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Details on Person PPAR-alpha is activated by binding polyunsaturated fatty aci...

Class:IdSummation:400148
_displayNamePPAR-alpha is activated by binding polyunsaturated fatty aci...
_timestamp2025-06-06 20:56:24
created[InstanceEdit:400195] May, B, 2009-03-24 02:23:25
modified[InstanceEdit:422134] May, B, 2009-05-26 17:27:28
[InstanceEdit:425911] May, B, 2009-06-08
[InstanceEdit:9709902] Stephan, Ralf, 2020-12-18
[InstanceEdit:9954125] D'Eustachio, Peter, 2025-06-06
textPPAR-alpha is activated by binding polyunsaturated fatty acids especially those having 18-22 carbon groups and 2-6 double bonds such as linoleiate, linolenate, arachidonate, and eicosapentaenoate. These ligands bind the C-terminal region of PPAR-alpha. The fibrate drugs are also agonists of PPAR-alpha.
Binding of a ligand causes a conformational change in PPAR-alpha so that it recruits coactivators. By analogy with the closely related receptor PPAR-gamma, PPAR-alpha probably binds TBL1 and TBLR1, which are responsible for recruiting the 19S proteasome to degrade corepressors during the exchange of corepressors for coactivators. The coactivators belong to the CBP-SRC-HAT complex (CBP/p300, SRC1, SRC2, SRC3, CARM1, SWI/SNF, BAF60C, PRIC320, and PRIC285), the ASC complex (PRIP/ASC2, PIMT), and the TRAP-DRIP-ARC-MEDIATOR complex (TRAP130, PBP/TRAP220). The coactivators contain LXXLL motifs (Nuclear Receptor Boxes) that interact with the AF-2 region in nuclear receptors such as PPAR-alpha. Additionally bilirubin binds to PPAR-alpha and acts as coactivator.
(summation)[BlackBoxEvent:400143] Fatty acid ligands activate PPARA [Homo sapiens]
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