title: [Nuclear receptors PPAR as a drug target in metabolic disorders].
abstract: Nuclear receptors regulate many basic cellular processes and their malfunction can lead to serious consequences including metabolic disorders, obesity and type 2 diabetes. Among many nuclear receptor families, the best known for their therapeutic use are the PPARs. These are key transcription factors determining, proper cellular metabolism of glucose and lipids, tissue sensitivity to insulin, appropriate immune responses including inflammatory processes and finally cell division and differentiation. Currently two types of PPAR activators are in medical use: in the therapy of type 2 diabetes--thiazolidinediones (TZDs), which act via PPARgamma receptors and in the treatment of dyslipidemia-fibrates, which act via PPARalpha receptors. The search for new drugs acting through PPAR mechanism consists in the design of new molecules with tissue specific proprieties, which would selectively bind and modulate the activity of appropriate receptors, thus reducing the number of adverse events typically observed with the use of full agonists. These molecules have been named selective nuclear receptor modulators (SNuRMs).
authors.affiliation: Zakład Regulacji Metabolizmu, Instytut Biochemii, Wydział Biologii UW, Warszawa.
authors.forename: Marta
authors.initials: M
authors.lastname: Stolarczyk
authors.forename: Wojciech
authors.initials: W
authors.lastname: Gutman
authors.forename: Rafał A
authors.initials: RA
authors.lastname: Derlacz
mesh_terms: D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy; D015195:Drug Design; D006801:Humans; D008659:Metabolic Diseases / Q000188:drug therapy* / Q000378:metabolism; D047493:PPAR alpha / Q000819:agonists; D047495:PPAR gamma / Q000819:agonists; D047492:Peroxisome Proliferator-Activated Receptors / Q000819:agonists* / Q000378:metabolism; D045162:Thiazolidinediones / Q000494:pharmacology
chemical_list: D047493:PPAR alpha; D047495:PPAR gamma; D047492:Peroxisome Proliferator-Activated Receptors; D045162:Thiazolidinediones