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Publication : The therapeutic potential of nuclear receptor modulators for treatment of metabolic disorders: PPARγ, RORs, and Rev-erbs.

First Author  Marciano DP Year  2014
Journal  Cell Metab Volume  19
Issue  2 Pages  193-208
PubMed ID  24440037 Mgi Jnum  J:210541
Mgi Id  MGI:5571423 Doi  10.1016/j.cmet.2013.12.009
Citation  Marciano DP, et al. (2014) The therapeutic potential of nuclear receptor modulators for treatment of metabolic disorders: PPARgamma, RORs, and Rev-erbs. Cell Metab 19(2):193-208
abstractText  Nuclear receptors (NRs) play central roles in metabolic syndrome, making them attractive drug targets despite the challenge of achieving functional selectivity. For instance, members of the thiazolidinedione class of insulin sensitizers offer robust efficacy but have been limited due to adverse effects linked to activation of genes not involved in insulin sensitization. Studies reviewed here provide strategies for targeting subsets of PPARgamma target genes, enabling development of next-generation modulators with improved therapeutic index. Additionally, emerging evidence suggests that targeting the NRs ROR and Rev-erb holds promise for treating metabolic syndrome based on their involvement in circadian rhythm and metabolism.
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