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Elucidating the binding specificity of interactive compounds targeting ATP-binding cassette subfamily G member 2 (ABCG2).
Mol Divers
January 2025
Data Science, Amity Institute of Integrative Sciences and Health, Amity University Haryana, Gurugram, India.
The ATP-binding cassette transporter superfamily plays a pivotal role in cellular detoxification and drug efflux. ATP-binding cassette subfamily G member 2 (ABCG2) referred to as the Breast cancer resistance protein has emerged as a key member involved in multidrug resistance displayed by cancer cells. Understanding the molecular basis of substrate and inhibitor recognition, and binding within the transmembrane domain of ABCG2 is crucial for the development of effective therapeutic strategies.
View Article and Find Full Text PDFNew metal complexes of 1H-benzimidazole-2-yl hydrazones: Cytostatic, proapoptotic and modulatory activity on kinase signaling pathways.
Arch Biochem Biophys
November 2024
Institute of Organic Chemistry with Centre of Phytochemistry, Bulgarian Academy of Sciences, Acad. G. Bonchev Str., build. 9, 1113, Sofia, Bulgaria; University of Chemical Technology and Metallurgy, 8 Kliment Ohridski Blvd., 1756, Sofia, Bulgaria. Electronic address:
The copper complexes of two 1H-benzimidazole-2-yl hydrazones were obtained by complexation with copper chloride. The molecular structure of the complexes was studied by microchemical analysis, SEM-EDX, IR and micro-Raman spectroscopy and DFT calculations. It was found that both ligands form 1:1 complexes with the copper, where the Cu ions are coordinated by N-atom from the benzimidazole ring, N-atom of the azomethine bond, O-atom from the ortho-OH group of the aromatic ring and one chlorine atom.
View Article and Find Full Text PDFIntegration of Machine Learning and Experimental Validation to Identify Anoikis-Related Prognostic Signature for Predicting the Breast Cancer Tumor Microenvironment and Treatment Response.
Genes (Basel)
November 2024
Institute of Physical Education and Sport, Shanxi University, Taiyuan 030006, China.
Anoikis-related genes (ANRGs) are crucial in the invasion and metastasis of breast cancer (BC). The underlying role of ANRGs in the prognosis of breast cancer patients warrants further study. The anoikis-related prognostic signature (ANRS) was generated using a variety of machine learning methods, and the correlation between the ANRS and the tumor microenvironment (TME), drug sensitivity, and immunotherapy was investigated.
View Article and Find Full Text PDFImatinib Impedes EMT and Notch Signalling by Inhibiting p300 Acetyltransferase in Breast Cancer Cells.
Mol Carcinog
February 2025
Department of Biosciences and Bioengineering, Indian Institute of Technology Guwahati, Guwahati, Assam, India.
Breast cancer remains a leading cause of cancer-related mortality among women, with current therapeutic approaches often limited by resistance and recurrence, especially in aggressive subtypes like triple-negative breast cancer. Drug repurposing has emerged as a promising strategy to address these challenges. In this study, we investigate the potential of Imatinib, a repurposed tyrosine kinase inhibitor, to inhibit epithelial-mesenchymal transition (EMT) in breast cancer cells by modulating the Notch signalling pathway.
View Article and Find Full Text PDFPPARγ antagonism as a new tool for preventing or overcoming endocrine resistance in luminal A breast cancers.
Biomed Pharmacother
November 2024
Department of Clinical and Biological Sciences, University of Turin, Corso Raffaello 30, Turin 10125, Italy. Electronic address:
Purpose: This research investigates the role of PPARγ in the complex molecular events underlying the acquisition of resistance to tamoxifen (Tam) in luminal A breast cancer (BC) cells. Furthermore, it focuses on evaluating the possibility of repurposing Imatinib mesylate, an FDA-approved anticancer agent recently recognized also as a PPARγ antagonist, for the personalized therapy of endocrine-resistant BC with increased PPARγ expression.
Methods: Differential gene expression between parental and Tam-resistant MCF7 cells was assessed by RNA-seq followed by bioinformatics analysis and validation by RT-qPCR.
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