针对结直肠癌中 EphA2 的激酶抑制剂。
Targeting EPHA2 with Kinase Inhibitors in Colorectal Cancer.
机构信息
Center for Biomolecular Magnetic Resonance, Institute for Organic Chemistry and Chemical Biology, Johann Wolfgang Goethe University, Max-von-Laue-Straße 7, 60438, Frankfurt am Main, Germany.
Laboratory of Cellular Oncology, Center for Cancer Research (CCR), National Cancer Institute (NCI), 37 Convent Drive, NIH Bethesda Campus Building 37, Room 4124, Bethesda, MD, 20892, USA.
出版信息
ChemMedChem. 2023 Dec 1;18(23):e202300420. doi: 10.1002/cmdc.202300420. Epub 2023 Oct 5.
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.
Ephrin 型-A2 受体酪氨酸激酶（EPHA2）参与多种癌症类型的发展和进展，包括结直肠癌（CRC）。也有证据表明，EPHA2 在开发针对结直肠癌临床使用的内皮生长因子受体（EGFR）单克隆抗体西妥昔单抗的耐药性方面发挥着关键作用。尽管 EPHA2 具有有前途的药理学潜力，但目前只有少数特异性抑制剂可用。在本概念论文中，描述了用低分子量（小分子）分子抑制 EPHA2 的一般策略。此外，还总结了使用小分子在 CRC 中抑制 EPHA2 的现有实例，突出了这种方法的潜力。
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