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PsychedeliaDokholyan Laboratory
TargetOther named receptors

Vascular endothelial growth factor receptor 2

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

Measurements
9
Compounds
8
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

VGFR2_HUMANKDRHomo sapiens

Vascular endothelial growth factor receptor 2

Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFA, VEGFC and VEGFD. Plays an essential role in the regulation of angiogenesis, vascular development, vascular permeability, and embryonic hematopoiesis. Promotes proliferation, survival, migration and differentiation of endothelial cells. Promotes reorganization of the actin cytoskeleton. Isoforms lacking a transmembrane domain, such as isoform 2 and isoform 3, may function as decoy receptors for VEGFA, VEGFC and/or VEGFD. Isoform 2 plays an important role as negative regulator of VEGFA- and VEGFC-mediated lymphangiogenesis by limiting the amount of free VEGFA and/or VEGFC and preventing their binding to FLT4. Modulates FLT1 and FLT4 signaling by forming heterodimers. Binding of vascular growth factors to isoform 1 leads to the activation of several signaling cascades. Activation of PLCG1 leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate and the activation of protein kinase C. Mediates activation of MAPK1/ERK2, MAPK3/ERK1 and the MAP kinase signaling pathway, as well as of the AKT1 signaling pathway. Mediates phosphorylation of PIK3R1, the regulatory subunit of phosphatidylinositol 3-kinase, reorganization of the actin cytoskeleton and activation of PTK2/FAK1. Required for VEGFA-mediated induction of NOS2 and NOS3, leading to the production of the signaling molecule nitric oxide (NO) by endothelial cells. Phosphorylates PLCG1. Promotes phosphorylation of FYN, NCK1, NOS3, PIK3R1, PTK2/FAK1 and SRC

Quoted from UniProt’s FUNCTION annotation for P35968 (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
VEGFB0.9990.1800.6500.998
CDH50.9990.6300.8000.998
NRP10.9990.8280.7000.997
VEGFC0.9990.9580.7000.999
PGF0.9990.0000.6500.998
VEGFD0.9990.3450.7000.998
PECAM10.9990.0450.8000.999
FGF20.9980.1680.6500.995
SRC0.9980.7960.9000.938
PDGFC0.9970.0000.6500.994

Where it sits in the cell

  • Vesicles
  • Nuclear membraneadditional
  • Cytosoladditional
  • Connecting pieceadditional
  • Mid pieceadditional
  • Principal pieceadditional

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

UniProt, curated Cell junction · Endoplasmic reticulum · Cell membrane · Cytoplasm · Nucleus · Cytoplasmic vesicle · Early endosome · Secreted

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.

  • Müller glia283.5 nCPM
  • Lymphatic endothelial cells240.8 nCPM
  • Vascular endothelial cells240.6 nCPM
  • Mesothelial cells191.9 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 — 1.4 nTPM, from KDRcerebellum — 0.4 nTPM, from KDRhippocampal formation — 1.8 nTPM, from KDRamygdala — 1.3 nTPM, from KDRhypothalamus — 1.5 nTPM, from KDRthalamus — no resolved target expressed herebasal ganglia — 2.3 nTPM, from KDRmedulla 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: retina 15.2, pituitary gland 6.0, midbrain 2.6, spinal cord 2.4.

Body

heart — 10.5 nTPM, from KDRsmooth muscle — 7.0 nTPM, from KDRlung — 13.2 nTPM, from KDRliver — 8.6 nTPM, from KDRkidney — 8.2 nTPM, from KDRstomach — 4.4 nTPM, from KDRduodenum — 2.1 nTPM, from KDRsmall intestine — 4.0 nTPM, from KDRcolon — 3.3 nTPM, from KDRadrenal gland — 6.5 nTPM, from KDRthyroid gland — 20.0 nTPM, from KDRpancreas — 2.8 nTPM, from KDRurinary bladder — 4.3 nTPM, from KDRskeletal muscle — 3.2 nTPM, from KDRspleen — 3.7 nTPM, from KDRsalivary gland — 3.6 nTPM, from KDR
020 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 KDR 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

  • retina15.2 nTPM
  • pituitary gland6.0 nTPM
  • midbrain2.6 nTPM
  • spinal cord2.4 nTPM
  • basal ganglia2.3 nTPM
  • hippocampal formation1.8 nTPM
  • hypothalamus1.5 nTPM
  • cerebral cortex1.4 nTPM
  • amygdala1.3 nTPM
  • cerebellum0.4 nTPM

Peripheral and autonomic · 16

  • thyroid gland20.0 nTPM
  • lung13.2 nTPM
  • heart muscle10.5 nTPM
  • liver8.6 nTPM
  • kidney8.2 nTPM
  • smooth muscle7.0 nTPM
  • adrenal gland6.5 nTPM
  • stomach 14.4 nTPM
  • urinary bladder4.3 nTPM
  • small intestine4.0 nTPM
  • spleen3.7 nTPM
  • salivary gland3.6 nTPM
  • colon3.3 nTPM
  • skeletal muscle3.2 nTPM
  • pancreas2.8 nTPM
  • duodenum2.1 nTPM

Transcript is not protein. These are RNA levels for KDR, 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 9

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

TargetClassTypeValue (nM)pXOrganismAssay
Vascular endothelial growth factor receptor 2Other named receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291829
Vascular endothelial growth factor receptor 2Other named receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291829
Vascular endothelial growth factor receptor 2Other named receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291829
Vascular endothelial growth factor receptor 2Other named receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291829
Vascular endothelial growth factor receptor 2Other named receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291829
Vascular endothelial growth factor receptor 2Other named receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291913
Vascular endothelial growth factor receptor 2Other named receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291913
Vascular endothelial growth factor receptor 2Other named receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291913
Vascular endothelial growth factor receptor 2Other named receptorsAC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL5291913
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