Article
Cell Biology
Zhiguo Niu, Jianing Fan, Fengzhe Chen, Huijie Yang, Xin Li, Ting Zhuang, Chunlei Guo, Qi Cao, Jian Zhu, Hui Wang, Qingsong Huang
Summary: Breast cancer is the most common malignancy in women globally. Abnormal expression of RBCK1 protein in breast tumors makes it a valuable diagnostic marker and drug target. Hypoxic regions in breast cancer activate the HIF1 pathway, influencing tumor recurrence and metastasis. Targeting RBCK1 could be a promising treatment strategy for ER-positive breast cancer.
CELL DEATH & DISEASE
(2022)
Article
Biology
Juan P. Munoz, Gloria M. Calaf
Summary: Acetylcholine (ACh) can activate the MAPK/ERK and PI3K/Akt pathways, induce p-ERα expression and nuclear translocation in breast cancer cell lines. However, ACh and 17β-estradiol have different mechanisms of action, and ACh can enhance cell viability and induce overexpression of specific EMT markers.
Article
Biochemistry & Molecular Biology
Jiahao Chen, Jingxin Liu, Pengguihang Zeng, Cai Zhao, Xinyi Liu, Jun Sun, Jia Wang, Peihang Fang, Wenjie Chen, Junjun Ding
Summary: Estrogen (E2) and BRCA1 deficiency synergistically induce DNA damage in breast cancer cells, possibly involving transcriptional activation of ER genes and changes in DNA damage distribution.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2022)
Article
Biochemistry & Molecular Biology
Shaimaa Hamza, Ekaterina E. E. Garanina, Mohammad Alsaadi, Svetlana F. F. Khaiboullina, Gulcin Tezcan
Summary: NLRP3 may contribute to the growth and propagation of breast cancer, and the effects of ER-alpha, PR, and HER2 on NLRP3 activation in breast cancer are still unknown.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Genetics & Heredity
Ajay Kumar, Arun Dhillon, Mohan Chowdenahalli Manjegowda, Neha Singh, Dixcy Jaba Sheeba John Mary, Sachin Kumar, Deepak Modi, Anil Mukund Limaye
Summary: This study reveals that estrogen suppresses HOXB2 expression, with ERα playing a role in this suppression. Future investigations should explore the implications of estrogen-mediated suppression on the proposed tumor suppressor function of HOXB2.
Article
Cell Biology
Xiaohong Xia, Chuyi Huang, Yuning Liao, Yuan Liu, Jinchan He, Zhenlong Shao, Tumei Hu, Cuifu Yu, Lili Jiang, Jinbao Liu, Hongbiao Huang
Summary: The study highlights the importance of deubiquitinase USP15 in preventing ERα degradation and promoting breast cancer progression. Knockdown of USP15 enhances the antitumor activities of tamoxifen on breast cancer cells. These findings provide a new approach to overcoming resistance to endocrine therapy and targeting the USP15-ERα axis for therapeutic strategies on ERα degradation.
CELL DEATH & DISEASE
(2021)
Article
Oncology
Sung Gwe Ahn, Soong June Bae, Yoonjung Kim, Jung Hwan Ji, Chihhao Chu, Dooreh Kim, Janghee Lee, Yoon Jin Cha, Kyung-A Lee, Joon Jeong
Summary: This study found that ESR1 mutations were rare in non-metastatic ER+ breast cancer patients, but were closely associated with primary endocrine resistance. Patients with ESR1 mutations had significantly lower survival rates and recurrence-free intervals compared to those without ESR1 mutations.
Article
Environmental Sciences
Juan P. Munoz, Rocio Araya-Osorio, Raul Mera-Adasme, Gloria M. Calaf
Summary: Recent reports have questioned the safety of glyphosate, the active ingredient in several herbicide formulations, suggesting that it may act as an endocrine disruptor by promoting estrogenic activity. This study aimed to investigate the mechanism by which glyphosate induces estrogenic effects using breast cancer cell line models. The results showed that high concentrations of glyphosate mimic the effects of estrogen, leading to the activation of estrogen receptor alpha and enhanced cell proliferation.
Article
Oncology
Charly Jehanno, Pascale Le Goff, Denis Habauzit, Yann Le Page, Sylvain Lecomte, Estelle Lecluze, Frederic Percevault, Stephane Avner, Raphael Metivier, Denis Michel, Gilles Flouriot
Summary: Hormone receptor positive breast cancer often develops resistance to treatment, leading to metastatic relapses. Understanding the molecular mechanisms behind this resistance is crucial. Hypoxia, a common feature of solid tumors, has been shown to promote endocrine resistance by down-regulating estrogen receptor alpha (ER alpha) expression.
Article
Chemistry, Medicinal
Lilan Xin, Jian Min, Hebing Hu, Yuanyuan Li, Chuanqian Du, Baohua Xie, Yan Cheng, Xiaofei Deng, Xiangping Deng, Kang Shen, Jian Huang, Chun -Chi Chen, Rey-Ting Guo, Chune Dong, Hai -Bing Zhou
Summary: In this study, a novel class of dual-targeting selective estrogen receptor degraders (SERDs) based on a three-dimensional oxabicycloheptene sulfonamide (OBHSA) scaffold equipped with aromatase inhibitor (AI) activity were identified. These compounds showed excellent ERa degradation activity, ARO inhibitory activity, and antiproliferative activity against drug-resistant breast cancer cells.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Oncology
Giuseppina Daniela Naimo, Martina Forestiero, Alessandro Paoli, Rocco Malivindi, Luca Gelsomino, Balazs Gyorffy, Adele Elisabetta Leonetti, Francesca Giordano, Salvatore Panza, Francesca Luisa Conforti, Paola Ruffo, Maria Luisa Panno, Loredana Mauro, Sebastiano Ando
Summary: Adiponectin enhances ERa-positive breast cancer cell growth and distant metastasis by promoting E-cadherin expression and altering cell polarity through the ERa/LKB1 complex. The presence of E-cadherin is crucial for the proliferative effects of adiponectin on breast cancer cells. Furthermore, adiponectin treatment leads to the colocalization of LKB1 and Cdc42 in the nucleus, impairing their cytosolic cooperation in maintaining cell polarity. These findings highlight the importance of adiponectin in breast cancer progression and metastasis.
INTERNATIONAL JOURNAL OF CANCER
(2023)
Review
Oncology
Ebony Hargrove-Wiley, Barbara Fingleton
Summary: Sex hormones such as estrogens and androgens play a crucial role in the pathophysiology of various cancers by regulating genomic and cellular processes. They can modulate immune signals and activities in tumor cells and leukocytes, affecting cancer progression. Understanding the impact of sex hormones on tumor immunity in the breast cancer microenvironment is important for developing effective therapies. Combining endocrine therapy with immunotherapy can enhance the antitumor immune response.
Article
Oncology
Stefania Bartoloni, Stefano Leone, Sara Pescatori, Manuela Cipolletti, Filippo Acconcia
Summary: Telaprevir reduces the levels and function of estrogen receptor alpha (ER alpha) by decreasing FOXA1 levels and activity. The antiviral compound interacts with IGF1-R and transduces its effect through the IGF1-R/AKT/FOXA1 pathway, resulting in cell death in ER alpha-expressing breast cancer cells.
MOLECULAR ONCOLOGY
(2022)
Article
Pharmacology & Pharmacy
Xi Liu, Qian Hu, Wanyan Wang, Hui Ma, Jiaqian Pu, Jiayan Cui, Ting Gong, Yu Wu, Weiqiang Lu, Jin Huang
Summary: Gain-of-function mutations in estrogen receptor alpha (ER alpha) are associated with hormone therapy resistance in breast cancer. A new GLPCA method was developed to evaluate ER alpha mutants, identifying natural products celastrol and gambogic acid as antagonists, which showed synergistic anti-cancer effects when combined with CDK4/6 inhibitor abemaciclib.
BIOCHEMICAL PHARMACOLOGY
(2021)
Review
Chemistry, Medicinal
Teesha Downton, Fiona Zhou, Davendra Segara, Rinath Jeselsohn, Elgene Lim
Summary: The translated article discusses the limitations of current endocrine therapies for ER-positive breast cancer and the mechanisms of drug resistance, focusing on ESR1 mutations. It also provides an overview of the development and research progress of oral SERDs in improving treatment outcomes.
DRUG DESIGN DEVELOPMENT AND THERAPY
(2022)