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Target intelligence / Profile preview
Transforming growth factor-beta receptor type 1 (TGFBR1)
- Target
- TGFBR1
- Molecular classification
- Receptor, Serine/threonine kinase receptor, Transmembrane protein
01
Overview
The **transforming growth factor-beta receptor type 1** (TGFBR1) is a transmembrane serine/threonine kinase receptor that binds TGF-β ligands on the cell surface, forming a complex with type 2 receptor (TGFBR2). Ligand engagement induces phosphorylation of TGFBR1 by TGFBR2, activating intracellular signaling cascades—chiefly through SMAD transcription factors—that regulate cell proliferation, differentiation, and apoptosis. This receptor is essential for embryonic development, immune regulation, tissue homeostasis, and tumor suppression. Aberrations in TGF-β signaling, such as mutations or altered expression, are implicated in a wide spectrum of human diseases, notably cancer, fibrosis, and inflammatory conditions.
- Other names
- TGF-β receptor type 1TGFBR1ALK5
02
Mechanism of action
Small molecule inhibition of receptor kinase activity (preventing phosphorylation and subsequent signal transduction) Blocking ligand-receptor interaction
03
Biological functions
Signal transductionCell proliferationCell differentiationApoptosis (cell death)Immune responseTissue homeostasisEmbryonic development
04
Disease associations
Cancer (particularly tumor suppression and progression)InflammationFibrosisCardiovascular diseaseAutoimmune diseases
05
Safety considerations
Compromised immune surveillance leading to higher infection or cancer risk (due to immunosuppressive effects of pan-inhibition)Impaired wound healingPotential for cardiovascular toxicity
06
Interacting drugs
Galunisertib (LY2157299)
2 more in the full profile.
07
Biomarkers
TGF-β1 ligand levels in serum or tumor microenvironmentPhosphorylated SMAD2/3 as markers of pathway activation
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