To understand the mechanisms leading to trastuzumab resistance in HER2-overexpressing breast tumors, we created trastuzumab-insensitive cell lines (SKBR3/100-8 and BT474/100-2). The cell lines maintain HER2 receptor overexpression and show increase in EGF receptor (EGFR). Upon trastuzumab treatment, SKBR3/100-8 and BT474/100-2 cell lines displayed increased growth rate and invasiveness. The tra...

Lapatinib is highly active against breast cancer with HER2 overexpression in preclinical and clinical settings. Constitutive activation of NF-κB is linked to proliferation and apoptosis in breast cancer cells. NF-κB can be activated by HER2 in breast cancer cells. However, the effect of lapatinib on NF-κB activity is not completely clear. In this ...

Human breast cancer cell line SKBR3 expresses high level of the ErbB2 molecule, which has been associated with poor prognosis of breast cancer. Elevated ErbB2 functions as a transactivating co-receptor and promotes the formation of ErbB2 containing heterodimers, which are more mitogenic and transforming, and have a higher ligand affinity and signaling potency by virtue of the potent latent kina...

Improved understanding of the molecular mechanisms by which small-molecule inhibitors of histone deacetylases (HDAC) induce programs, such as cellular differentiation and apoptosis, would undoubtedly assist their clinical development as anticancer agents. As modulators of gene transcript levels, HDAC inhibitors (HDACi) typically affect only 5% to 10% of actively transcribed genes with approxima...

Both erbB3 and IGF-1 receptor (IGF-1R) have been shown to play an important role in trastuzumab resistance. However, it remains unclear whether erbB3- and IGF-1R-initiated signaling pathways possess distinct effects on the sensitivity of lapatinib, a dual tyrosine kinase inhibitor against both EGFR and erbB2, in trastuzumab-resistant breast cancer. Here, we show that the trastuzumab-resistant S...

Treatment of HER2+ breast cancer with trastuzumab is effective and combination anti-HER2 therapies have demonstrated benefit over monotherapy in the neoadjuvant and metastatic settings. This study investigated the therapeutic potential of targeting the BAG-1 protein co-chaperone in trastuzumab-responsive or -resistant cells. In the METABRIC dataset, BAG-1 mRNA was significantly elevated in HER2...

introduction: auger electron based radioimmunotherapy (rit) using 111in-dota-trastuzumab (111in-dota-antiher2) feasibility was studied in vitro on a her2/neu positive cell line, skbr3. methods:111in-dota-antiher2 was prepared according to the optimized conditions followed by quality control tests including radiochemical purity; immunoreactivity). skbr3 as a her2/neu positive cell line was used ...

Evaluation of anticancer effect of Sapindus trifoliatus (familySapindaceae) which has long been prescribed for various infectious and malignant diseases. Bio-assays of extracts from Sapindus trifoliatus showed that a fraction (fraction 3) from an ethanolic extract had an antiproliferative effect on SKBR3 and MDA-MB435 human breast cancer cells. The ED50 value of Sapindus trifoliatus, fraction 3...

We report the rational design, based on docking simulations, and synthesis of the first fluorescent and selective probe of GPER for bioimaging purposes and functional dissecting studies. It has been conceived as a Bodipy derivative and obtained by accessible and direct synthesis. Its optical properties have been measured in different solvents, showing insensitivity to their polarity. Its bindin...

the polyphenol silybin has anti-oxidant and anti-cancer properties. the poor bioavailability of some polyphenols (flavonoids, and terpenoids) can be improved by binding them to phosphatidylcholine (phytosome technology). many studies have focused on the most common phytosome, silybin-phosphatidylcholine, particularly for its hepatoprotective effects. however, in recent years, studies have also ...