Liver X receptor

Revision as of 13:17, 17 December 2017 by Michal Harel (talk | contribs)


Function

Liver X receptprs (LXR) are ligand-activated transcription factors of the nuclear receptor family. There are two LXR isoforms α and β which form heterodimers with retinoic X receptor upon activation and bind to the LXR response element found in the promoter region of the target genes[1]. LXR is a lipogenic transcription factor[2]. LXRs modulate the expression of genes in cholesterol and lipid metabolism in response to changes in cellular cholesterol status.

Disease

Treatment of mice demonstrating Wilson disease with LXR agonist reduced disease manifestations without worsening neurological symptoms associated with the conventional therapy based on copper chelation[3].

Relevance

LXRs have emerged as promising drug targets for anti-atherosclerotic therapies[4].

Structural highlights

Human liver X receptpr β ligand binding domain complex with retinoic X receptor β and modulator (PDB code 5kya)

Drag the structure with the mouse to rotate

3D Structures of liver X receptpr3D Structures of liver X receptpr

Updated on 17-December-2017

ReferencesReferences

  1. Baranowski M. Biological role of liver X receptors. J Physiol Pharmacol. 2008 Dec;59 Suppl 7:31-55. PMID:19258656
  2. Cha JY, Repa JJ. The liver X receptor (LXR) and hepatic lipogenesis. The carbohydrate-response element-binding protein is a target gene of LXR. J Biol Chem. 2007 Jan 5;282(1):743-51. doi: 10.1074/jbc.M605023200. Epub 2006 Nov, 14. PMID:17107947 doi:http://dx.doi.org/10.1074/jbc.M605023200
  3. Hamilton JP, Koganti L, Muchenditsi A, Pendyala VS, Huso D, Hankin J, Murphy RC, Huster D, Merle U, Mangels C, Yang N, Potter JJ, Mezey E, Lutsenko S. Activation of liver X receptor/retinoid X receptor pathway ameliorates liver disease in Atp7B(-/-) (Wilson disease) mice. Hepatology. 2016 Jun;63(6):1828-41. doi: 10.1002/hep.28406. Epub 2016 Feb 22. PMID:26679751 doi:http://dx.doi.org/10.1002/hep.28406
  4. Oosterveer MH, Grefhorst A, Groen AK, Kuipers F. The liver X receptor: control of cellular lipid homeostasis and beyond Implications for drug design. Prog Lipid Res. 2010 Oct;49(4):343-52. doi: 10.1016/j.plipres.2010.03.002. Epub, 2010 Apr 2. PMID:20363253 doi:http://dx.doi.org/10.1016/j.plipres.2010.03.002

Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)

Michal Harel, Joel L. Sussman, Jaime Prilusky, Alexander Berchansky