sotrastaurin has been researched along with Breast-Neoplasms* in 2 studies
2 other study(ies) available for sotrastaurin and Breast-Neoplasms
| Article | Year |
|---|---|
Novel Aurora A and Protein Kinase C (α, β1, β2, and θ) Multitarget Inhibitors: Impact of Selenium Atoms on the Potency and Selectivity.
Aurora kinases and protein kinase C (PKC) have been shown to be involved in different aspects of cancer progression. To date, no dual Aurora/PKC inhibitor with clinical efficacy and low toxicity is available. Here, we report the identification of compound Topics: Antineoplastic Agents; Aurora Kinase A; Breast Neoplasms; Cell Line, Tumor; Drug Screening Assays, Antitumor; Female; Humans; Hydrogen Bonding; Isoenzymes; Molecular Docking Simulation; Protein Kinase C; Protein Kinase Inhibitors; Selenium Compounds; Small Molecule Libraries; Structure-Activity Relationship; Substrate Specificity; Tumor Stem Cell Assay | 2022 |
Protein kinase C targeting of luminal (T-47D), luminal/HER2-positive (BT474), and triple negative (HCC1806) breast cancer cells in-vitro with AEB071 (Sotrastaurin) is efficient but mediated by subtype specific molecular effects.
Protein kinase C (PKC) plays a pivotal role in malignant cell proliferation, apoptosis, invasiveness and migration. However, its exploitation as therapeutic target in breast cancer has been merely explored. Here were evaluated the AEB071 (Sotrastaurin™) treatment efficiency of breast cancer cell lines derived from estrogen receptor positive (T-47D), estrogen/HER2 receptor positive (BT474), and triple negative (HCC1806) breast cancer cells under 2D (monolayer) and 3D (multicellular tumor spheroids) culture conditions. Additionally, spheroid cocultures of BC and N1 fibroblasts were analyzed.. We quantitatively assessed the proliferation capacity of breast cancer cells and fibroblasts as a function of AEB071 treatment using flow cytometry. The activities of PKC isoforms, substrates, and key molecules of the PKC signaling known to be involved in the regulation of tumor cell proliferation and cellular survival were additionally evaluated. Moreover, a multigene expression analysis (PanCancer Pathways assay) using the nanoString™ technology was applied.. All breast cancer cell lines subjected to this study were sensitive to AEB071 treatment, whereby cell proliferation in 2D culture was considerably (BT474) or moderately (HCC1806) retarded in G0/G1 or in G2/M phase (T-47D) of the cell cycle. Regardless of the breast cancer subtype the efficiency of AEB071 treatment was significantly lower in the presence of N1 fibroblast cells. Subtype specific driver molecules, namely IL19, c-myb, and NGFR were mostly affected by the AEB071 treatment.. A combined targeting of PKC and a subtype specific driver molecule might complement specified breast cancer treatment. Topics: Breast Neoplasms; Cell Line, Tumor; Cell Proliferation; Female; Humans; Protein Kinase C; Pyrroles; Quinazolines; Receptor, ErbB-2 | 2022 |