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studies of a peptidomimetic that targets EGFR dimerization in NSCLC. | LitMetric

Studies related to lung cancer have shown a link between human epidermal growth factor receptor-2 (HER2) expression and poor prognosis in patients with non-small cell lung cancer (NSCLC). HER2 overexpression has been observed in 3-38% of NSCLC, while strong HER2 protein overexpression is found in 2.5% of NSCLC. However, HER2 dimerization is important in lung cancer, including EGFR mutated NSCLC. Since HER2 dimerization leads to cell proliferation, targeting the dimerization of HER2 will have a significant impact on cancer therapies. A peptidomimetic has been designed that can be used as a therapeutic agent for a subset of NSCLC patients overexpressing HER2 or possessing HER2 as well as EGFR mutation. A cyclic peptidomimetic () has been designed to inhibit protein-protein interactions of HER2 with its dimerization partners EGFR and HER3. Compound exhibited antiproliferative activity in HER2-positive NSCLC cell lines at nanomolar concentrations. Western blot analysis showed that inhibited phosphorylation of HER2 and Akt and . Stability studies of at various temperature and pH (pH 1 and pH 7.6), and in the presence of liver microsomes indicated that was stable against thermal and chemical degradation. Pharmacokinetic parameters were evaluated in nude mice by administrating single doses of 4 mg/kg and 6 mg/kg of via IV. The anticancer activity of was evaluated using an experimental metastasis lung cancer model in mice. Compound suppressed the tumor growth in mice when compared to control. A proximity ligation assay further proved that inhibits HER2:HER3 and EGFR: HER2 dimerization. Overall, these results suggest that can be a potential treatment for HER2-dimerization related NSCLC.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7477407PMC
http://dx.doi.org/10.7150/jca.46320DOI Listing

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