A human peroxisome-proliferator-activated receptor-gamma is activated by inducers of adipogenesis, including thiazolidinedione drugs

Eur J Biochem. 1996 Jul 1;239(1):1-7. doi: 10.1111/j.1432-1033.1996.0001u.x.


We have cloned a human cognate of the mouse peroxisome-proliferator-activated receptor-gamma (hPPAR gamma) from a human placenta cDNA library. Sequence analysis reveals a high degree of similarity with the mouse receptor and, like other PPAR, hPPAR gamma forms heterodimers with the retinoid X receptor alpha (RXR alpha) and binds in vitro to DNA elements containing direct repeats of the sequence TGACCT. In common with mouse PPAR gamma, hPPAR gamma is expressed strongly in adipose tissue, but significant levels also are detectable in placenta, lung and ovary. In vitro trans-activation data suggest hPPAR gamma is only poorly activated by xenobiotic peroxisome proliferators, although certain fatty acids and eicosanoids are potent activators of this receptor. Both mouse and human PPAR gamma are capable of being activated by thiazolidinedione drugs, although the two receptors appear to differ in their sensitivity to these compounds. Taken together, these data suggest a high degree of structural and functional similarity between mouse and human PPAR gamma, and provide evidence for variation in human receptor structure which may result in differential sensitivity to activators.

MeSH terms

  • Adipose Tissue / drug effects*
  • Adipose Tissue / metabolism
  • Amino Acid Sequence
  • Animals
  • Base Sequence
  • Benzopyrans / pharmacology
  • Chromans / pharmacology
  • DNA, Complementary
  • Fatty Acids / pharmacology
  • Humans
  • Mice
  • Molecular Sequence Data
  • Pioglitazone
  • RNA, Messenger / genetics
  • RNA, Messenger / metabolism
  • Receptors, Cytoplasmic and Nuclear / genetics
  • Receptors, Cytoplasmic and Nuclear / metabolism*
  • Thiazoles / pharmacology*
  • Thiazolidinediones*
  • Transcription Factors / genetics
  • Transcription Factors / metabolism*
  • Transcriptional Activation / drug effects
  • Troglitazone


  • Benzopyrans
  • Chromans
  • DNA, Complementary
  • Fatty Acids
  • RNA, Messenger
  • Receptors, Cytoplasmic and Nuclear
  • Thiazoles
  • Thiazolidinediones
  • Transcription Factors
  • Troglitazone
  • ciglitazone
  • Pioglitazone
  • englitazone

Associated data

  • GENBANK/X90563