Receptor tyrosine kinases (RTKs) are a family of cell surface receptors that play crucial roles in various cellular processes, including cell growth and proliferation, differentiation, migration
or metabolism. They function by binding extracellular ligands, which triggers receptor dimerization and activation of their intracellular tyrosine kinase domains. This initiates downstream
signaling cascades that regulate key cellular functions (Figure 1). RTKs are highly relevant targets within drug discovery because they are frequently dysregulated in cancer and other diseases. Many successful targeted therapies inhibit RTKs (e.g. imatinib, erlotinib), showing that the receptors provide opportunities for developing selective inhibitors.