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TGFBR1 is a transmembrane serine/threonine kinase receptor that plays a central role in the transforming growth factor-beta (TGF-β) signaling pathway. Upon ligand binding and activation by TGFBR2, TGFBR1 phosphorylates SMAD proteins, propagating signals into the cell to regulate cellular processes like proliferation, differentiation, and apoptosis. It has dual roles as tumor suppressor/promoter, and is implicated in various diseases, including Loeys-Dietz syndrome and cancer. Several small-molecule inhibitors target TGFBR1 kinase activity.
Small-molecule inhibitors that target TGFBR1's kinase activity, preventing phosphorylation and activation of downstream signaling molecules such as SMADs.
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