XCT-790 is a potent and selective inverse agonist ligand of the estrogen-related receptor alpha (ERRα).[1] Independent of its inhibition of ERRα, XCT-790 is a potent mitochondrial electron transport chain uncoupler.[2]

Mitochondrial electron transport chain uncoupling effect

XCT-790 has been shown to uncouple oxygen consumption from ATP production in mitochondria at very low, nanomolar-range doses independently of ERRα expression. Its effects are similar to proton ionophores such as FCCP, which disrupt mitochondrial transmembrane electrochemical gradients. This uncoupling leads to a fast drop in ATP production and, consequently, a prompt activation of AMPK.[2]

References

  1. ^ Busch BB, Stevens WC Jr, Martin R, Ordentlich P, Zhou S, Sapp DW, Horlick RA, Mohan R; Stevens (November 2004). "Identification of a selective inverse agonist for the orphan nuclear receptor estrogen-related receptor alpha". J. Med. Chem. 47 (23): 5593–6. doi:10.1021/jm049334f. PMID 15509154.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  2. ^ a b Eskiocak B; Aktar Ali; White MA (July 7, 2014). "The estrogen-related receptor α inverse agonist XCT 790 is a nanomolar mitochondrial uncoupler". Biochemistry. 53 (29): 4839–4846. doi:10.1021/bi500737n. PMC 4116149. PMID 24999922.


Allikas: http://en.wikipedia.org/wiki/XCT790
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