May EPH/Ephrin Targeting Revolutionize Lung Cancer Treatment?

• Published in: International journal of molecular sciences Vol. 24; no. 1; p. 93
• Main Authors: Psilopatis, Iason, Karniadakis, Ioannis, Danos, Konstantinos Stylianos, Vrettou, Kleio, Michaelidou, Kleita, Mavridis, Konstantinos, Agelaki, Sofia, Theocharis, Stamatios
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI 21.12.2022; MDPI AG
• Subjects: Animals; Carcinoma, Non-Small-Cell Lung; EPH; ephrin; ephrin receptor; Ephrin-A1 - metabolism; Ephrin-A2; Ephrins - metabolism; Humans; lung cancer; Lung Neoplasms - drug therapy; precision medicine; Review; treatment; lung cancer; treatment; precision medicine; ephrin receptor; EPH; ephrin
• ISSN: 1422-0067; 1661-6596; 1422-0067
• DOI: 10.3390/ijms24010093

Lung cancer (LC) is the leading cause of cancer death in the United States. Erythropoietin-producing hepatocellular receptors (EPHs) comprise the largest receptor tyrosine kinases (RTKs) family in mammals. EPHs along with their ligands, EPH-family receptor-interacting proteins (ephrins), have been found to be either up- or downregulated in LC cells, hence exhibiting a defining role in LC carcinogenesis and tumor progression. In their capacity as membrane-bound molecules, EPHs/ephrins may represent feasible targets in the context of precision cancer treatment. In order to investigate available therapeutics targeting the EPH/ephrin system in LC, a literature review was conducted, using the MEDLINE, LIVIVO, and Google Scholar databases. EPHA2 is the most well-studied EPH/ephrin target in LC treatment. The targeting of EPHA2, EPHA3, EPHA5, EPHA7, EPHB4, EPHB6, ephrin-A1, ephrin-A2, ephrin-B2, and ephrin-B3 in LC cells or xenograft models not only directly correlates with a profound LC suppression but also enriches the effects of well-established therapeutic regimens. However, the sole clinical trial incorporating a NSCLC patient could not describe objective anti-cancer effects after anti-EPHA2 antibody administration. Collectively, EPHs/ephrins seem to represent promising treatment targets in LC. However, large clinical trials still need to be performed, with a view to examining the effects of EPH/ephrin targeting in the clinical setting.