Khelline is naturally occurring furochromone exhibited significant Epidermal Growth Factor Receptor (EGFR) inhibitory activity. The newly synthesized compounds 2-5 displayed the most potent EGFR inhibitory activity on MCF-7 and HeLa. In vitro study against 59 different human tumour cell lines derived from nine cancer type in NCI (USA), which was presented and documented. Molecular docking simulation was performed to position compounds 1-5 into the EGFR active site to determine the probable binding mode.
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http://dx.doi.org/10.3109/14756366.2012.719504 | DOI Listing |
Biochem Pharmacol
January 2025
CAS Key Laboratory of Nano-Bio Interface, Suzhou Institute of Nano-Tech and Nano-Bionics, Chinese Academy of Sciences, Suzhou 215123, China. Electronic address:
CAR-T cell therapy has been proven to be effective on hematological tumors, although graft-versus-host disease and cytokine release syndrome(CRS) limit its application to a certain extent. However, CAR-T therapy for solid tumors met challenges, among which the lack of tumor-specific antigens (TSA) and immunosuppressive tumor microenvironment (TME) are the most important factors. CAR-NK could be a good alternative to CAR-T in some ways since they can induce mild CRS and are independent of HLA-matching, but the efficacy of CAR-NKs remains limited in solid tumors.
View Article and Find Full Text PDFBalkan Med J
January 2025
Department of Clinical Pharmacy, China Pharmaceutical University, School of Basic Medicine and Clinical Pharmacy, Nanjing, China.
Acta Pharmacol Sin
January 2025
State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin, 300350, China.
Histone lysine-specific demethylase 1 (LSD1) is overexpressed in various solid and hematological tumors, suggesting its potential as a therapeutic target, but there are currently no LSD1 inhibitors available on the market. In this study we employed a computer-guided approach to identify novel LSD1/EGFR dual inhibitors as a potential therapeutic agent for non-small cell lung cancer. Through a multi-stage virtual screening approach, we found L-1 and L-6, two compounds with unique scaffolds that effectively inhibit LSD1 with IC values of 6.
View Article and Find Full Text PDFCan Respir J
December 2024
Department of Rehabilitation, Hospital of Chengdu University of Traditional Chinese Medicine, Chengdu 610072, China.
This study aimed to investigate the effect of Fuzheng Yiai Decoction (FZYA) on epidermal growth factor receptor-tyrosine kinase inhibitor (EGFR-TKI) drug resistance in lung adenosquamous carcinoma (ASC). The expression of thyroid transcription factor 1 (TTF1) and p63 in tumor cells was observed by immunofluorescence staining. Meanwhile, 25 nude mice successfully inoculated with the human lung ASC cell line NCI-H596 were randomly divided into five groups, namely, the model, gefitinib, low-, medium-, and high-dose FZYA with gefitinib groups.
View Article and Find Full Text PDFEur J Med Chem
December 2024
School of Pharmacy, Hangzhou Medical College, Hangzhou, 310053, China; School of Pharmacy, Zhejiang University, Hangzhou, 310058, China. Electronic address:
Dysregulated activation of the PI3K/AKT/mTOR pathway is crucial in the development of cancer, and disrupting it could potentially lead to cancer suppression, making it a viable strategy for cancer treatment. Here, as a consecutive work of our team, we described the identification and optimization of PI3K/mTOR inhibitors based on triazine scaffold, which exhibited potent PI3K/mTOR inhibitor activity. The systematically structure-activity relationship (SAR) results demonstrated that compound 5nh displayed high efficacy against PI3Kα and mTOR, with the IC values of 0.
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