Efficacy and mechanism of action of Proellex, an antiprogestin in aromatase overexpressing and Letrozole resistant T47D breast cancer cells

2013 ◽  
Vol 133 ◽  
pp. 30-42 ◽  
Author(s):  
Akash Gupta ◽  
Rajeshwari Mehta ◽  
Fatouma Alimirah ◽  
Xinjian Peng ◽  
Genoveva Murillo ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Mechanism Of Action ◽  
Breast Cancer Cells

scholarly journals Conjugation of palbociclib with MHI-148 has an increased cytotoxic effect for breast cancer cells and an altered mechanism of action

2021 ◽  
Author(s):  
Euphemia Leung ◽  
Petr Tomek ◽  
Moana Tercel ◽  
Johannes Reynisson ◽  
Thomas In Hyeup Park ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Endocrine Therapy ◽  
Mechanism Of Action ◽  
Oestrogen Receptor ◽  
Breast Cancer Cells ◽  
Cytotoxic Effect ◽  
Near Infrared ◽  
Triple Negative ◽  
Mammalian Cell Lines

The CDK4/6 inhibitor palbociclib, combined with endocrine therapy, has been shown to be effective in postmenopausal women with oestrogen receptor positive, HER2-negative advanced or metastatic breast cancer. However, palbociclib is not as effective in the highly aggressive triple-negative breast cancer that lacks sensitivity to chemotherapy or endocrine therapy. We hypothesized that conjugation of the near-infrared dye MHI-148 with palbociclib can produce a potential theranostic in triple-negative as well as oestrogen receptor positive breast cancer cells. In our study, the conjugate was found to have enhanced activity in all mammalian cell lines tested in vitro. However, the conjugate was cytotoxic and did not induce G1 cell cycle arrest in breast cancer cells suggesting the mechanism of action differed from the parent compound palbociclib. The study highlights the importance of investigating the mechanism of conjugates of near-infrared dyes to therapeutic compounds as conjugation can potentially result in a change of mechanism or target, with an enhanced cytotoxic effect in this case.

scholarly journals Unacylated ghrelin and AZP531 suppress the 3D growth of breast cancers

2020 ◽  
Author(s):  
CheukMan C. Au ◽  
John B. Furness ◽  
Kara Britt ◽  
Sofya Oshchepkova ◽  
Heta Ladumor ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Mechanism Of Action ◽  
Breast Cancer Cells ◽  
Therapeutic Potential ◽  
3D Culture ◽  
Mapk Signaling ◽  
Unacylated Ghrelin ◽  
Ghrelin Receptor

ABSTRACTBreast cancer is the most common type of cancer in women and notwithstanding important therapeutic advances, it remains the second leading cause of cancer-related death in the US. Despite extensive research relating to the hormone ghrelin, responsible for the stimulation of growth hormone release and appetite, little is known of the effects of its unacylated form, especially in cancer. One major area of research relates to its reported effects to increase insulin sensitivity in diabetics, this being the basis for the development of unacylated ghrelin analog, AZP531 or livoletide, now in clinical trials for the treatment of Prader-Willi Syndrome. The mechanism of action of unacylated ghrelin is largely uncharacterized, in any system, because it does not bind to or activate the cognate ghrelin receptor, GHSR1a. The present study aimed to characterize effects of unacylated ghrelin on breast cancer cells, define its mechanism of action, and explore the therapeutic potential of unacylated ghrelin or analog AZP531. We report potent effects of unacylated ghrelin, at picomolar doses, on the growth of breast cancer cells, dependent on 3D culture and activation of Gαi. Suppression of MAPK signaling by unacylated ghrelin leads to cell cycle arrest and apoptosis. AZP531 also suppresses the growth of breast cancer cells in vitro and in xenografts, and may be a novel approach for the safe and effective treatment of breast cancer.

Anticancer activity and mechanism of action evaluation of an acylhydrazone Cu(II) complex toward breast cancer cells, spheroids and mammospheres.

ChemMedChem ◽  
2021 ◽  
Author(s):  
Lucia M. Balsa ◽  
Maria R. Rodriguez ◽  
Beatriz S. Parajón-Costa ◽  
Ana C. González Baró ◽  
Martin J. Lavecchia ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Anticancer Activity ◽  
Cancer Cells ◽  
Mechanism Of Action ◽  
Breast Cancer Cells

Synthesis of Bioactive Diarylheptanoids from Alpinia officinarum and Their Mechanism of Action for Anticancer Properties in Breast Cancer Cells

2021 ◽  
Vol 84 (2) ◽  
pp. 352-363
Author(s):  
Sunita Gamre ◽  
Mrityunjay Tyagi ◽  
Sucheta Chatterjee ◽  
Birija S. Patro ◽  
Subrata Chattopadhyay ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Mechanism Of Action ◽  
Breast Cancer Cells ◽  
Anticancer Properties ◽  
Alpinia Officinarum

scholarly journals Effects of Ulinastatin on Proliferation and Apoptosis of Breast Cancer Cells by Inhibiting the ERK Signaling Pathway

2021 ◽  
Vol 2021 ◽  
pp. 1-6
Author(s):  
Zeyu Xing ◽  
Xin Wang ◽  
Jiaqi Liu ◽  
Gang Liu ◽  
Menglu Zhang ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Mechanism Of Action ◽  
Breast Cancer Cells ◽  
Erk Signaling ◽  
Control Group ◽  
Hoechst 33258 ◽  
Protein Levels ◽  
Proliferation And Apoptosis ◽  
Positive Rate

Purpose. To explore the effects of ulinastatin on the proliferation and apoptosis of breast cancer cells and the relevant mechanism of action. Methods. Breast cancer cells (MCF-7) were cultured and randomly divided into three groups, namely, control group, ulinastatin group, and ulinastatin+extracellular-regulated protein kinase (ERK) inhibitor group. Then, the Cell Counting Kit-8 (CCK-8) assay was carried out to detect the effect of ulinastatin on the viability of breast cancer cells. The effects of ulinastatin on the proliferation and apoptosis of breast cancer cells were determined via EdU staining and Hoechst 33258 staining assays, respectively. The messenger ribonucleic acid (mRNA) and protein expression levels of ERK and forkhead box O3 (FOXO3) in breast cancer cells were measured through reverse transcription-polymerase chain reaction (RT-PCR) and Western blotting. Results. In comparison with the control group, the ulinastatin group displayed decreased viability of breast cancer cells, a decreased positive rate of 5-ethynyl-2 ′ -deoxyuridine (EdU) staining, an increased positive rate of Hoechst 33258 staining, and reduced mRNA and protein levels of ERK and FOXO3 in breast cancer cells. Compared with those in the ulinastatin group, the viability of breast cancer cells was lowered, the positive rate of EdU staining was reduced, the positive rate of Hoechst 33258 staining was raised, and the mRNA and protein levels of ERK and FOXO3 in breast cancer cells clearly declined in the ulinastatin+ERK inhibitor group. Conclusion. Ulinastatin inhibits the proliferation and promotes the apoptosis of breast cancer cells. The possible mechanism of action is associated with the suppression of the ERK signaling pathway.

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