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Complex Structure of LXR with an agonistComplex Structure of LXR with an agonist
Structural highlights
Function[NR1H2_HUMAN] Orphan receptor. Binds preferentially to double-stranded oligonucleotide direct repeats having the consensus half-site sequence 5'-AGGTCA-3' and 4-nt spacing (DR-4). Regulates cholesterol uptake through MYLIP-dependent ubiquitination of LDLR, VLDLR and LRP8 (By similarity). Evolutionary Conservation Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf. Publication Abstract from PubMedA series of 4-(3-aryloxyaryl)quinolines with sulfone substituents on the terminal aryl ring (7) was prepared as LXR agonists. High affinity LXR ligands with excellent agonist potency and efficacy in functional assays of LXR activity were identified. In general, these sulfone agonists were equal to or superior to previously described alcohol and amide analogs in terms of affinity, functional potency, and microsomal stability. Many of the sulfones had LXRbeta binding IC(50) values <10nM while the most potent compounds in an ABCA1 mRNA induction assay in J774 mouse cells had EC(50) values <10nM and were as efficacious as T0901317. 4-(3-Aryloxyaryl)quinoline sulfones are potent liver X receptor agonists.,Bernotas RC, Singhaus RR, Kaufman DH, Travins JM, Ullrich JW, Unwalla R, Quinet E, Evans M, Nambi P, Olland A, Kauppi B, Wilhelmsson A, Goos-Nilsson A, Wrobel J Bioorg Med Chem Lett. 2010 Jan 1;20(1):209-12. Epub 2009 Oct 31. PMID:19932617[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
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