Synthesis and Biological Assessment of Chalcone and Pyrazoline Derivatives as novel inhibitor for ELF3-MED23 Interaction (Updated July 8, 2024).

A preprint abstract from biorxiv.org discusses a potential alternative therapeutic approach to trastuzumab, a monoclonal antibody drug used to target HER2 overexpression in various solid tumors. The study focuses on targeting the protein-protein interaction between ELF3 and MED23 as a potential intervention for HER2-overexpressing cancers. The researchers synthesized 26 compounds and found that compound 10 effectively disrupted the ELF3-MED23 interaction, leading to a reduction in HER2 levels and downstream signals in gastric cancer cells. Compound 10 also demonstrated anticancer activity in trastuzumab-refractory cases, suggesting its potential as a therapeutic option for trastuzumab-resistant gastric cancers. However, it is important to note that this preprint has not been peer-reviewed. [Extracted from the article]