TGF-β Receptors
The transforming growth factor-β family of polypeptides (TGF-β1, TGF-β2 and TGF-β3) are involved in the regulation of cellular processes, including cell division, differentiation, motility, adhesion and death. TGF-β signals by binding the TGF-β type II receptor (TGF-βRII) which transphosphorylates and activates the type I receptor (TGF-βRI). Activated TGF-βRI then phosphorylates a subset of SMAD proteins, Smad2 and Smad3, which translocate to the nucleus where they form transcription complexes with DNA binding factors and co-activators/co-repressors.
More Information and Gene Data »TGF-β Receptors - More Information
TGF-β functions as a tumor suppressor by inhibiting the cell cycle in the G1 phase. Administration of TGF-β is able to protect against mammary tumor development in transgenic mouse models in vivo. Disruption of the TGF-β/SMAD pathway has been implicated in a variety of human cancers, with the majority of colon and gastric cancers being caused by an inactivating mutation of TGF-βRII. Homozygous deletions of TGF-βRI and inactivating mutations of SMAD genes have also been found.
A pro-oncogenic role for TGF-β has also been proposed. Once cells lose their sensitivity to TGF-β1-mediated growth inhibition, autocrine TGF-β signaling can promote tumorigenesis. Elevated levels of TGF-β1 are often observed in advanced carcinomas, and have been correlated with increased tumor invasiveness and disease progression.
TGF-β Receptor Gene Data
| Gene | Species | Gene Symbol | Gene Accession No. | Protein Accession No. |
|---|
| TGF-βRI | Human | TGFBR1 | NM_004612 | P36897 |
| Mouse | Tgfbr1 | BC063260 | Q64729 | |
| Rat | Tgfbr1 | NM_012775 | P80204 | |
| TGF-βRII | Human | TGFBR2 | NM_003242 | P37173 |
| Mouse | Tgfbr2 | NM_009371 | Q62312 | |
| Rat | Tgfbr2 | NM_031132 | P38438 | |
| More TGF-β Receptor genes » | ||||
TGF-β Receptor Products
Inhibitors |
|
Cat.No. |
Product Name / Activity |
| 2939 | A 83-01 |
| Selective inhibitor of TGF-βRI, ALK4 and ALK7 | |
| 2902 | D 4476 |
| TGF-βRI inhibitor. Also inhibits CK1 | |
| 2718 | LY 364947 |
| Selective inhibitor of TGF-βRI | |
| 1614 | SB 431542 |
| Potent, selective inhibitor of TGF-βRI, ALK4 and ALK7 | |
| 3211 | SB 525334 |
| Selective inhibitor of TGF-βRI | |
| 3269 | SD 208 |
| Potent ATP-competitive TGF-βRI inhibitor | |
| 3742 |
SJN 2511 |
| Selective inhibitor of TGF-βRI | |
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