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PsychedeliaDokholyan Laboratory
TargetEnzymes

Receptor tyrosine-protein kinase erbB-2

Named enzymes, including the metabolising cytochromes and the monoamine oxidases.

Measurements
18
Compounds
10
Binding constants
7
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

ERBB2_HUMANERBB2Homo sapiens

Receptor tyrosine-protein kinase erbB-2

Protein tyrosine kinase that is part of several cell surface receptor complexes, but that apparently needs a coreceptor for ligand binding. Essential component of a neuregulin-receptor complex, although neuregulins do not interact with it alone. GP30 is a potential ligand for this receptor. Regulates outgrowth and stabilization of peripheral microtubules (MTs). Upon ERBB2 activation, the MEMO1-RHOA-DIAPH1 signaling pathway elicits the phosphorylation and thus the inhibition of GSK3B at cell membrane. This prevents the phosphorylation of APC and CLASP2, allowing its association with the cell membrane. In turn, membrane-bound APC allows the localization of MACF1 to the cell membrane, which is required for microtubule capture and stabilization
In the nucleus is involved in transcriptional regulation. Associates with the 5'-TCAAATTC-3' sequence in the PTGS2/COX-2 promoter and activates its transcription. Implicated in transcriptional activation of CDKN1A; the function involves STAT3 and SRC. Involved in the transcription of rRNA genes by RNA Pol I and enhances protein synthesis and cell growth

Quoted from UniProt’s FUNCTION annotation for P04626 (reviewed).

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
ERBB40.9990.8500.9000.983
GRB70.9990.8400.5000.990
NRG10.9990.8980.9000.998
EGFR0.9990.9980.9000.983
ERBIN0.9990.8420.8000.993
GRB20.9990.9340.9000.993
SHC10.9990.9210.9000.991
ERBB30.9990.9970.9000.984
CD440.9990.6950.9000.992
SRC0.9990.8500.9000.980

Where it sits in the cell

  • Plasma membrane
  • Nucleoplasmadditional
  • Cytosoladditional

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

UniProt, curated Cell membrane · Cell projection, ruffle membrane · Early endosome · Cytoplasm, perinuclear region · Nucleus · Cytoplasm

Expression by cell type

Single cell type RNA, the 2 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Esophageal apical cells241.3 nCPM
  • Prostatic club cells178.9 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 — 10.0 nTPM, from ERBB2cerebellum — 4.4 nTPM, from ERBB2hippocampal formation — 7.4 nTPM, from ERBB2amygdala — 11.8 nTPM, from ERBB2hypothalamus — 6.3 nTPM, from ERBB2thalamus — no resolved target expressed herebasal ganglia — 14.9 nTPM, from ERBB2medulla 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: pituitary gland 17.0, midbrain 12.7, retina 7.5, spinal cord 6.0.

Body

heart — 53.9 nTPM, from ERBB2smooth muscle — 23.3 nTPM, from ERBB2lung — 34.1 nTPM, from ERBB2liver — 30.7 nTPM, from ERBB2kidney — 83.9 nTPM, from ERBB2stomach — 46.8 nTPM, from ERBB2duodenum — 59.8 nTPM, from ERBB2small intestine — 63.4 nTPM, from ERBB2colon — 63.8 nTPM, from ERBB2adrenal gland — 5.2 nTPM, from ERBB2thyroid gland — 53.6 nTPM, from ERBB2pancreas — 36.0 nTPM, from ERBB2urinary bladder — 37.4 nTPM, from ERBB2skeletal muscle — 19.5 nTPM, from ERBB2spleen — 6.7 nTPM, from ERBB2salivary gland — 65.8 nTPM, from ERBB2
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 ERBB2 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

  • pituitary gland17.0 nTPM
  • basal ganglia14.9 nTPM
  • midbrain12.7 nTPM
  • amygdala11.8 nTPM
  • cerebral cortex10.0 nTPM
  • retina7.5 nTPM
  • hippocampal formation7.4 nTPM
  • hypothalamus6.3 nTPM
  • spinal cord6.0 nTPM
  • cerebellum4.4 nTPM

Peripheral and autonomic · 16

  • kidney83.9 nTPM
  • salivary gland65.8 nTPM
  • colon63.8 nTPM
  • small intestine63.4 nTPM
  • duodenum59.8 nTPM
  • heart muscle53.9 nTPM
  • thyroid gland53.6 nTPM
  • stomach 146.8 nTPM
  • urinary bladder37.4 nTPM
  • pancreas36.0 nTPM
  • lung34.1 nTPM
  • liver30.7 nTPM
  • smooth muscle23.3 nTPM
  • skeletal muscle19.5 nTPM
  • spleen6.7 nTPM
  • adrenal gland5.2 nTPM

Transcript is not protein. These are RNA levels for ERBB2, 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.

Equilibrium binding constants 7

Ki and Kd — a concentration at equilibrium. Directly comparable across rows at the same target.

TargetClassTypeValue (nM)pXOrganismAssay
Receptor tyrosine-protein kinase erbB-2EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909205
Receptor tyrosine-protein kinase erbB-2EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909205
Receptor tyrosine-protein kinase erbB-2EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909205
Receptor tyrosine-protein kinase erbB-2EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909205
Receptor tyrosine-protein kinase erbB-2EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909205
Receptor tyrosine-protein kinase erbB-2EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909205
Receptor tyrosine-protein kinase erbB-2EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909205

Functional readouts 11

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

TargetClassTypeValue (nM)pXOrganismAssay
Receptor tyrosine-protein kinase erbB-2EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291788
Receptor tyrosine-protein kinase erbB-2EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291788
Receptor tyrosine-protein kinase erbB-2EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291788
Receptor tyrosine-protein kinase erbB-2EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909205
Receptor tyrosine-protein kinase erbB-2EnzymesAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291788
Receptor tyrosine-protein kinase erbB-2EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909205
Receptor tyrosine-protein kinase erbB-2EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909205
Receptor tyrosine-protein kinase erbB-2EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909205
Receptor tyrosine-protein kinase erbB-2EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909205
Receptor tyrosine-protein kinase erbB-2EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909205
Receptor tyrosine-protein kinase erbB-2EnzymesIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909205
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