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
Hauptverfasser: Wilson, Kalin, Shiuan, Eileen, Brantley-Sieders, Dana M.
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container_end_page 2495
container_issue 14
container_start_page 2483
container_title Oncogene
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creator Wilson, Kalin
Shiuan, Eileen
Brantley-Sieders, Dana M.
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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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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