1999
DOI: 10.1073/pnas.96.1.266
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Structural requirements of ligands for the oxysterol liver X receptors LXRα and LXRβ

Abstract: LXR␣ and -␤ are nuclear receptors that regulate the metabolism of several important lipids, including cholesterol and bile acids. Previously, we have proposed that LXRs regulate these pathways through their interaction with specific, naturally occurring oxysterols, including 22(R)-hydroxycholesterol, 24(S)-hydroxycholesterol, and 24(S),25-epoxycholesterol. Using a ligand binding assay that incorporates scintillation proximity technology to circumvent many of the problems associated with assaying extremely hydr… Show more

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Cited by 868 publications
(704 citation statements)
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“…For the GM colony formation assay, Lin − cells were resuspended in Iscove's modified Dulbecco's medium supplemented with 2% FBS and plated in mouse methylcellulose‐based medium containing FBS, stem cell factor, interleukin‐3, interleukin‐6, and erythropoietin (StemCell Technologies), supplemented with 10% interleukin‐3 culture supplement (VWR) and 2 ng/mL GM colony‐stimulating factor (R&D Systems) 33. The cell suspension for either assay was plated at a concentration of 103 Lin − cells/mL in 6‐well SmartDish plates using 16‐gauge blunt‐ended needles (StemCell Technologies) at a volume of 1 mL per well and incubated at 37°C with 5% CO 2 for 7 days (EPC colony formation assay) or 10 days (GM colony formation assay). For activation of LXRs, 1 μmol/L GW3965 (Tocris) was added to each medium mix before plating.…”
Section: Methodsmentioning
confidence: 99%
See 1 more Smart Citation
“…For the GM colony formation assay, Lin − cells were resuspended in Iscove's modified Dulbecco's medium supplemented with 2% FBS and plated in mouse methylcellulose‐based medium containing FBS, stem cell factor, interleukin‐3, interleukin‐6, and erythropoietin (StemCell Technologies), supplemented with 10% interleukin‐3 culture supplement (VWR) and 2 ng/mL GM colony‐stimulating factor (R&D Systems) 33. The cell suspension for either assay was plated at a concentration of 103 Lin − cells/mL in 6‐well SmartDish plates using 16‐gauge blunt‐ended needles (StemCell Technologies) at a volume of 1 mL per well and incubated at 37°C with 5% CO 2 for 7 days (EPC colony formation assay) or 10 days (GM colony formation assay). For activation of LXRs, 1 μmol/L GW3965 (Tocris) was added to each medium mix before plating.…”
Section: Methodsmentioning
confidence: 99%
“…Widely referred to as the “cholesterol‐sensing nuclear receptors,” LXRs are endogenously activated by oxysterols, which are oxidized derivatives of cholesterol. LXRα and LXRβ share 77% sequence homology in their ligand‐binding domain and largely appear to have overlapping transcriptional functions 3, 4. Interest in LXRs as potential drug targets stems from their potent capability to induce reverse cholesterol transport by increasing expression of the cholesterol efflux transporters Abca1 and Abcg1 5, 6.…”
mentioning
confidence: 99%
“…LXRa and LXRb (also known as NR1H3 and NR1H2, respectively) were originally thought of as 'orphan' nuclear receptors as their natural ligands were not known. The naturally occurring oxysterols 22-R-hydroxycholesterol and 24,25-epoxycholesterol and long-chain fatty acids have since been identified as ligands for LXR (Janowski et al, 1999). LXRa is highly expressed in the liver but also at lower levels in adrenal glands, intestine, adipose, macrophages, kidney and lung whereas LXRb is more ubiquitously expressed (Repa and Mangelsdorf, 2000).…”
Section: Nuclear Receptorsmentioning
confidence: 99%
“…Some oxysterols were identified as natural ligands for LXR [4], and have anti-allergic activity; e.g., topical application of LXR-activating oxysterols in mice reduces irritant and allergic cutaneous inflammation [5]. More recently, Heine et al reported that activation of LXRs reduces IgE production from B cells stimulated with anti-CD40 and IL-4 [6].…”
Section: Introductionmentioning
confidence: 99%