A series of 6-alkoxy-4-anilinoquinazoline compounds was prepared and evaluated for in vitro inhibition of the erbB2 and EGFR kinase activity. The IC(50) values of the best compounds were below 0.10 uM. Further, several of these compounds inhibit the growth of erbB2 and EGFR over-expressing tumor cell lines at concentrations below 1 uM.
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http://dx.doi.org/10.1016/j.bmcl.2003.10.010 | DOI Listing |
Diagn Pathol
January 2025
Pathology Department, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, No. 1277, Jiefang Avenue, Wuhan, 430022, Hubei Province, China.
Breast cancer became the most prevalent malignancy among women, and HER2 expression status is critical for treatment decisions. With the emergence of ADC drugs, HER2 low-expressing patients who previously did not respond well to traditional anti-HER2 therapies may now benefit. In this study, immunohistochemistry (IHC) and fluorescence in situ hybridization (FISH) were applied to assess HER2 expression in 349 patients with HER2-non-positive breast cancer.
View Article and Find Full Text PDFBMC Genom Data
January 2025
Medical Oncology, Central Hospital of Guangdong Provincial Nongken, Zhanjiang, Guangdong, China.
Proc Natl Acad Sci U S A
January 2025
Laboratory of Precision Medicine and Biopharmaceuticals, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.
Recurrent missense mutations in the human epidermal growth factor receptor 2 (HER2) have been identified across various human cancers. Among these mutations, the active S310F mutation in the HER2 extracellular domain stands out as not only oncogenic but also confers resistance to pertuzumab, an antibody drug widely used in clinical cancer therapy, by impeding its binding. In this study, we have successfully employed computational-aided rational design to undertake directed evolution of pertuzumab, resulting in the creation of an evolved pertuzumab variant named Ptz-SA.
View Article and Find Full Text PDFMedicine (Baltimore)
January 2025
Department of Thyroid and Breast Surgery, Hebei General Hospital, Shijiazhuang, Hebei Province, China.
To assess whether metabolic syndrome can be used as a reference index to evaluate the efficacy of neoadjuvant chemotherapy treatment for breast cancer (BC). Seventy cases of female BC patients who received neoadjuvant chemotherapy treatment and surgical treatment at the Glandular Surgery Department of Hebei Provincial People's Hospital from January 2021 to December 2023 were retrospectively collected, and clinical data such as puncture pathology were recorded. The clinical data were analyzed by 1-way analysis using the χ2 test, and further multifactorial logistic regression analysis was performed for statistically significant differences.
View Article and Find Full Text PDFJ Cancer Res Ther
December 2024
Department of Medical Oncology, National Cancer Center/National Clinical Research Center for Cancer/Cancer Hospital and Shenzhen Hospital, Chinese Academy of Medical Sciences and Peking Union Medical College, Shenzhen, People's Republic of China.
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