PHGY 210 Lecture Notes - Lecture 6: Thiazolidinedione, Insulin Resistance, Orphan Receptor
28 Nov 2015
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Most highly expressed in tissues that display high rates of fatty acid metabolism: subsequent to discovery that ppar bound peroxisomal proliferators, it was discovered that. Ppar bound certain types of fatty acids and their metabolites: more recently, shown that ligand-activated ppar receptors stimulated expression of several genes controlling fatty acid metabolism. Thus, some fatty acids can control their own metabolism through ppar by inducing the expression of genes encoding metabolic enzymes required for fatty acid catabolism. One of the most fascinating of all orphan receptors. Most highly expressed in adipose tissue intestine and spleen. First high affinity ligand for ppar was identified in large ligand screen at glaxo-wellcome, and turned out to be thiazolidinedione (tzd) Tzds are fascinating because they were originally developed as antidiabetic drugs, although their molecular targets were not known (this was not uncommon: the molecular target of aspirin was not known for over 100 years)
