Affiliation:
1. 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
2. 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
Abstract
AbstractThe 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.
Funder
Horizon 2020 Framework Programme
Subject
Organic Chemistry,General Pharmacology, Toxicology and Pharmaceutics,Molecular Medicine,Drug Discovery,Biochemistry,Pharmacology
Cited by
1 articles.
订阅此论文施引文献
订阅此论文施引文献,注册后可以免费订阅5篇论文的施引文献,订阅后可以查看论文全部施引文献