PMID- 15828219 OWN - NLM STAT- MEDLINE DCOM- 20050527 LR - 20181201 IS - 0047-1852 (Print) IS - 0047-1852 (Linking) VI - 63 IP - 4 DP - 2005 Apr TI - [PPARs as molecular targets for drug discovery]. PG - 549-55 AB - Peroxisome proliferator-activated receptors (PPARs) are ligand-inducible transcription factors. PPARs form the heterodimers with retinoid X receptors (RXRs), and modulate specific gene expressions related to the lipid and carbohydrate metabolism. Since fibrate-type lipid-lowering agents and thiazolidinedione (TZD)-type antidiabetic agents are identified as PPARalpha and gamma agonists, respectively, a number of ligands for PPARs have been developed, including PPAR subtype-selective and dual agonists. Recent report that RXR antagonist exhibited antidiabetic and antiobestic activities in animal model experiments, PPARs partial agonists, antagonists, and RXR antagonists have been also synthesized and their function in vivo are under investigations. In this paper, recent studies on the ligands for the PPAR-RXR heterodimers are reviewed. FAU - Kagechika, Hiroyuki AU - Kagechika H AD - School of Biomedical Science, Tokyo Medical and Dental University. FAU - Miyachi, Hiroyuki AU - Miyachi H LA - jpn PT - Journal Article PT - Review PL - Japan TA - Nihon Rinsho JT - Nihon rinsho. Japanese journal of clinical medicine JID - 0420546 RN - 0 (Hypoglycemic Agents) RN - 0 (Peroxisome Proliferator-Activated Receptors) RN - 0 (Pregnane X Receptor) RN - 0 (Receptors, Cytoplasmic and Nuclear) RN - 0 (Receptors, Steroid) SB - IM MH - *Drug Design MH - Hypoglycemic Agents/therapeutic use MH - Peroxisome Proliferator-Activated Receptors/*agonists/*physiology MH - Pregnane X Receptor MH - Receptors, Cytoplasmic and Nuclear/antagonists & inhibitors/physiology MH - Receptors, Steroid/antagonists & inhibitors/physiology RF - 20 EDAT- 2005/04/15 09:00 MHDA- 2005/05/28 09:00 CRDT- 2005/04/15 09:00 PHST- 2005/04/15 09:00 [pubmed] PHST- 2005/05/28 09:00 [medline] PHST- 2005/04/15 09:00 [entrez] PST - ppublish SO - Nihon Rinsho. 2005 Apr;63(4):549-55.