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Transforming growth factor beta receptor type I; Transforming growth factor beta receptor type II (TGFBR1 (type I), TGFBR2 (type II))
- Target
- TGFBR1 (type I), TGFBR2 (type II)
- Molecular classification
- Receptor, Serine/threonine kinase, Transmembrane signaling receptor, TGFβ receptor family
01
Overview
Transforming growth factor beta receptor type I (TGFBR1) and transforming growth factor beta receptor type II (TGFBR2) are transmembrane serine/threonine kinase receptors fundamental to TGF-β signaling, a pathway that regulates cell proliferation, differentiation, apoptosis, and tissue homeostasis. Upon TGF-β ligand binding, the constitutively active TGFBR2 phosphorylates and activates TGFBR1, which then propagates signaling via phosphorylation of SMAD transcription factors and diverse downstream effectors. Dysregulation of these receptors is implicated in cancer, fibrosis, cardiovascular and autoimmune diseases. Both receptors are regarded as major therapeutic targets, with several inhibitors and antibodies in clinical development for oncology and fibroproliferative disorders.
- Other names
- ALK5Activin A receptor type II-like kinase (for TGFBR1)MFS2 (for TGFBR2)
02
Mechanism of action
Inhibition of receptor kinase activity to block downstream SMAD signaling; Antagonism of ligand-receptor binding; Modulation of receptor dimerization and phosphorylation cascades leading to transcription factor activation
03
Biological functions
Signal transductionRegulation of cell proliferationCell differentiationApoptosis (cell death)Immune responseTissue homeostasisChemotaxisEpithelial-mesenchymal transition (EMT)Wound healing
04
Disease associations
Cancer (as tumor suppressors or promoters depending on context)Fibrosis (renal, pulmonary, hepatic, cardiac)InflammationCardiovascular disease (e.g., Loeys-Dietz syndrome)Autoimmune disordersDiabetesDevelopmental disorders
05
Safety considerations
Increased risk of immunosuppressionImpairment of wound healingRisk of promoting tumor progression in certain contexts (e.g., advanced cancer)Potential for off-target effects in cardiac and connective tissue
06
Interacting drugs
Galunisertib (LY2157299, TGFBR1 inhibitor)
5 more in the full profile.
07
Biomarkers
Phosphorylation status of SMAD2/3Expression levels of TGFBR1 or TGFBR2TGF-β ligand levels in serum or tissuesDownstream target gene expression (e.g., CDK inhibitors p15, p21)
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