PPARG
PPARG (Peroxisome proliferator-activated receptor gamma) is a protein that switches other genes on and off. The public catalogues list it as a drug target, and clinical evidence ties its variants to diagnosis, prognosis or drug response. Tied to Colorectal cancer, Thyroid cancer and Endometrial cancer.
Overview
Ligand-activated transcription factor that forms obligate heterodimers with the retinoic acid receptor and acts as a key regulator of biological processes, such as adipocyte differentiation, lipid metabolism, glucose homeostasis and beta-oxidation of fatty acids. Activated by lipid ligands: binds peroxisome proliferators, such as hypolipidemic drugs, and fatty acids, such as prostaglandin J2 metabolites. Ligand-binding results in a conformational change in the receptor, promoting dissociation of repressors and recruitment of coactivators, and subsequent activation of target gene expression.
Open Targets scores its association with cancer at 0.79 (direct and indirect evidence; datatypes genetic literature 0.30, clinical 0.58, affected pathway 0.25, literature 1.00, genetic association 0.50, somatic mutation 0.93, animal model 0.38).
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · PPARG (Peroxisome proliferator-activated receptor gamma) is a protein that switches other genes on and off. The public catalogues list it as a drug target, and clinical evidence ties its variants to diagnosis, prognosis or drug response. Tied to Colorectal cancer, Thyroid cancer and Endometrial cancer.
- 1 · What it is
PPARG (Peroxisome proliferator-activated receptor gamma) is a protein that switches other genes on and off. The public catalogues list it as a drug target, and clinical evidence ties its variants to diagnosis, prognosis or drug response. Tied to Colorectal cancer, Thyroid cancer and Endometrial cancer.
- 2 · What goes wrong in cancer
Ligand-activated transcription factor that forms obligate heterodimers with the retinoic acid receptor and acts as a key regulator of biological processes, such as adipocyte differentiation, lipid metabolism, glucose homeostasis and beta-oxidation of fatty acids.
- 3 · How drugs use it
No product in this corpus aims at PPARG 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:9236 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt P37231 (protein name, function text, keywords and locations (REST API)); Open Targets ENSG00000132170 (association with cancer (MONDO_0004992) 0.79; per-cancer scores at or above 0.5: colorectal cancer 0.59, endometrial cancer 0.54, thyroid cancer 0.56 (GraphQL API, CC0))
Biology
Ligand-activated transcription factor that forms obligate heterodimers with the retinoic acid receptor and acts as a key regulator of biological processes, such as adipocyte differentiation, lipid metabolism, glucose homeostasis and beta-oxidation of fatty acids. Activated by lipid ligands: binds peroxisome proliferators, such as hypolipidemic drugs, and fatty acids, such as prostaglandin J2 metabolites. Ligand-binding results in a conformational change in the receptor, promoting dissociation of repressors and recruitment of coactivators, and subsequent activation of target gene expression. Specifically binds to DNA specific PPAR response elements (PPRE) and modulates the transcription of its target genes, such as acyl-CoA oxidase. Acts as a critical regulator of gut homeostasis by suppressing NF-kappa-B-mediated pro-inflammatory responses. Plays a role in the regulation of cardiovascular circadian rhythms by regulating the transcription of BMAL1 in the blood vessels. Location: Nucleus; Cytoplasm (UniProt). Locus 3p25.2 (HGNC).
- Colorectal cancer: Open Targets association 0.59 with colorectal cancer (MONDO_0005575)
- Thyroid cancer: Open Targets association 0.56 with thyroid cancer (MONDO_0002108)
- Endometrial cancer: Open Targets association 0.54 with endometrial cancer (MONDO_0011962)
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: Open Targets known-drug datatype score 0.58. 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:"PPARG" OR ABSTRACT:"PPARG" OR TITLE:"peroxisome proliferator activated receptor gamma" OR ABSTRACT:"peroxisome proliferator activated receptor gamma" OR TITLE:"Peroxisome proliferator-activated receptor gamma" OR ABSTRACT:"Peroxisome proliferator-activated receptor gamma" OR TITLE:"PPARG1" OR ABSTRACT:"PPARG1" OR TITLE:"PPARG2" OR ABSTRACT:"PPARG2" OR TITLE:"NR1C3" OR ABSTRACT:"NR1C3") 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 PPARG, not a curated reading list.
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