Targeting EPHA2 with Kinase Inhibitors in Colorectal Cancer

The ephrin type-A 2 receptor tyrosine kinase (EPHA2) is involved in the development and progression of various cancer types, including colorectal cancer (CRC). There is also evidence that EPHA2 plays a key role in the development of resistance to the endothelial growth factor receptor (EGFR) monoclonal antibody Cetuximab used clinically in CRC. Despite the promising pharmacological potential of EPHA2, only a handful of specific inhibitors are currently available. In this concept paper, general strategies for EPHA2 inhibition with molecules of low molecular weight (small molecules) are described. Furthermore, available examples of inhibiting EPHA2 in CRC using small molecules are summarized, highlighting the potential of this approach. Targeting the kinase EPHA2 in colorectal cancer (CRC): The kinase EPHA2 plays a role in the development and progression of CRC and seems to be involved in resistance mechanism towards a monoclonal antibody. This concept paper reviews the present results of targeting EPHA2 in CRC with small molecules and highlights the potential of this approach.+image

Automated summary

This concept paper describes the general strategies for EPHA2 inhibition with small molecules and summarizes the potential of targeting EPHA2 in CRC. EPHA2 plays a crucial role in the development and resistance mechanisms of CRC.