English (United Kingdom)

https://curated-unify.zendy.io/wp-json/zendy-region/v1/featured_content/oa?rat=en

https://curated-unify.zendy.io/wp-json/zendy-region/v1/highlighted_journal/

Zendy Plus

Presents the access of premium content as premium feature

Premium Content

Presents the keyphrase highlighting as premium feature

Keyphrase Highlighting

Presents the summarisation as premium feature

Summarisation

Insights

Presents the pdf analysis as premium feature

PDF Analysis

Presents the zaia usage as premium feature

ZAIA

Zendy Tools

Zendy Open

Most non‐small‐cell lung cancers ( NSCLC s) harboring activating mutations in the epidermal growth factor receptor ( EGFR ) are initially responsive to  EGFR  tyrosine kinase inhibitors ( EGFR ‐ TKI s); however, they invariably develop resistance to these drugs.  E 7820 is an angiogenesis inhibitor that decreases integrin‐α2 expression and is currently undergoing clinical trials. We investigated whether  E 7820 in combination with erlotinib, an  EGFR ‐ TKI , could overcome  EGFR ‐ TKI ‐resistance in the  NSCLC  cell lines  A 549 ( KRAS ; G12S), H1975 ( EGFR ;  L 858R/ T 790M), and  H 1650 ( PTEN ; loss,  EGFR ; exon 19 deletion), which are resistant to erlotinib. Immunohistochemical analysis was carried out in xenografted tumors to investigate anti‐angiogenesis activity and endothelial cell apoptosis levels by endothelial cell marker  CD 31 and  TUNEL  staining, respectively. Treatment with  E 7820 (50 mg/kg) with erlotinib (60 mg/kg) showed a synergistic antitumor effect in three xenograft models. Immunohistochemical analysis indicated that combined treatment with E7820 and erlotinib significantly decreased microvessel density and increased apoptosis of tumor‐associated endothelial cells compared with use of only one of the agents. This combination increased apoptosis in  HUVEC s through activation of both intrinsic and extrinsic apoptosis pathways  in vitro . The combination of  E 7820 with erlotinib is an alternative strategy to overcome erlotinib resistance in  NSCLC  by enhancement of the anti‐angiogenic activity of  E 7820.

cancer science

Enhanced anti‐angiogenic effect of  E 7820 in combination with erlotinib in epidermal growth factor receptor–tyrosine kinase inhibitor‐resistant non‐small‐cell lung cancer xenograft models