Oncogenic functions and therapeutic targeting of EphA2 in cancer
More than 25 years of research and preclinical validation have defined EphA2 receptor tyrosine kinase as a promising molecular target for clinical translation in cancer treatment. Molecular, genetic, biochemical, and pharmacological targeting strategies have been extensively tested in vitro and in v...
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Veröffentlicht in: | Oncogene 2021-04, Vol.40 (14), p.2483-2495 |
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description | More than 25 years of research and preclinical validation have defined EphA2 receptor tyrosine kinase as a promising molecular target for clinical translation in cancer treatment. Molecular, genetic, biochemical, and pharmacological targeting strategies have been extensively tested in vitro and in vivo, and drugs like dasatinib, initially designed to target SRC family kinases, have been found to also target EphA2 activity. Other small molecules, therapeutic targeting antibodies, and peptide-drug conjugates are being tested, and more recently, approaches harnessing antitumor immunity against EphA2-expressing cancer cells have emerged as a promising strategy. This review will summarize preclinical studies supporting the oncogenic role of EphA2 in breast cancer, lung cancer, glioblastoma, and melanoma, while delineating the differing roles of canonical and noncanonical EphA2 signaling in each setting. This review also summarizes completed and ongoing clinical trials, highlighting the promise and challenges of targeting EphA2 in cancer. |
doi_str_mv | 10.1038/s41388-021-01714-8 |
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Academic</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>Oncogene</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Wilson, Kalin</au><au>Shiuan, Eileen</au><au>Brantley-Sieders, Dana M.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Oncogenic functions and therapeutic targeting of EphA2 in cancer</atitle><jtitle>Oncogene</jtitle><stitle>Oncogene</stitle><addtitle>Oncogene</addtitle><date>2021-04-08</date><risdate>2021</risdate><volume>40</volume><issue>14</issue><spage>2483</spage><epage>2495</epage><pages>2483-2495</pages><issn>0950-9232</issn><eissn>1476-5594</eissn><abstract>More than 25 years of research and preclinical validation have defined EphA2 receptor tyrosine kinase as a promising molecular target for clinical translation in cancer treatment. 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subjects | 631/67/1059/602 692/53 Apoptosis Brain cancer Breast cancer Cancer Care and treatment Cell Biology Cell receptors Cellular signal transduction Clinical trials Drug development EphA2 protein Genetic aspects Glioblastoma Health aspects Human Genetics Humans Internal Medicine Kinases Lung cancer Medicine Medicine & Public Health Melanoma Molecular targeted therapy Neoplasms - genetics Oncogenes Oncogenes - genetics Oncology Oncology, Experimental Protein tyrosine kinase Protein-tyrosine kinase receptors Receptor, EphA2 - metabolism Review Article Therapeutic targets |
title | Oncogenic functions and therapeutic targeting of EphA2 in cancer |
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