Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

PPARA (Q07869) - Overview - Molecular Target Synopsis

Protein


PPARA, Peroxisome proliferator-activated receptor alpha
UniProt Q07869

Also Known as PPARA_HUMAN, PPARA, NR1C1, PPAR

Ligand-activated transcription factor. Key regulator of lipid metabolism. Activated by the endogenous ligand 1-palmitoyl-2-oleoyl-sn-glycerol-3-phosphocholine (16:0/18:1-GPC). Activated by oleylethanolamide, a naturally occurring lipid that regulates satiety. Receptor for peroxisome proliferators such as hypolipidemic drugs and fatty acids. Regulates the peroxisomal beta-oxidation pathway of fatty acids. Functions as transcription activator for the ACOX1 and P450 genes. Transactivation activity requires heterodimerization with RXRA and is antagonized by NR2C2. May be required for the propagation of clock information to metabolic pathways regulated by PER2. Heterodimer; with RXRA. This heterodimerization is required for DNA binding and transactivation activity. Interacts with NCOA3 coactivator. Interacts with CITED2; the interaction stimulates its transcriptional activity. Also interacts with PPARBP in vitro. Interacts with AKAP13, LPIN1, PRDM16 and coactivator NCOA6. Interacts with ASXL1 and ASXL2. Interacts with PER2. Interacts with SIRT1; the interaction seems to be modulated by NAD(+) levels (PubMed:24043310).

5HYK
CRYSTAL STRUCTURE OF THE COMPLEX PPARALPHA/AL26-29
RCSB/PDB
Inspect Structure
See all 3D Structures for PPARA

Isoforms / Transcripts (Protein Coding)


Drugs


PPARA is targeted by Approved Drugs Fenofibric Acid, Clofibrate, Fenofibrate, Gemfibrozil. (see details)
Fenofibric Acid
Clofibrate
Fenofibrate
Gemfibrozil

Sub-cellular localization


UniProt: PPARA is active in the following subcellular-locations: nucleus.
GO terms: PPARA is active in the following subcellular-locations: nucleoplasm, nucleus, RNA polymerase II transcription factor complex.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project PPARA has gain in 3 cell-lines, loss in 3 cell-lines and no signal in 999 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: HCC_2998, COLO205, MDA_N

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: HM7, IM-95m, IM-95

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: SK-N-SH, A549, IMR-90

(see details)

3D Structures


For PPARA there are:
18 structures (30 chains) solved
18 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


PPARA has been screened with 3816 compounds (7746 bioactivities), 1143 compounds have bioactivities that show binding affinity of <= 500nM (1808 bioactivities). (see details)