To date, the RTKs superfamily has 58 members that fall into 20 subfamilies. Receptor tyrosine kinases (RTKs) are key regulators of normal cellular processes, and they are also involved in the development and progression of many types of cancer ( 1). In this review, we analyzed the structural and functional features of ROR1 and discussed therapeutic strategies targeting this kinase. The function of ROR1 as a tyrosine kinase remains poorly understood, although accumulating evidence have demonstrated its intrinsic tyrosine kinase activity. However, small molecule inhibitors targeting ROR1 are underappreciated because of the initial characterization of ROR1 as a peusdokinase. Antibody-based immunotherapies targeting ROR1 have been developed and evaluated in preclinical and clinical studies with promising outcomes. Studies have demonstrated that it plays an important role in oncogenesis by activating cell survival signaling events, particularly the non-canonical WNT signaling pathway. Receptor tyrosine kinase ROR1 plays an essential role in embryogenesis and is overexpressed in many types of malignant tumors.
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