Targeting EPHA2 with Kinase Inhibitors in Colorectal Cancer

Abstract: 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.

Location
Deutsche Nationalbibliothek Frankfurt am Main
Extent
Online-Ressource
Language
Englisch

Bibliographic citation
Targeting EPHA2 with Kinase Inhibitors in Colorectal Cancer ; day:05 ; month:10 ; year:2023 ; extent:7
ChemMedChem ; (05.10.2023) (gesamt 7)

Creator
Tröster, Alix
Jores, Nathalie
Mineev, Konstantin S.
Sreeramulu, Sridhar
DiPrima, Michael
Tosato, Giovanna
Schwalbe, Harald

DOI
10.1002/cmdc.202300420
URN
urn:nbn:de:101:1-2023100515381510436918
Rights
Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.
Last update
14.08.2025, 11:01 AM CEST

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