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

PPARD (Q03181) - Overview - Molecular Target Synopsis

Protein


PPARD, Peroxisome proliferator-activated receptor delta
UniProt Q03181

Also Known as PPARD_HUMAN, PPARD, NR1C2, PPARB

Ligand-activated transcription factor. Receptor that binds peroxisome proliferators such as hypolipidemic drugs and fatty acids. Has a preference for poly-unsaturated fatty acids, such as gamma-linoleic acid and eicosapentanoic acid. Once activated by a ligand, the receptor binds to promoter elements of target genes. Regulates the peroxisomal beta-oxidation pathway of fatty acids. Functions as transcription activator for the acyl-CoA oxidase gene. Decreases expression of NPC1L1 once activated by a ligand. Heterodimer with the retinoid X receptor.

5Y7X
HUMAN PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR (PPAR) DELTA IN COMPLEXED WITH A POTENT AND SELECTIVE AGONIST
RCSB/PDB
Inspect Structure
See all 3D Structures for PPARD

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


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



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project PPARD has gain in 3 cell-lines, loss in 1 cell-lines and no signal in 1001 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SF_539, MDA_MB_231, U251

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: SW 1573, HCC4011, HCC2935

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: IMR-90, SK-N-SH, HUVEC

(see details)

3D Structures


For PPARD there are:
42 structures (80 chains) solved
40 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


PPARD has been screened with 2394 compounds (4519 bioactivities), 771 compounds have bioactivities that show binding affinity of <= 500nM (1430 bioactivities). (see details)