Review of the structural and dynamic mechanisms of PPAR γ partial agonism

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dc.contributor.authorKroker, A.
dc.contributor.authorBruning, J.
dc.date.issued2015
dc.description.abstractPPARγ (peroxisome proliferator activated receptor γ) is a ligand activated transcription factor of the nuclear receptor superfamily that controls the expression of a variety of genes involved in fatty acid metabolism, adipogenesis, and insulin sensitivity. While endogenous ligands of PPARγ include fatty acids and eicosanoids, synthetic full agonists of the receptor, including members of the thiazolidinedione (TZD) class, have been widely prescribed for the treatment of type II diabetes mellitus (T2DM). Unfortunately, the use of full agonists has been hampered by harsh side effects with some removed from the market in many countries. In contrast, partial agonists of PPARγ have been shown to retain favourable insulin sensitizing effects while exhibiting little to no side effects and thus represent a new potential class of therapeutics for the treatment of T2DM. Partial agonists have been found to not only display differences in transcriptional and cellular outcomes, but also act through distinct structural and dynamic mechanisms within the ligand binding cavity compared to full agonists.
dc.description.statementofresponsibilityAlice J. Kroker and John B. Bruning
dc.identifier.citationPPAR Research, 2015; 2015:816856-1-816856-15
dc.identifier.doi10.1155/2015/816856
dc.identifier.issn1687-4757
dc.identifier.issn1687-4765
dc.identifier.orcidBruning, J. [0000-0002-6919-1824]
dc.identifier.urihttp://hdl.handle.net/2440/99423
dc.language.isoen
dc.publisherHindawi Publishing Corporation
dc.rightsCopyright © 2015 A. J. Kroker and J. B. Bruning. This is an open access article distributed under the Creative Commons Attribution License,which permits unrestricted use, distribution, and reproduction in any medium, provided the originalwork is properly cited.
dc.source.urihttps://doi.org/10.1155/2015/816856
dc.titleReview of the structural and dynamic mechanisms of PPAR γ partial agonism
dc.title.alternativeReview of the structural and dynamic mechanisms of PPAR gamma partial agonism
dc.typeJournal article
pubs.publication-statusPublished

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