A new challenging and promising era of tyrosine kinase inhibitors.

Protein kinases are key regulators that govern complex cellular processes. Dysregulation of kinase signaling is associated in many human diseases, particularly cancers and developmental and metabolic disorders. Tyrosine kinase inhibitors have achieved great success in molecular targeted therapies for cancer and now is expanding to other therapeutic areas. The onset of drug resistance to prolonged TKI treatment brings new challenges in TKI drug development. The deep understanding of disease pathologies related to TKs and drug resistance mechanisms will generate new waves for seeking highly selective, potent, and safe TKIs.