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The transforming growth factor β (TGF-β) superfamily is the largest family of secreted growth factors, comprising multiple subfamilies, including TGF-βs, bone morphogenetic proteins (BMPs), growth and differentiation factors (GDFs), activins, inhibins, and glial cell-derived neurotrophic factors (GDNFs). TGF-β signaling is initiated upon ligand binding to heteromeric complexes of type I and type II transmembrane serine/threonine kinase receptors. This binding triggers transphosphorylation of type I receptors by type II receptors, which then phosphorylate receptor-regulated Smads (R-Smads). These R-Smads associate with the co-Smad Smad4, translocate to the nucleus, and activate target gene transcription—a pathway known as canonical Smad signaling. In addition, the receptor complex can also activate non-Smad signaling pathways via interactions with receptor-interacting proteins. TGF-β superfamily members regulate diverse biological processes, including cell proliferation, differentiation, migration, adhesion, apoptosis, and extracellular matrix (ECM) production, and are closely implicated in the pathogenesis of various diseases.