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TargetOther named receptors

TGF-beta receptor type-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
1
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

TGFR2_HUMANTGFBR2Homo sapiens

TGF-beta receptor type-2

Transmembrane serine/threonine kinase forming with the TGF-beta type I serine/threonine kinase receptor, TGFBR1, the non-promiscuous receptor for the TGF-beta cytokines TGFB1, TGFB2 and TGFB3. Transduces the TGFB1, TGFB2 and TGFB3 signal from the cell surface to the cytoplasm and thus regulates a plethora of physiological and pathological processes including cell cycle arrest in epithelial and hematopoietic cells, control of mesenchymal cell proliferation and differentiation, wound healing, extracellular matrix production, immunosuppression and carcinogenesis. The formation of the receptor complex composed of 2 TGFBR1 and 2 TGFBR2 molecules symmetrically bound to the cytokine dimer results in the phosphorylation and activation of TGFBR1 by the constitutively active TGFBR2. Activated TGFBR1 phosphorylates SMAD2 which dissociates from the receptor and interacts with SMAD4. The SMAD2-SMAD4 complex is subsequently translocated to the nucleus where it modulates the transcription of the TGF-beta-regulated genes. This constitutes the canonical SMAD-dependent TGF-beta signaling cascade. Also involved in non-canonical, SMAD-independent TGF-beta signaling pathways
Has transforming growth factor beta-activated receptor activity
Has transforming growth factor beta-activated receptor activity
Binds TGFB1, TGFB2 and TGFB3 in the picomolar affinity range without the participation of additional receptors. Blocks activation of SMAD2 and SMAD3 by TGFB1

Quoted from UniProt’s FUNCTION annotation for P37173 (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
TGFB10.9990.9860.9000.999
TGFB30.9990.9840.9000.997
TGFB20.9990.9320.0000.997
TGFBR10.9990.9860.9000.986
SMAD30.9980.0910.9000.985
SMAD20.9980.0910.9000.979
ENG0.9970.6300.0000.992
SMAD40.9960.0910.9000.960
SMAD70.9940.6440.9000.855
ACVRL10.9920.5280.8000.916

Where it sits in the cell

  • Plasma membrane

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

UniProt, curated Cell membrane · Membrane raft · Secreted

Expression by cell type

Single cell type RNA, the 7 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Lymphatic endothelial cells890.2 nCPM
  • Vascular endothelial cells805.9 nCPM
  • Neutrophils767.3 nCPM
  • Choroid plexus epithelial cells582 nCPM
  • Microglia559.4 nCPM
  • pDCs462.8 nCPM
  • Alveolar cells type 1446.4 nCPM

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Other measurements 1

Everything else ChEMBL recorded for this compound — percentage inhibition, efficacy, half-life, cytotoxicity. Reported in the assay's own units, which is why no value is converted here.

TargetClassTypeValue (nM)pXOrganismAssay
TGF-beta receptor type-2Other named receptorsActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL4151475