Targeting EPHA2 with Kinase Inhibitors in Colorectal Cancer.
Targeting EPHA2 with Kinase Inhibitors in Colorectal Cancer.
复制标题
使用激酶抑制剂靶向治疗结直肠癌中的 EPHA2。
DOI：
10.1002/cmdc.202300420
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发表时间：
2023
期刊：
影响因子：
3.4
通讯作者：
Schwalbe,Harald
中科院分区：
文献类型：
--
作者：
Tröster,Alix;Jores,Nathalie;Mineev,KonstantinS;Sreeramulu,Sridhar;DiPrima,Michael;Tosato,Giovanna;Schwalbe,Harald
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.
