Growth factor receptor (GFR) (GFR)

Growth factor receptors are a diverse group of transmembrane proteins that play a critical role in regulating fundamental cellular processes such as growth, proliferation, differentiation, and survival (Lemmon & Schlessinger, 2010). Most physiological growth factor receptors belong to the receptor tyrosine kinase (RTK) family, which includes well-known members like the epidermal growth factor receptor (EGFR), vascular endothelial growth factor receptor (VEGFR), and fibroblast growth factor receptor (FGFR) (Du & Lovly, 2018). Upon binding to their specific ligands, these receptors undergo dimerization and autophosphorylation, triggering complex intracellular signaling cascades like the MAPK/ERK and PI3K/Akt pathways (Yarden & Pines, 2012). Dysregulation of these receptors, often through overexpression or activating mutations, is a hallmark of many cancers and other proliferative diseases (Casaletto & McClatchey, 2012). Consequently, they are major therapeutic targets for a wide range of drugs, including monoclonal antibodies and small-molecule kinase inhibitors, which aim to block aberrant signaling and inhibit disease progression (Gschwind et al., 2004).

Other names

Receptor tyrosine kinaseRTKGrowth factor receptor familyPhysiological growth factor receptors

Drugs targeting growth factor receptors typically act by either binding to the extracellular domain to prevent ligand interaction and receptor dimerization or by competitively inhibiting the ATP-binding site within the intracellular tyrosine kinase domain to block downstream signaling cascades (Lemmon & Schlessinger, 2010; Gschwind et al., 2004).