Targeting FGFRs for tumor therapy: current status and novel strategies Supplementary dataset

The FGF receptors (FGFRs) belong to a family of receptor tyrosine kinases. Abundant evidence shows
that FGFRs are closely related to tumor cell invasion and angiogenesis. Hence, targeted modulation
of FGFRs has become an effective strategy for cancer treatment. Recently, the development of smallmolecule
inhibitors targeting FGFRs has been extensively studied, and three inhibitors have been approved
for marketing. Based on the clinical problems with the current inhibitors, there is a need to develop
novel inhibitors and technologies to address the pitfalls. This review summarizes recent advances in
small-molecule inhibitors targeting FGFRs, focusing on structure–activity relationships. Moreover, recent
progress of novel technologies are summarized to provide a reference for promoting the application of
drugs targeting FGFRs in tumor therapy.