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PsychedeliaDokholyan Laboratory
TargetOther named receptors

Oxysterols receptor LXR-alpha

A named receptor outside the families above. The catch-all is explicit rather than silent: these are receptors, but they are not grouped.

Measurements
2
Compounds
1
Binding constants
0
Median pX
—

I · Identity

What this target is

Its function as UniProt states it, where in a cell the protein is found, and which cell types and tissues transcribe its gene.

Protein

NR1H3_HUMANNR1H3Homo sapiens

Oxysterols receptor LXR-alpha

Nuclear receptor that exhibits a ligand-dependent transcriptional activation activity19481530,25661920,37478846. Interaction with retinoic acid receptor (RXR) shifts RXR from its role as a silent DNA-binding partner to an active ligand-binding subunit in mediating retinoid responses through target genes defined by LXRES37478846. LXRES are DR4-type response elements characterized by direct repeats of two similar hexanuclotide half-sites spaced by four nucleotides (By similarity). Plays an important role in the regulation of cholesterol homeostasis, regulating cholesterol uptake through MYLIP-dependent ubiquitination of LDLR, VLDLR and LRP819481530. Interplays functionally with RORA for the regulation of genes involved in liver metabolism (By similarity). Induces LPCAT3-dependent phospholipid remodeling in endoplasmic reticulum (ER) membranes of hepatocytes, driving SREBF1 processing and lipogenesis (By similarity). Via LPCAT3, triggers the incorporation of arachidonate into phosphatidylcholines of ER membranes, increasing membrane dynamics and enabling triacylglycerols transfer to nascent very low-density lipoprotein (VLDL) particles. Via LPCAT3 also counteracts lipid-induced ER stress response and inflammation, likely by modulating SRC kinase membrane compartmentalization and limiting the synthesis of lipid inflammatory mediators (By similarity)

Quoted from UniProt’s FUNCTION annotation for Q13133 (reviewed). The superscript numbers are UniProt’s own PubMed citations, kept in the sentence and in order, each linking to the paper it names.

What it acts with

STRING’s highest-confidence human functional partners. The combined score mixes several kinds of evidence, so each channel is shown separately — a partner supported by experiment is a different claim from one supported only by text mining, and for a receptor this is where its coupling appears as evidence rather than as assertion.

PartnerCombinedExperimentDatabaseText mining
RXRA0.9990.9860.9000.812
RXRB0.9980.9820.9000.338
NCOA10.9920.9780.5000.323
ABCA10.9670.0490.5000.935
SREBF10.9640.2920.5000.908
RXRG0.9610.9080.0000.569
NR0B20.9410.5100.0000.871
ABCG10.9320.0530.5000.862
NR1H20.9150.0000.9000.171
ABCG50.9120.0530.4000.846

Where it sits in the cell

  • Nucleoplasm
  • Cytosoladditional

Human Protein Atlas, by antibody immunofluorescence in cell lines — a different assay from the expression figures below, which are RNA.

UniProt, curated Nucleus · Cytoplasm

Expression by cell type

Single cell type RNA, the 4 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Kupffer cells226.5 nCPM
  • Late spermatids72.8 nCPM
  • Hepatocytes72 nCPM
  • Enterocytes68.6 nCPM

Expression by tissue

The tissues this gene is enriched in, by consensus RNA. A tissue absent from this list is one the Atlas does not call specific for this gene, which is not the same as absent from it.

  • liver84.3 nTPM

II · Anatomy

Where the gene is transcribed

The same two atlases the compound plates use, asked about this gene alone. Brain on the left, peripheral and autonomic tissues on the right.

Brain

cerebral cortex — 7.5 nTPM, from NR1H3cerebellum — 3.8 nTPM, from NR1H3hippocampal formation — 6.3 nTPM, from NR1H3amygdala — 8.0 nTPM, from NR1H3hypothalamus — 6.0 nTPM, from NR1H3thalamus — no resolved target expressed herebasal ganglia — 10.4 nTPM, from NR1H3medulla oblongata — no resolved target expressed here

basal ganglia: drawn as the caudate nucleus, putamen and globus pallidus.

Measured but not drawn — this anatomogram has no outline for them: midbrain 10.6, pituitary gland 7.2, spinal cord 5.9, retina 2.1.

Body

heart — 18.2 nTPM, from NR1H3smooth muscle — 7.3 nTPM, from NR1H3lung — 23.4 nTPM, from NR1H3liver — 84.3 nTPM, from NR1H3kidney — 23.2 nTPM, from NR1H3stomach — 15.6 nTPM, from NR1H3duodenum — 45.5 nTPM, from NR1H3small intestine — 38.6 nTPM, from NR1H3colon — 24.1 nTPM, from NR1H3adrenal gland — 19.3 nTPM, from NR1H3thyroid gland — 20.0 nTPM, from NR1H3pancreas — 15.8 nTPM, from NR1H3urinary bladder — 24.4 nTPM, from NR1H3skeletal muscle — 8.8 nTPM, from NR1H3spleen — 51.8 nTPM, from NR1H3salivary gland — 13.9 nTPM, from NR1H3
084 nTPM

Square-root ramp · shared scale across both plates

Shading is transcript level — not affinity, and not affinity combined with expression. Outlined but unshaded organs hold none of NR1H3 transcript above the atlas’s detection threshold. Anatomy from EMBL-EBI Anatomogram (Apache License 2.0); regions identified by Uberon (uberon.org), CC BY 3.0.

Brain · 10

  • midbrain10.6 nTPM
  • basal ganglia10.4 nTPM
  • amygdala8.0 nTPM
  • cerebral cortex7.5 nTPM
  • pituitary gland7.2 nTPM
  • hippocampal formation6.3 nTPM
  • hypothalamus6.0 nTPM
  • spinal cord5.9 nTPM
  • cerebellum3.8 nTPM
  • retina2.1 nTPM

Peripheral and autonomic · 16

  • liver84.3 nTPM
  • spleen51.8 nTPM
  • duodenum45.5 nTPM
  • small intestine38.6 nTPM
  • urinary bladder24.4 nTPM
  • colon24.1 nTPM
  • lung23.4 nTPM
  • kidney23.2 nTPM
  • thyroid gland20.0 nTPM
  • adrenal gland19.3 nTPM
  • heart muscle18.2 nTPM
  • pancreas15.8 nTPM
  • stomach 115.6 nTPM
  • salivary gland13.9 nTPM
  • skeletal muscle8.8 nTPM
  • smooth muscle7.3 nTPM

Transcript is not protein. These are RNA levels for NR1H3, shaded on √nTPM so that a three-order range stays legible — on a linear ramp every region but the strongest would read as blank, which looks like absence rather than less. A region carrying no shading is one the atlas reports no consensus value for, not one where the gene is silent. And a gene being transcribed somewhere is not evidence that any compound reaches it. Human Protein Atlas, RNA expression, nTPM (normalized transcripts per million), consensus tissue dataset.

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Functional readouts 2

IC₅₀, EC₅₀, AC₅₀ and potency. Assay-dependent, and not interchangeable with a binding constant.

TargetClassTypeValue (nM)pXOrganismAssay
Oxysterols receptor LXR-alphaOther named receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291838
Oxysterols receptor LXR-alphaOther named receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291839
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