Therapeutic role of peroxisome proliferator-activated receptors in obesity, diabetes and inflammation.
Peroxisome proliferator-activated receptors (PPARs) are members of the nuclear receptor family and play a significant role in regulation of lipid metabolism, hepatic peroxisomal enzyme expression, insulin sensitivity and glucose homeostasis. PPARs have been classified into three subtypes encoded by different genes: PPARalpha (NR1C1), PPARdelta (NR1C2), and PPARgamma (NR1C3). Each subtype of PPARs appears to be differently expressed in a tissue-specific manner because of their binding to specific consensus DNA sequences, known as PPREs (peroxisome proliferator response elements). Thus, PPARs have emerged as potential molecular targets for the design and synthesis of a different class of compounds, considering the conformation of receptors for the treatment of human metabolic disorders. This review covers the rapid progress made in functional analysis of PPARs and progress made towards the identification of ligands for each subtype receptor.
Ram
Vishnu Ji
VJ
Medicinal Chemistry Division, Central Drug Research Institute, Lucknow 226001, India. vjiram@yahoo.com
D000818:Animals; D003920:Diabetes Mellitus / Q000188:drug therapy*; D006801:Humans; D007249:Inflammation / Q000188:drug therapy*; D009765:Obesity / Q000188:drug therapy*; D018160:Receptors, Cytoplasmic and Nuclear / Q000187:drug effects / Q000502:physiology*; D014157:Transcription Factors / Q000187:drug effects / Q000502:physiology*
D018160:Receptors, Cytoplasmic and Nuclear; D014157:Transcription Factors