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PsychedeliaDokholyan Laboratory
TargetOther named receptors

Oxysterols receptor LXR-beta

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

NR1H2_HUMANNR1H2Homo sapiens

Oxysterols receptor LXR-beta

Nuclear receptor that exhibits a ligand-dependent transcriptional activation activity25661920. 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; DLDLR and LRP8. 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 (By similarity). 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). Plays an anti-inflammatory role during the hepatic acute phase response by acting as a corepressor: inhibits the hepatic acute phase response by preventing dissociation of the N-Cor corepressor complex20159957

Quoted from UniProt’s FUNCTION annotation for P55055 (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
RXRA0.9980.9090.9000.827
RXRB0.9930.9800.5000.315
ABCA10.9910.6280.8000.900
NCOA20.9750.9690.0000.230
RXRG0.9510.9290.0000.291
XPR10.9320.0000.0000.932
NCOA10.9230.8060.5000.274
NR1H30.9150.0000.9000.171
OGT0.9030.0710.9000.046
ABCG50.8980.0530.4000.821

Where it sits in the cell

  • Nucleoplasm
  • Vesiclesadditional

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

UniProt, curated Nucleus

Expression by cell type

Single cell type RNA, the 1 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Syncytiotrophoblasts191 nCPM

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 — 67.4 nTPM, from NR1H2cerebellum — 46.2 nTPM, from NR1H2hippocampal formation — 48.7 nTPM, from NR1H2amygdala — 50.2 nTPM, from NR1H2hypothalamus — 46.0 nTPM, from NR1H2thalamus — no resolved target expressed herebasal ganglia — 53.5 nTPM, from NR1H2medulla 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 53.8, spinal cord 50.6, pituitary gland 43.7, retina 8.7.

Body

heart — 91.3 nTPM, from NR1H2smooth muscle — 18.9 nTPM, from NR1H2lung — 71.5 nTPM, from NR1H2liver — 64.0 nTPM, from NR1H2kidney — 71.1 nTPM, from NR1H2stomach — 62.9 nTPM, from NR1H2duodenum — 40.5 nTPM, from NR1H2small intestine — 59.1 nTPM, from NR1H2colon — 83.4 nTPM, from NR1H2adrenal gland — 65.9 nTPM, from NR1H2thyroid gland — 61.3 nTPM, from NR1H2pancreas — 46.9 nTPM, from NR1H2urinary bladder — 83.4 nTPM, from NR1H2skeletal muscle — 140.7 nTPM, from NR1H2spleen — 61.1 nTPM, from NR1H2salivary gland — 50.4 nTPM, from NR1H2
0141 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 NR1H2 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

  • cerebral cortex67.4 nTPM
  • midbrain53.8 nTPM
  • basal ganglia53.5 nTPM
  • spinal cord50.6 nTPM
  • amygdala50.2 nTPM
  • hippocampal formation48.7 nTPM
  • cerebellum46.2 nTPM
  • hypothalamus46.0 nTPM
  • pituitary gland43.7 nTPM
  • retina8.7 nTPM

Peripheral and autonomic · 16

  • skeletal muscle140.7 nTPM
  • heart muscle91.3 nTPM
  • colon83.4 nTPM
  • urinary bladder83.4 nTPM
  • lung71.5 nTPM
  • kidney71.1 nTPM
  • adrenal gland65.9 nTPM
  • liver64.0 nTPM
  • stomach 162.9 nTPM
  • thyroid gland61.3 nTPM
  • spleen61.1 nTPM
  • small intestine59.1 nTPM
  • salivary gland50.4 nTPM
  • pancreas46.9 nTPM
  • duodenum40.5 nTPM
  • smooth muscle18.9 nTPM

Transcript is not protein. These are RNA levels for NR1H2, 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-betaOther named receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291836
Oxysterols receptor LXR-betaOther named receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291837
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