Chapter 8. Modulators of peroxisome proliferator-activated receptors (PPARs)

摘要: Publisher Summary This chapter presents an overview of the modulators peroxisome proliferator-activated receptors (PPARs). PPARs comprise a family ligand-activated transcription factors belonging to nuclear receptor gene superfamily. There are three PPAR subtypes that products separate genes and commonly designated as PPARα, PPARγ, PPARδ. In addition ligand-binding domain (LBD), these also have N-terminal DNA binding domain. The is least well characterized bears little homology among subtypes. has somewhat greater remaining variation allows be pharmacologically distinct. Upon ligand, forms heterodimer with 9- cis -retinoic acid (RXR). highly conserved DNA-binding domains recognize, together their RXR partner, sequences (response elements) containing direct repeats hexanucleotide AGGTCA separated by one nucleotide. interacts downstream machinery ultimately turns on target genes. discusses X-ray crystal structures PPARδ fatty or synthetic fibrate ligand provides PPARα agonists, PPARγ modulators.