Liver X Receptor Beta Library
Liver X receptors (LXRs) are nuclear receptors that regulate the metabolism of cholesterol and bile acids. LXRs function as nuclear cholesterol sensors that are activated in response to elevated intracellular cholesterol levels in multiple cell types.
Stimulation of LXR by agonists activates a number of genes that are involved in the regulation of lipid metabolism and cholesterol efflux from cells. The ability of LXRs to promote reverse cholesterol transport, to limit inflammation, and to improve glucose tolerance makes them attractive targets for drugs developed for the treatment of cardiovascular, metabolic, and/or inflammatory diseases. Synthetic LXR agonists promote cholesterol efflux and inhibit inflammation in vivo and inhibit the development of atherosclerosis in animal models. Unfortunately, known ligands share the undesirable side effect of inducing lipogenesis and hypertriglyceridemia by transactivating genes involved in fatty acid biosynthesis.
OTAVAchemicals offers new Liver X receptor (LXR) target-focused library which is targeted towards Liver X receptor β and comprises 486 compounds.
To design this library we performed molecular docking of our Drug-Like Collection
of compounds in crystal structure of human LXRβ (PDB ID: 1UPV). The most important polar interaction of a ligand and LXRβ is a hydrogen bond with His435. This bond is observed in many LXR receptor-ligand complexes, including those with steroid compounds. The presence of this hydrogen bond has been used as a criteria to filter docking results in order to identify the most consistent binding modes. Finally, the complexes retained after filtering were subjected to visual analysis to exclude ligands with inappropriate binding.
The library comprises drug-like compounds only.
All compounds are in stock, cherry-picking is available.
The library (DB, SD, XLS, PDF format) as well as the price-list is available on request. Feel free to contact us or use on-line form below to send an inquiry if you are interested to obtain this library or if you need more information.
Zelcer N, Tontonoz P. Liver X receptors as integrators of metabolic and inflammatory signaling. J Clin Invest. 2006 116(3) 607-14
Quinet EM, Savio DA, Halpern AR, Chen L, Miller CP, Nambi P. Gene-selective modulation by a synthetic oxysterol ligand of the liver X receptor. J Lipid Res. 2004 (10) 1929-42