PREX2
PREX2 is a gene that drives cell growth when it is altered. The public catalogues list it as a drug target, an oncogene driver, a tumour suppressor and a biomarker, and clinical evidence ties its variants to diagnosis, prognosis or drug response.
Overview
Functions as a RAC1 guanine nucleotide exchange factor (GEF), activating Rac proteins by exchanging bound GDP for free GTP. Its activity is synergistically activated by phosphatidylinositol 3,4,5-trisphosphate and the beta gamma subunits of heterotrimeric G protein. Mediates the activation of RAC1 in a PI3K-dependent manner.
CIViC holds 1 clinical evidence item and 0 assertions across 1 variant, naming Vemurafenib. Open Targets scores its association with cancer at 0.73 (direct and indirect evidence; datatypes literature 0.91, animal model 0.42, genetic association 0.45, somatic mutation 0.82). IntOGen calls it a driver in 13 cohorts (10 activating, 3 loss-of-function), covering Bladder Urothelial Carcinoma, Invasive Breast Carcinoma, Colon Adenocarcinoma, Diffuse Large B-Cell Lymphoma, NOS, Oesophageal Adenocarcinoma, Oesophageal Squamous Cell Carcinoma and others.
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · PREX2 is a gene that drives cell growth when it is altered. The public catalogues list it as a drug target, an oncogene driver, a tumour suppressor and a biomarker, and clinical evidence ties its variants to diagnosis, prognosis or drug response.
- 1 · What it is
PREX2 is a gene that drives cell growth when it is altered. The public catalogues list it as a drug target, an oncogene driver, a tumour suppressor and a biomarker, and clinical evidence ties its variants to diagnosis, prognosis or drug response.
- 2 · What goes wrong in cancer
Functions as a RAC1 guanine nucleotide exchange factor (GEF), activating Rac proteins by exchanging bound GDP for free GTP.
- 3 · How drugs use it
No product in this corpus aims at PREX2 yet. Drugs fit a pocket that exists only in one shape of the mutant protein and hold it there, off.
External identifiers
Sources: HGNC HGNC:22950 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt Q70Z35 (protein name, function text, keywords and locations (REST API)); CIViC gene PREX2 (1 evidence items, 0 assertions, 1 variants; diseases: Melanoma (GraphQL API, CC0)); Open Targets ENSG00000046889 (association with cancer (MONDO_0004992) 0.73; per-cancer scores at or above 0.5: colorectal cancer 0.55, gastric cancer 0.51, oesophageal cancer 0.52, melanoma 0.60, skin cancer 0.57, breast cancer 0.57 (GraphQL API, CC0)); IntOGen PREX2 (driver in 13 cohorts (Act 10, LoF 3); Compendium_Cancer_Genes.tsv release 20240920, CC0 1.0)
Biology
Functions as a RAC1 guanine nucleotide exchange factor (GEF), activating Rac proteins by exchanging bound GDP for free GTP. Its activity is synergistically activated by phosphatidylinositol 3,4,5-trisphosphate and the beta gamma subunits of heterotrimeric G protein. Mediates the activation of RAC1 in a PI3K-dependent manner. May be an important mediator of Rac signalling, acting directly downstream of both G protein-coupled receptors and phosphoinositide 3-kinase. Locus 8q13.2 (HGNC).
- Oesophageal cancer: Open Targets association 0.52 with oesophageal cancer (MONDO_0007576); IntOGen driver in 3 cohorts (ESCA, ESCC)
- Colorectal cancer: Open Targets association 0.55 with colorectal cancer (MONDO_0005575); IntOGen driver in 1 cohort (COAD)
- Gastric & gastro-oesophageal junction cancer: Open Targets association 0.51 with gastric cancer (MONDO_0001056); IntOGen driver in 1 cohort (STAD)
- Breast cancer: Open Targets association 0.57 with breast cancer (MONDO_0007254); IntOGen driver in 1 cohort (BRCA)
- Bladder & urothelial cancer: IntOGen driver in 1 cohort (BLCA)
- Hepatocellular carcinoma: IntOGen driver in 1 cohort (HCC)
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 1 therapies; IntOGen calls it an activating (Act) driver in 10 cohorts; IntOGen calls it a loss-of-function (LoF) driver in 3 cohorts; CIViC holds 1 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:"PREX2" OR ABSTRACT:"PREX2" OR TITLE:"phosphatidylinositol-3,4,5-trisphosphate dependent Rac exchange factor 2" OR ABSTRACT:"phosphatidylinositol-3,4,5-trisphosphate dependent Rac exchange factor 2" OR TITLE:"Phosphatidylinositol 3,4,5-trisphosphate-dependent Rac exchanger 2 protein" OR ABSTRACT:"Phosphatidylinositol 3,4,5-trisphosphate-dependent Rac exchanger 2 protein" OR TITLE:"DEP.2" OR ABSTRACT:"DEP.2" OR TITLE:"FLJ12987" OR ABSTRACT:"FLJ12987" OR TITLE:"P-REX2" OR ABSTRACT:"P-REX2") 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 PREX2, not a curated reading list.