Targeting ERBB Receptors in Cancer

摘要: Tyrosine kinases are a large and diverse family of proteins found only in metazoans. The ERBB family, which encompasses subgroup I the receptor tyrosine kinase (RTK) superfamily, has four members: epidermal growth factor (EGFR)/ErbB1, ErbB2, ErbB3, ErbB4. RTKs contain an extracellular domain that binds peptide ligands; they span membrane once have intracellular portion with protein activity (Fig. 4.1). Ligand binding induces formation dimers, as consequence intrinsic is activated transfers phosphate group from bound ATP to specific side chains on signaling bind active RTKs. Subsequently, multiple pathways become activated. receptor/ligand been investigated depth for many years, comprehensive maps describing links between plasma receptors, cytoplasmic pathways, nucleus available (Oda 2005).