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IC-4, a new irreversible EGFR inhibitor, exhibits prominent anti-tumor and anti-angiogenesis activities.
Li, Ying-Bo; Wang, Zhong-Qing; Yan, Xu; Chen, Mei-Wan; Bao, Jiao-Lin; Wu, Guo-Sheng; Ge, Ze-Mei; Zhou, De-Min; Wang, Yi-Tao; Li, Run-Tao.
Afiliação
  • Li YB; State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
Cancer Lett ; 340(1): 88-96, 2013 Oct 28.
Article em En | MEDLINE | ID: mdl-23856030
ABSTRACT
Accumulating evidence suggested that the irreversible tyrosine kinase inhibitors (TKIs) have potential to override the acquired resistance to target-based therapies. Herein, we reported IC-4 as a novel irreversible TKI for epidermal growth factor receptor (EGFR). IC-4 potentially suppressed proliferation, induced apoptosis and a G2/M cell cycle arrest in breast cancer cells, correlating with inhibition of EGF-induced EGFR activation, but independent of DNA damage. In addition, IC-4 exhibited anti-angiogenetic activities both in vitro and in vivo. It suppressed cell viability and proliferation induced by various growth factors in human umbilical vein endothelial cells (HUVECs). IC-4 also inhibited HUVECs migration and tube formation. In transgenic zebrafish embryo model, IC-4 was shown to suppress formation of intersegmental vessel and development of subintestinal vessels. Taken together, these results demonstrated that IC-4 is a new irreversible EGFR-TKI, exhibiting potent anti-breast cancer and anti-angiogenetic effects.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Tiocarbamatos / Neoplasias da Mama / Processamento de Proteína Pós-Traducional / Inibidores da Angiogênese / Receptores ErbB Tipo de estudo: Prognostic_studies Limite: Animals / Female / Humans Idioma: En Revista: Cancer Lett Ano de publicação: 2013 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Tiocarbamatos / Neoplasias da Mama / Processamento de Proteína Pós-Traducional / Inibidores da Angiogênese / Receptores ErbB Tipo de estudo: Prognostic_studies Limite: Animals / Female / Humans Idioma: En Revista: Cancer Lett Ano de publicação: 2013 Tipo de documento: Article