Target intelligence / Profile preview

Transforming growth factor beta receptor 2 (TGFBR2)

Target
TGFBR2
Molecular classification
Receptor, Serine/threonine protein kinase, Transmembrane protein
01

Overview

Transforming growth factor beta receptor 2 is a transmembrane serine/threonine kinase that forms a heterodimeric complex with transforming growth factor beta receptor type 1 to mediate signal transduction from extracellular transforming growth factor beta ligands (TGFB1/2/3) into the cell. Upon ligand binding, it phosphorylates and activates downstream effectors such as SMAD proteins to regulate transcription of genes involved in cell proliferation, differentiation, apoptosis, wound healing, immune response modulation, and extracellular matrix production. It acts as a tumor suppressor gene; loss-of-function or frameshift mutations are associated with several inherited syndromes affecting connective tissues and increased cancer risk due to impaired control over cellular proliferation. Frameshift mutant neoantigens derived from this gene can be recognized by the immune system and are being explored for personalized cancer immunotherapies.

Other names
TGF-beta receptor type IITGF-beta receptor 2TGFR2Transforming growth factor, beta receptor II (70/80kDa)
02

Mechanism of action

Drugs targeting this molecule may act as inhibitors or agonists of the serine/threonine kinase activity or modulate downstream SMAD signaling pathways.

03

Biological functions

Signal transductionCell proliferation regulationCell cycle arrestApoptosis (cell death)Differentiation (cell maturation)Wound healingImmunosuppression
04

Disease associations

Cancer (tumor suppressor gene, various tumors)Connective tissue disorders (e.g., Marfan syndrome, Loeys-Dietz syndrome, Osler–Weber–Rendu syndrome)Cardiovascular disease
05

Safety considerations

Potential safety concerns include effects on normal cell proliferation, wound healing, immune suppression, and risk of promoting tumorigenesis if signaling is dysregulated.Targeting mutant forms may reduce off-target effects but could still impact normal tissue homeostasis.
06

Interacting drugs

Fostamatinib
07

Biomarkers

Mutations in TGFBR2 serve as biomarkers for certain cancers and connective tissue diseases such as Loeys-Dietz syndrome and Marfan syndrome.Frameshift mutations can generate neoantigens relevant for immunotherapy patient selection.

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