Article
Medicine, Research & Experimental
Guan-Yu Ruan, Li-Xiang Ye, Jian-Song Lin, Hong-Yu Lin, Li-Rui Yu, Cheng-Yan Wang, Xiao-Dan Mao, Shui-Hua Zhang, Peng-Ming Sun
Summary: The study found that kaempferol, a phytoestrogen, can suppress the proliferation and migration abilities of endometrial cancer cells and promote apoptosis. The mechanisms of action involve HSD17B1-related estrogen metabolism pathways. These findings provide new insights into the potential of phytoestrogens in medical applications.
JOURNAL OF TRANSLATIONAL MEDICINE
(2023)
Review
Biochemistry & Molecular Biology
Kenta Yoh, Kazuhiro Ikeda, Kuniko Horie, Satoshi Inoue
Summary: Estrogen is an essential hormone that primarily functions in the female reproductive system and has pleiotropic effects in various tissues and organs. Low estrogen levels, such as in postmenopausal women, can lead to disorders like cardiovascular disease, dementia, metabolic syndrome, osteoporosis, sarcopenia, and frailty. Estrogen receptors (ERs) and estrogen-related receptors (ERRs) play crucial roles in muscle physiology, including muscle mass maintenance, exercise physiology, and regeneration, particularly in relation to mitochondrial function and metabolism.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Review
Endocrinology & Metabolism
Kaoru Sato, Ken-ichi Takayama, Satoshi Inoue
Summary: Estrogens play an important role in the female reproductive system and also regulate physiological processes associated with learning and memory in the brain. They have neuroprotective effects in the pathogenesis of Alzheimer's disease (AD), which has a higher incidence in older and postmenopausal women. Estrogens bind to estrogen receptors (ERs) and activate transcriptional machineries, and also stimulate signal transduction through membrane ERs (mERs). Estrogen-related receptors (ERRs), which lack estrogen-binding capabilities, are expressed in the human brain and implicated in AD pathogenesis.
FRONTIERS IN ENDOCRINOLOGY
(2023)
Review
Biochemistry & Molecular Biology
Alina Kurylowicz
Summary: Menopausal decline in estrogen levels leads to changes in adipose tissue distribution and increased obesity prevalence in women. Hormone replacement therapy can partially restore these effects, indicating the significant role of estrogen in adipocyte regulation. Preclinical studies have shown involvement of estrogen in adipose tissue development, metabolism, and inflammation. However, the relationship between estrogen and obesity is bidirectional, as estrogen deficiency leads to fat accumulation and impairs adipocyte function, while obese individuals have altered expression of estrogen receptors and key enzymes involved in their synthesis. This narrative review provides an overview of estrogen's role in adipose tissue development, physiology, and obesity-related dysfunction, as well as discussing potential therapeutic applications in obesity treatment.
Article
Oncology
Hong Liu, Yang Huang, Jing Yang, Xuejiao Xu, Qiaomei Dai, Yuwei Zhang, Li Zhao, Mengdi Zhang, Jing Zhang, Tonghui Liu, Lili Zhong
Summary: This study demonstrates that K-3-G may improve age-related cognitive decline by inhibiting microglial inflammation through its action on estrogen receptors (ERs). K-3-G upregulates the expression of ERα and ERβ, reduces the number of inflammatory cells, and decreases production of inflammatory molecules in mice. In BV2 microglial cells, K-3-G exhibits similar anti-inflammatory effects and its effects are partially diminished by an ER antagonist.
EXPERIMENTAL CELL RESEARCH
(2023)
Review
Oncology
Susanne Schueler-Toprak, Maciej Skrzypczak, Carsten Gruendker, Olaf Ortmann, Oliver Treeck
Summary: Ovarian cancer is the most lethal gynecological cancer mainly diagnosed in advanced stages, while endometrial cancer is often detected in early stages. Treatment options for recurrent or advanced disease are limited. Estrogens and their receptors play a role in both ovarian and endometrial cancers. This article provides an update on the current understanding of the roles of estrogen receptors in these cancers and highlights the need for further research.
Article
Oncology
Laura Giraldi, Emma Kofoed Lauridsen, Andrea Daniela Maier, Jorgen Vinslov Hansen, Helle Broholm, Kare Fugleholm, David Scheie, Tina Norgaard Munch
Summary: Meningiomas are the most common primary intracranial tumor in adults, and can experience dramatic growth during pregnancy, though the exact reasons remain unknown. Contrary to previous hypotheses, the study did not find evidence supporting prolactin as a key contributor to pregnancy-related meningioma growth. Similarities between cases and controls suggest that meningiomas early in life may represent a distinct biological entity.
Article
Fisheries
Shiyan Liu, Haofeng Ouyang, Chong Han, Jingjun Huang, Qiaoying Zhu, Dingrui Liu, Linqiang Han, Shuisheng Li, Guifeng Li, Haoran Lin, Yong Zhang
Summary: The study cloned six estrogen-related receptors (errs) from the gonads of mandarin fish and analyzed their expression patterns and functions.
AQUACULTURE REPORTS
(2022)
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
Multidisciplinary Sciences
Husam Oda, Elham Hedayati, Annelie Lindstrom, Ivan Shabo
Summary: Accumulating evidence shows that tumor-associated macrophages play a role in tumor progression, and high macrophage infiltration is associated with advanced tumor stages and poor prognosis in breast cancer. This study investigates the relationship between macrophage infiltration, GATA-3 expression, hormonal status, and differentiation grade in early breast cancer. The results suggest that macrophage infiltration may impact the differentiation, malignant behavior, and prognosis of breast cancer, regardless of the morphological and hormonal states of the cancer cells in the primary tumor.
Review
Endocrinology & Metabolism
Xue-Ling Xu, Zheng-Yuan Huang, Kun Yu, Jun Li, Xiang-Wei Fu, Shou-Long Deng
Summary: This review focuses on the role of ER alpha and ER beta in polycystic ovary syndrome (PCOS), ovarian cancer, and premature ovarian failure (POF), as well as the major challenges of existing therapies. It provides a reference for the treatment of estrogen target tissue ovarian diseases.
FRONTIERS IN ENDOCRINOLOGY
(2022)
Article
Geriatrics & Gerontology
Nina E. Baumgartner, Katelyn L. Black, Shannon M. McQuillen, Jill M. Daniel
Summary: Both previous and continuous midlife estradiol treatment can increase levels of nuclear ER alpha in the hippocampus, impacting gene expression and protein levels related to estrogen effects on memory, indicating a long-lasting regulatory role of hippocampal ER alpha in memory.
NEUROBIOLOGY OF AGING
(2021)
Article
Genetics & Heredity
Roya Ramezankhani, Afshin Abdi Ghavidel, Saadyeh Rashidi, Mahbubeh Rojhannezhad, Hamid Reza Abolkheir, Malihe Mirhosseini, Sara Taleahmad, Massoud Vosough
Summary: Pancreatic cancer is a leading cause of cancer mortality worldwide, with higher incidence and mortality rates in male patients. Efforts to improve therapeutic outcomes have been limited by low efficiency and drug resistance. This study identifies genetic factors that may link gender to pancreatic cancer progression and survival rates, highlighting the importance of androgenic effectors and axon guidance in tumorigenesis.
FRONTIERS IN GENETICS
(2022)
Article
Biochemistry & Molecular Biology
Woo-Ram Park, Da Jung Lim, Hyunkyu Sang, Eunae Kim, Jae-Hak Moon, Hueng-Sik Choi, In Seon Kim, Don-Kyu Kim
Summary: The aphid estrogen-related receptor (ERR) plays a crucial role in the fecundity and glycolytic control of aphids. Research on MpERR revealed that it modulates aphid fecundity by regulating glycolytic gene expression, providing insights into the growth and development mechanisms of aphids.
INSECT BIOCHEMISTRY AND MOLECULAR BIOLOGY
(2021)
Article
Medicine, Research & Experimental
Lei Wang, Jia Yi, Ling-yun Lu, Yue-ying Zhang, Lan Wang, Guo-sheng Hu, Yi-chen Liu, Jian-cheng Ding, Hai-feng Shen, Fang-qing Zhao, Hai-hua Huang, Wen Liu
Summary: The study revealed that estrogen can induce a circRNA program, with circPGR playing a crucial role in ER-positive breast cancer cell growth and tumorigenesis by acting as a ceRNA for miR-301a-5p to regulate cell cycle genes.
Article
Chemistry, Multidisciplinary
Liu-shan Chen, Meng Zhang, Peng Chen, Xiao-feng Xiong, Pei-qing Liu, Hai-bin Wang, Jun-jian Wang, Juan Shen
Summary: This study investigates the role of m(6)A modification in osteogenesis and reveals the functional significance of the FTO-PPARG axis in promoting the osteogenesis of human MSCs. It also sheds light on the role of m(6)A modification in mediating osteoporosis and osteonecrosis.
ACTA PHARMACOLOGICA SINICA
(2022)
Article
Chemistry, Multidisciplinary
Hong Wang, Zhe Chang, Guo-di Cai, Ping Yang, Jiang-he Chen, Shan-shu Yang, Yin-feng Guo, Ming-yu Wang, Xue-hua Zheng, Jin-ping Lei, Pei-qing Liu, De-peng Zhao, Jun-jian Wang
Summary: A series of novel indomethacin derivatives were evaluated for their anti-tumor effects in castration-resistant prostate cancer, with CZ-212-3 showing the most potent efficacy by degrading AR and its variants to inhibit tumor growth.
ACTA PHARMACOLOGICA SINICA
(2022)
Article
Cell Biology
Lin Zhong, Bin Yang, Zhenhua Zhang, Junfeng Wang, Xiaojuan Wang, Yinfeng Guo, Weifeng Huang, Qianqian Wang, Guodi Cai, Fan Xia, Shengning Zhou, Shuai Ma, Yichu Nie, Jinping Lei, Min Li, Peiqing Liu, Wenbin Deng, Yonghong Liu, Fanghai Han, Junjian Wang
Summary: This study found that autophagy-related gene 4B (ATG4B) was overexpressed in advanced gastric cancer (GCa) tumors and was associated with poor prognosis. Researchers identified Azalomycin F4a (Am-F4a) as a potent ATG4B inhibitor through screening a natural compound library. Am-F4a effectively inhibited GCa cell autophagy by directly binding to and inhibiting ATG4B, leading to suppressed tumor growth and reduced cell migration and invasion. Additionally, Am-F4a sensitized tumors to chemotherapy.
CELL DEATH & DISEASE
(2022)
Article
Pharmacology & Pharmacy
Hong Wang, Qianqian Wang, Guodi Cai, Zhijian Duan, Zoann Nugent, Jie Huang, Jianwei Zheng, Alexander D. Borowsky, Jian Jian Li, Peiqing Liu, Hsing-Jien Kung, Leigh Murphy, Hong-Wu Chen, Junjian Wang
Summary: Metabolic and epigenetic reprogramming contribute to cancer therapeutic resistance. In this study, it was found that TIGAR, an antioxidant and glucose metabolic regulator, interacts with NRF2 to stimulate NSD2 expression. Nuclear accumulation of TIGAR is associated with therapeutic resistance and poor survival.
ACTA PHARMACEUTICA SINICA B
(2022)
Article
Pharmacology & Pharmacy
Jianghe Chen, Yiwei Hu, Jian Zhang, Qianyu Wang, Xiongzhi Wu, Weiye Huang, Qianqian Wang, Guodi Cai, Hong Wang, Tianmiao Ou, Weineng Feng, Peiqing Liu, Yonghong Liu, Junfeng Wang, Jie Huang, Junjian Wang
Summary: This study reveals the function of RAR-related orphan receptor gamma (RORγ) in small cell lung cancer (SCLC) and identifies the anti-cancer activity of its natural inhibitor, N-hydroxyapiosporamide (N-hydap). The findings show that depletion of RORγ affects cell growth in SCLC and N-hydap inhibits RORγ activity, leading to reprogramming of neuroendocrine fate. The study suggests that RORγ could be a potential target for SCLC and N-hydap may be a promising therapeutic drug candidate.
PHARMACOLOGICAL RESEARCH
(2022)
Article
Microbiology
Jin Zhao, Jiaoshan Chen, Congcong Wang, Yajie Liu, Minchao Li, Yanjun Li, Ruiting Li, Zirong Han, Junjian Wang, Ling Chen, Yuelong Shu, Genhong Cheng, Caijun Sun
Summary: The key enzyme KMO and its metabolite QUIN show promise as novel broad-spectrum antiviral factors, inhibiting viral infections and disease progression by modulating calcium signaling pathways and interferon production. These findings have important implications for the development of new antiviral drugs.
Article
Biochemistry & Molecular Biology
Shumin Ouyang, Huaxuan Li, Linlin Lou, Qiuyao Huang, Zhenhua Zhang, Jianshan Mo, Min Li, Jiaye Lu, Kai Zhu, Yunjie Chu, Wen Ding, Jianzheng Zhu, Ziyou Lin, Lin Zhong, Junjian Wang, Peibin Yue, James Turkson, Peiqing Liu, Yuanxiang Wang, Xiaolei Zhang
Summary: Inhibition of STAT3 can trigger ferroptosis and provide a new therapeutic strategy for gastric cancer and chemotherapy resistance. STAT3 negatively regulates the FNR associated genes and establishes a negative STAT3-ferroptosis regulatory axis in gastric cancer. A selective STAT3 inhibitor, W1131, shows significant anti-tumor effects in gastric cancer models by inducing ferroptosis and restores sensitivity to chemotherapy.
Article
Chemistry, Multidisciplinary
Jia-Luo Huang, Xue-Long Yan, Wei Li, Run-Zhu Fan, Shen Li, Jianghe Chen, Zhenhua Zhang, Jun Sang, Lu Gan, Gui-Hua Tang, Hongwu Chen, Junjian Wang, Sheng Yin
Summary: This study identified a highly potent importin-beta 1 inhibitor DD1, which selectively inhibited the growth and survival of CRPC cells and completely blocked tumor growth. Mechanistic studies showed that DD1 reduced the nuclear accumulation of key CRPC drivers, shutting down their downstream oncogenic signaling. These findings suggest that importin-beta 1 is an effective therapeutic target in CRPC and DD1 can be developed as a potential treatment for this disease.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2022)
Article
Biochemistry & Molecular Biology
Zhibo Hu, Junjie Chen, Qianqian Liu, Qilin Wu, Shenhua Chen, Junjian Wang, Jing Li, Lan Liu, Zhizeng Gao
Summary: One new cyclohexenone derivative (1) and two undescribed drimane sesquiterpenes (2 and 3), along with seven known drimane sesquiterpenes, were isolated from a seagrass-derived fungus Aspergillus insuetus SYSU6925. The structures of these metabolites were determined through comprehensive spectroscopic analysis. Compounds 1-3, 5, and 7 exhibited weak to moderate antifungal activities against four phytopathogenic fungi, with MIC values ranging from 50 to 200 mu g/mL. Compound 1, a rare cyclohexenone derivative with an n-propyl group, showed more potent inhibitory activities (MIC, 50 mu g/mL) against F. oxysporum compared to the positive control (Triadimefon). Compounds 2 and 3 also demonstrated potent anti-inflammatory activities by inhibiting nitric oxide (NO) production in RAW264.7 cells with IC50 values of 21.5 +/- 1.1 and 32.6 +/- 1.16 mu M, respectively.
CHEMISTRY & BIODIVERSITY
(2023)
Article
Chemistry, Medicinal
Zongbo Feng, Chunju Yang, Yi Zhang, Huaxuan Li, Wei Fang, Junhua Wang, Yichu Nie, Chang-Yun Wang, Zhiqing Liu, Zhimin Jiang, Junjian Wang, Yuanxiang Wang
Summary: Protein lysine methyltransferases G9a and GLP are important in cellular processes. A covalent inhibitor, compound 27, has been discovered to effectively inhibit cell proliferation and reduce H3K9me2 levels. It also shows significant antitumor efficacy in vivo.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Multidisciplinary Sciences
Lu Han, Zhiteng Luo, Yingchen Ju, Bingyi Chen, Taotao Zou, Junjian Wang, Jun Xu, Qiong Gu, Xiang-Lei Yang, Paul Schimmel, Huihao Zhou
Summary: Aminoacyl-transfer RNA (tRNA) synthetases (aaRSs) are essential enzymes in protein translation, categorized into two classes with distinct active site architectures. The orphan GlyRS in bacteria has a unique X-shaped structure. A cocrystal structure elucidates how this orphan GlyRS specifically recognizes its substrate tRNA. The X shape of orphan GlyRS suggests potential nonactive site targets for aaRS-directed antibiotics.
Article
Biochemistry & Molecular Biology
Shuai Ma, Yiwei Hu, Jianjiao Chen, Xiaojuan Wang, Chenxi Zhang, Qianqian Liu, Guodi Cai, Hong Wang, Jianwei Zheng, Qianqian Wang, Lin Zhong, Bin Yang, Shengning Zhou, Yonghong Liu, Fanghai Han, Junjian Wang, Junfeng Wang
Summary: A novel compound named arthpyrone M (Art-M) derived from marine fungus Arthrinium arundinis showed potential antitumor activity against gastric cancer (GC) by inhibiting cell proliferation, invasion, and migration. The mechanism was found to be through suppressing the mTORC1 pathway. Additionally, Art-M enhanced the sensitivity of GC cells to apatinib and showed better efficacy when used in combination.
CHEMICO-BIOLOGICAL INTERACTIONS
(2023)
Article
Immunology
Qin Yang, Zhenhua Zhang, Ziye Chen, Yiyuan Wang, Yan Chen, Jiehuang Zheng, Ruopeng Li, Lihong Li, Lixia Mo, Qinghe Liang, Fengsheng Chen, Junjian Wang, Xiaojuan Li
Summary: The study reveals that Flot2 gene expression is significantly reduced in B cells from patients with bacterial sepsis and endotoxin-induced septic mice. Flot2 deficiency aggravates sepsis by facilitating effector B cells rather than regulatory B cells, leading to increased inflammation and lung injury. These findings highlight the importance of Flot2 as a novel controller of B cells in the pathogenesis and progression of sepsis.
Article
Biochemistry & Molecular Biology
Yiwei Hu, Shuai Ma, Xiaoyan Pang, Mengjing Cong, Qianqian Liu, Fanghai Han, Junjian Wang, Weineng Feng, Yonghong Liu, Junfeng Wang
Summary: Small cell lung cancer (SCLC) is a high-grade neuroendocrine carcinoma that has a higher proliferative rate, earlier metastasis, and poorer outcomes compared to non-small cell lung cancer (NSCLC). Through molecular networking, new pyridone alkaloids were discovered and evaluated for their cytotoxicity against cancer cell lines. One of the alkaloids, arthpyrone O showed potent efficacy against SCLC cells in vitro and inhibited tumor growth in vivo, suggesting its potential as a drug discovery scaffold.
Article
Pharmacology & Pharmacy
Jia-Luo Huang, Xue-Long Yan, Dong Huang, Lu Gan, Huahua Gao, Run-Zhu Fan, Shen Li, Fang-Yu Yuan, Xinying Zhu, Gui-Hua Tang, Hong-Wu Chen, Junjian Wang, Sheng Yin
Summary: The study optimized a natural importin-beta 1 inhibitor DD1 to improve its tolerability and oral bioavailability, resulting in an analog called DD1-Br. DD1-Br exhibited potent inhibition of survival in castration-resistant prostate cancer cells and effectively prevented tumor growth in resistant CRPC models. Mechanistic study revealed that DD1-Br targeted importin-beta 1 and suppressed the nuclear accumulation of key CRPC drivers, including AR-V7, thereby inhibiting oncogenic signaling.
ACTA PHARMACEUTICA SINICA B
(2023)
