Category Ranking
98%
Total Visits
921
Avg Visit Duration
2 minutes
Citations
20
Article Abstract
It is generally believed that EGFR/HER2 dual-target inhibitors may overcome the resistance of EGFR TKIs caused by HER2 overexpression. The structure-based synthesis and biological evaluation of quinazoline derivatives as EGFR/HER2 dual-target inhibitors has been studied in this paper. II-1, II-2, III-3, III-4 displayed comparable inhibitory potency against EGFR and HER2 and II-1 showed remarkable antiproliferative activities against NCI-H358/PC-9/Calu-3/NCI-H1781 (EGFR IC = 0.30 nM, HER2 IC = 6.07 nM, NCI-H358 GI = 23.30 nM, PC-9 GI = 1.95 nM, Calu-3 GI = 23.13 nM NCI-H1781 GI = 41.61 nM).
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2022.128703 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Synthesis and biological evaluation of new series of quinazoline derivatives as EGFR/HER2 dual-target inhibitors.
Bioorg Med Chem Lett
July 2022
School of Pharmaceutical Science, Jiangnan University, Wuxi, China. Electronic address:
It is generally believed that EGFR/HER2 dual-target inhibitors may overcome the resistance of EGFR TKIs caused by HER2 overexpression. The structure-based synthesis and biological evaluation of quinazoline derivatives as EGFR/HER2 dual-target inhibitors has been studied in this paper. II-1, II-2, III-3, III-4 displayed comparable inhibitory potency against EGFR and HER2 and II-1 showed remarkable antiproliferative activities against NCI-H358/PC-9/Calu-3/NCI-H1781 (EGFR IC = 0.
View Article and Find Full Text PDFAntitumor Effects of MEHD7945A, a Dual-Specific Antibody against EGFR and HER3, in Combination with Radiation in Lung and Head and Neck Cancers.
Mol Cancer Ther
September 2015
Department of Human Oncology, University of Wisconsin School of Medicine and Public Health, Madison, Wisconsin.
Article Synopsis
- Human epidermal growth factor receptors (EGFR, HER2, HER3, HER4) are crucial in cancer growth and treatment responses, prompting research into a new dual-target antibody, MEHD7945A, which targets EGFR and HER3 together.
- The study demonstrated that MEHD7945A, when combined with radiation therapy, enhances the effectiveness of the radiation by increasing DNA damage in cancer cells and inhibiting signaling pathways that promote tumor growth.
- Results showed that patients' tumors treated with MEHD7945A and radiation exhibited reduced tumor growth and vascular markers, indicating its potential as a significant enhancer in radiation treatment for lung and head and neck cancers, warranting further clinical trials.