP1" OR TITLE:"Yes1 associated transcriptional regulator" OR ABSTRACT:"Yes1 associated transcriptional regulator" OR TITLE:"Transcriptional coactivator YAP1" OR ABSTRACT:"Transcriptional coactivator YAP1" OR TITLE:"YAP65" OR ABSTRACT:"YAP65" OR TITLE:"YAP-1" OR ABSTRACT:"YAP-1") 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 YAP1, not a curated reading list.