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PsychedeliaDokholyan Laboratory
TargetOther named receptors

Vascular endothelial growth factor receptor 1

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

Measurements
14
Compounds
7
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

VGFR1_HUMANFLT1Homo sapiens

Vascular endothelial growth factor receptor 1

Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFA, VEGFB and PGF, and plays an essential role in the development of embryonic vasculature, the regulation of angiogenesis, cell survival, cell migration, macrophage function, chemotaxis, and cancer cell invasion. Acts as a positive regulator of postnatal retinal hyaloid vessel regression (By similarity). May play an essential role as a negative regulator of embryonic angiogenesis by inhibiting excessive proliferation of endothelial cells. Can promote endothelial cell proliferation, survival and angiogenesis in adulthood. Its function in promoting cell proliferation seems to be cell-type specific. Promotes PGF-mediated proliferation of endothelial cells, proliferation of some types of cancer cells, but does not promote proliferation of normal fibroblasts (in vitro). Has very high affinity for VEGFA and relatively low protein kinase activity; may function as a negative regulator of VEGFA signaling by limiting the amount of free VEGFA and preventing its binding to KDR. Modulates KDR signaling by forming heterodimers with KDR. Ligand binding leads to the activation of several signaling cascades. Activation of PLCG leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate and the activation of protein kinase C. Mediates phosphorylation of PIK3R1, the regulatory subunit of phosphatidylinositol 3-kinase, leading to activation of phosphatidylinositol kinase and the downstream signaling pathway. Mediates activation of MAPK1/ERK2, MAPK3/ERK1 and the MAP kinase signaling pathway, as well as of the AKT1 signaling pathway. Phosphorylates SRC and YES1, and may also phosphorylate CBL. Promotes phosphorylation of AKT1 at 'Ser-473'. Promotes phosphorylation of PTK2/FAK116685275
Phosphorylates PLCG
May function as decoy receptor for VEGFA
May function as decoy receptor for VEGFA
May function as decoy receptor for VEGFA
Has a truncated kinase domain; it increases phosphorylation of SRC at 'Tyr-418' by unknown means and promotes tumor cell invasion

Quoted from UniProt’s FUNCTION annotation for P17948 (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
VEGFC0.9990.0480.6500.998
VEGFB0.9990.9550.7000.999
PGF0.9990.9770.7000.999
VEGFD0.9990.0700.6500.998
KDR0.9940.5100.0000.984
NRP10.9930.3450.0000.989
FGF20.9930.1680.6500.978
PDGFC0.9890.0000.6500.972
ANGPT10.9840.1150.6500.952
ANGPT20.9830.1150.6500.936

Where it sits in the cell

  • Plasma membrane
  • Actin filamentsadditional
  • 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 · Endosome · Secreted · Cytoplasm

Expression by cell type

Single cell type RNA, the 8 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Syncytiotrophoblasts1,703.8 nCPM
  • Extravillous trophoblasts1,644.7 nCPM
  • Vascular endothelial cells1,218.5 nCPM
  • Müller glia545.6 nCPM
  • Migrating cytotrophoblasts449.7 nCPM
  • Cytotrophoblasts308.8 nCPM
  • Neutrophils284.2 nCPM
  • Late spermatids279.5 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.

  • placenta394.3 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 — 15.7 nTPM, from FLT1cerebellum — 10.1 nTPM, from FLT1hippocampal formation — 21.9 nTPM, from FLT1amygdala — 16.2 nTPM, from FLT1hypothalamus — 18.2 nTPM, from FLT1thalamus — no resolved target expressed herebasal ganglia — 23.7 nTPM, from FLT1medulla 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 46.2, midbrain 25.8, spinal cord 21.3, pituitary gland 8.8.

Body

heart — 44.1 nTPM, from FLT1smooth muscle — 15.7 nTPM, from FLT1lung — 23.6 nTPM, from FLT1liver — 16.4 nTPM, from FLT1kidney — 32.9 nTPM, from FLT1stomach — 9.8 nTPM, from FLT1duodenum — 6.6 nTPM, from FLT1small intestine — 8.8 nTPM, from FLT1colon — 9.2 nTPM, from FLT1adrenal gland — 10.0 nTPM, from FLT1thyroid gland — 45.0 nTPM, from FLT1pancreas — 10.4 nTPM, from FLT1urinary bladder — 12.6 nTPM, from FLT1skeletal muscle — 17.9 nTPM, from FLT1spleen — 16.8 nTPM, from FLT1salivary gland — 6.7 nTPM, from FLT1
046 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 FLT1 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

  • retina46.2 nTPM
  • midbrain25.8 nTPM
  • basal ganglia23.7 nTPM
  • hippocampal formation21.9 nTPM
  • spinal cord21.3 nTPM
  • hypothalamus18.2 nTPM
  • amygdala16.2 nTPM
  • cerebral cortex15.7 nTPM
  • cerebellum10.1 nTPM
  • pituitary gland8.8 nTPM

Peripheral and autonomic · 16

  • thyroid gland45.0 nTPM
  • heart muscle44.1 nTPM
  • kidney32.9 nTPM
  • lung23.6 nTPM
  • skeletal muscle17.9 nTPM
  • spleen16.8 nTPM
  • liver16.4 nTPM
  • smooth muscle15.7 nTPM
  • urinary bladder12.6 nTPM
  • pancreas10.4 nTPM
  • adrenal gland10.0 nTPM
  • stomach 19.8 nTPM
  • colon9.2 nTPM
  • small intestine8.8 nTPM
  • salivary gland6.7 nTPM
  • duodenum6.6 nTPM

Transcript is not protein. These are RNA levels for FLT1, 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
Vascular endothelial growth factor receptor 1Other named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909118
Vascular endothelial growth factor receptor 1Other named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909118
Vascular endothelial growth factor receptor 1Other named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909118
Vascular endothelial growth factor receptor 1Other named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909118
Vascular endothelial growth factor receptor 1Other named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909118
Vascular endothelial growth factor receptor 1Other named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909118
Vascular endothelial growth factor receptor 1Other named receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909118

Functional readouts 7

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

TargetClassTypeValue (nM)pXOrganismAssay
Vascular endothelial growth factor receptor 1Other named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909118
Vascular endothelial growth factor receptor 1Other named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909118
Vascular endothelial growth factor receptor 1Other named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909118
Vascular endothelial growth factor receptor 1Other named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909118
Vascular endothelial growth factor receptor 1Other named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909118
Vascular endothelial growth factor receptor 1Other named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909118
Vascular endothelial growth factor receptor 1Other named receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909118
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