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2-methoxyestradiol

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https://www.readbyqxmd.com/read/29772242/synthesis-molecular-modeling-and-biological-evaluation-of-potent-analogs-of-2-methoxyestradiol
#1
Nora Al-Kazaale, Phuong T Tran, Farhad Haidari, Eirik Johansson Solum, Sandra Liekens, Peter Vervaeke, Ingebrigt Sylte, Jing-Jy Cheng, Anders Vik, Trond Vidar Hansen
The endogenous steroid 2-methoxyestradiol (1) has attracted a great interest as a lead compound towards the development of new anti-cancer drugs. Herein, the synthesis, molecular modeling, anti-proliferative and anti-angiogenic effects of ten 2-ethyl and four 2-methoxy analogs of estradiol are reported. The ethyl group was introduced to the steroid A-ring using a novel Friedel-Crafts alkylation protocol. Several analogs displayed potent anti-proliferative activity with IC50 -values in the submicromolar range towards the CEM human leukemia cancer cell line...
May 14, 2018: Steroids
https://www.readbyqxmd.com/read/29679638/inhibition-of-immunoproteasome-promotes-angiogenesis-via-enhancing-hypoxia-inducible-factor-1%C3%AE-abundance-in-rats-following-focal-cerebral-ischaemia
#2
Xingyong Chen, Xu Zhang, Ting Chen, Xiulong Jiang, Xiaosong Wang, Huixin Lei, Yinzhou Wang
Angiogenesis after ischemic stroke contributes to the restoration of blood supply in the ischemic zone. Strategies to improve angiogenesis may facilitate the function recovery after stroke. Growing evidence shows that proteasome inhibitors enhance angioneurogenesis and induces a long-term neuroprotection after cerebral ischemia in rodents' models. We have previously reported that inhibition of the immunoproteasome subunit low molecular mass peptide 2 (LMP2) offers a strong neuroprotection in ischemic stroke rats...
April 18, 2018: Brain, Behavior, and Immunity
https://www.readbyqxmd.com/read/29672318/a-novel-2-methoxyestradiol-analogue-is-responsible-for-vesicle-disruption-and-lysosome-aggregation-in-breast-cancer-cells
#3
Sandra D Nkandeu, Iman van den Bout, Marianne J Cronjé, Dirk H van Papendorp, Anna M Joubert
BACKGROUND: 2-Methoxyestradiol (2ME2) is an endogenous metabolite of 17-β-estradiol with anti-proliferative and anti-angiogenic properties. Due to 2ME2's rapid metabolism and low oral bioavailability in in vivo settings, 2ME2 analogues have been designed to alleviate these issues. One of these compounds is 2-ethyl-3-O-sulphamoyl-estra-1,3,5(10)16-tetraene (ESE-16). A previous work alluded to the ability of ESE-16 to induce autophagic cell death. Therefore, we investigated the mode of action of ESE-16 by studying its effects on autophagy, vesicle formation, and lysosomal organisation...
April 19, 2018: Pharmacology
https://www.readbyqxmd.com/read/29606130/proteasome-inhibitors-modulate-anticancer-and-anti-proliferative-properties-via-nf-kb-signaling-and-ubiquitin-proteasome-pathways-in-cancer-cell-lines-of-different-organs
#4
Asaf A Qureshi, Eleanor G Zuvanich, Dilshad A Khan, Shahida Mushtaq, Neerupma Silswal, Nilofer Qureshi
BACKGROUND: Cancer is second most common cause of death in the United State. There are over 100 different types of cancer associated with different human organs, predominantly breast, liver, pancreas, prostate, colon, rectum, lung, and stomach. We have recently reported properties of pro-inflammatory (for treatment of various types of cancers), and anti-inflammatory (for cardiovascular disease and diabetes) compounds. The major problem associated with development of anticancer drugs is their lack of solubility in aqueous solutions and severe side effects in cancer patients...
April 2, 2018: Lipids in Health and Disease
https://www.readbyqxmd.com/read/29568313/the-in-vitro-effects-of-a-novel-estradiol-analog-on-cell-proliferation-and-morphology-in-human-epithelial-cervical-carcinoma
#5
Laura Susan Boyd, Devrim Gozuacik, Anna Margaretha Joubert
Background: The majority of novel chemotherapeutics target the cell cycle, aiming to effect arrest and cause apoptosis. One such agent, 2-methoxyestradiol (2ME), has been shown to possess anticancer properties against numerous cancer types, both in vitro and in vivo. Despite its promise, 2ME has exhibited limitations, including low oral bioavailability and rapid hepatic enzymatic inactivation in vivo. A novel sulphamoylated estrogen analog, 2-ethyl-3- O -sulphamoyl-estra-1,3,5(10)16-tetraene (ESE-16), was in silico-designed in our laboratory to overcome these issues...
2018: Cellular & Molecular Biology Letters
https://www.readbyqxmd.com/read/29566125/the-roles-of-id-1-in-human-pancreatic-ductal-adenocarcinoma-and-the-therapeutic-effects-of-2-methoxyestradiol
#6
Lie Yao, Xiang Zou, Chen Jin, Jie Fan, Zhongyi Guo, Quanjun Lin, Ji Li, Deliang Fu
Pancreatic ductal adenocarcinoma (PDAC) has poor prognosis and high mortality rate. Inhibitor of differentiation-1 (ID-1) overexpression has already been reported to be associated with low survival, but the detailed roles of ID-1 in PDAC are unclear. As an ID-1 inhibitor, 2-methoxyestradiol (2-ME) has been shown effective in the anti-tumor therapies, but its effect on PDAC is unknown. In this study, ID-1 overexpression and knockdown stable SW1990 cells were used to examine proliferation, migration and invasion abilities...
March 16, 2018: Carcinogenesis
https://www.readbyqxmd.com/read/29523268/the-reduction-in-circulating-levels-of-estrogen-and-progesterone-in-women-with-preeclampsia
#7
Jiayi Wan, Zheng Hu, Ke Zeng, Yongxiang Yin, Min Zhao, Miaoxin Chen, Qi Chen
Abnormalities in the development of placental vasculature in early pregnancy and the failure of transformation of the spiral arteries are associated with the pathogenesis of preeclampsia. Sex hormones influence neovascularisation during pregnancy. However the profiling of estrogen and progesterone in preeclampsia is controversial. In this study we investigated the serum levels of estrogen and progesterone in women with preeclampsia. Blood samples were collected from 86 preeclamptic and 97 gestation-matched normotensive pregnancies...
January 2018: Pregnancy Hypertension
https://www.readbyqxmd.com/read/29477834/enriched-housing-promotes-post-stroke-neurogenesis-through-calpain-1-stat3-hif-1%C3%AE-vegf-signaling
#8
Xiaoying Wu, Shengqun Liu, Zhenhua Hu, Guosong Zhu, Gaifang Zheng, Guangzhi Wang
Enriched environment (EE) has been shown to promote neurogenesis and functional recovery after ischemic stroke. However, the underlying molecular mechanisms are not fully understood. In this study, C57BL/6 mice underwent middle cerebral artery occlusion (60 min) followed by reperfusion, after which mice were housed in either standard environment (SE) or EE and allowed to survive for 3, 4, 6 or 10 weeks. Ipsilateral subventricular zone (SVZ) or striatum cells were dissociated from ischemic hemispheric brains of enriched mice at 14 days post-ischemia (dpi) and cultured in vitro...
February 26, 2018: Brain Research Bulletin
https://www.readbyqxmd.com/read/29426916/2-methoxyestradiol-protects-against-pressure-overload-induced-left-ventricular-hypertrophy
#9
Zaid H Maayah, Jody Levasseur, Ramanaguru Siva Piragasam, Ghada Abdelhamid, Jason R B Dyck, Richard P Fahlman, Arno G Siraki, Ayman O S El-Kadi
Numerous experimental studies have supported the evidence that 2-methoxyestradiol (2 ME) is a biologically active metabolite that mediates multiple effects on the cardiovascular system, largely independent of the estrogen receptor. 2 ME is a major cytochrome P450 1B1 (CYP1B1) metabolite and has been reported to have vasoprotective and anti-inflammatory actions. However, whether 2 ME would prevent cardiac hypertrophy induced by abdominal aortic constriction (AAC) has not been investigated yet. Therefore, the overall objectives of the present study were to elucidate the potential antihypertrophic effect of 2 ME and explore the mechanism(s) involved...
February 9, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29405079/differential-effects-of-some-novel-synthetic-oestrogen-analogs-on-oxidative-pc12-cell-death-caused-by-serum-deprivation
#10
Irene B Sørvik, Eirik Johansson Solum, Nils A Labba, Trond Vidar Hansen, Ragnhild E Paulsen
Oestrogens with no or reduced oestrogen receptor (ER) binding properties are reported to have neuroprotective functions. However, we have previously shown that the hormonally inactive isomer of 17β-estradiol (17β-E), 17α-estradiol (17α-E), down-regulates glutathione (GSH) synthesis, and fails to rescue serum deprivation-induced cell death in the rat pheochromocytoma cell line PC12 in micromolar concentration. The present study examined cellular protective effects of new 17β-E analogs and 2-methoxyestradiol (2-ME) analogs with no or little oestrogen activity...
February 2018: Free Radical Research
https://www.readbyqxmd.com/read/29365274/2-methoxyestradiol-causes-mmp-9-mediated-transactivation-of-egfr-and-angiotensin-type-1-receptor-downregulation-in-rat-aortic-smooth-muscle-cells
#11
Benard Ogola, Yong Zhang, Laxmi Iyer, Thomas Thekkumkara
Studies have demonstrated the therapeutic potential of estrogen metabolite 2-Methoxyestradiol (2ME2) in several cardiovascular disorders, including hypertension. However, the exact mechanism(s) remains unknown. In this study, primary rat aortic smooth muscle cells (RASMCs) were exposed to 2ME2 and angiotensin type 1 receptor (AT1R) expression, function and associated signaling pathways were evaluated. 2ME2 downregulated AT1R expression in a concentration and time-dependent manner, which was correlated with reduced mRNA expression...
January 24, 2018: American Journal of Physiology. Cell Physiology
https://www.readbyqxmd.com/read/29287795/hif-1%C3%AE-l-pgds-ppar%C3%AE-regulates-hypoxia-induced-anp-secretion-in-beating-rat-atria
#12
Xiang Li, Ying Zhang, Bo Zhang, Xia Liu, Lan Hong, Li-Ping Liu, Cheng-Zhe Wu, Xun Cui
Lipocalin-type prostaglandin D synthase (L-PGDS) and peroxisome proliferator activated receptor γ (PPARγ) play important roles in cardiovascular diseases. Nevertheless, effects of hypoxia-inducible factor 1α (HIF-1α) on L-PGDS and PPARγ protein levels and its role in hypoxia-induced atrial natriuretic peptide (ANP) secretion are unclear. In perfused beating rat atria, we observed that hypoxia significantly increased HIF-1α protein levels and stimulated ANP secretion, while upregulating L-PGDS. Hypoxia-induced ANP secretion was clearly attenuated by HIF-1α antagonist 2-methoxyestradiol, downregulating both HIF-1α and L-PGDS protein levels...
January 2018: Prostaglandins & Other Lipid Mediators
https://www.readbyqxmd.com/read/29275365/2-methoxyestradiol-affects-mitochondrial-biogenesis-pathway-and-succinate-dehydrogenase-complex-flavoprotein-subunit-a-in-osteosarcoma-cancer-cells
#13
Magdalena Gorska-Ponikowska, Alicja Kuban-Jankowska, Stephan A Eisler, Ugo Perricone, Giosuè Lo Bosco, Giampaolo Barone, Stephan Nussberger
BACKGROUND/AIM: Dysregulation of mitochondrial pathways is implicated in several diseases, including cancer. Notably, mitochondrial respiration and mitochondrial biogenesis are favored in some invasive cancer cells, such as osteosarcoma. Hence, the aim of the current work was to investigate the effects of 2-methoxyestradiol (2-ME), a potent anticancer agent, on the mitochondrial biogenesis of osteosarcoma cells. MATERIALS AND METHODS: Highly metastatic osteosarcoma 143B cells were treated with 2-ME separately or in combination with L-lactate, or with the solvent (non-treated control cells)...
January 2018: Cancer Genomics & Proteomics
https://www.readbyqxmd.com/read/29242064/hypoxia-inducible-factor-1-in-clinical-and-experimental-aortic-aneurysm-disease
#14
Wei Wang, Baohui Xu, Haojun Xuan, Yingbin Ge, Yan Wang, Lixin Wang, Jianhua Huang, Weiguo Fu, Sara A Michie, Ronald L Dalman
OBJECTIVE: Mural angiogenesis and macrophage accumulation are two pathologic hallmarks of abdominal aortic aneurysm (AAA) disease. The heterodimeric transcription factor hypoxia-inducible factor 1 (HIF-1) is an essential regulator of angiogenesis and macrophage function. In this study, we investigated HIF-1 expression and activity in clinical and experimental AAA disease. METHODS: Human aortic samples were obtained from 24 AAA patients and six organ donors during open abdominal surgery...
December 11, 2017: Journal of Vascular Surgery
https://www.readbyqxmd.com/read/29227648/quinazolinone-based-anticancer-agents-synthesis-antiproliferative-sar-antitubulin-activity-and-tubulin-co-crystal-structure
#15
Wolfgang Dohle, Fabrice L Jourdan, Grégory Menchon, Andrea E Prota, Paul A Foster, Pascoe Mannion, Ernest Hamel, Mark P Thomas, Philip G Kasprzyk, Eric Ferrandis, Michel O Steinmetz, Mathew P Leese, Barry V L Potter
Quinazolinone-based anticancer agents were designed, decorated with functional groups from a 2-methoxyestradiol-based microtubule disruptor series, incorporating the aryl sulfamate motif of steroid sulfatase (STS) inhibitors. The steroidal AB-ring system was mimicked, favoring conformations with an N-2 substituent occupying D-ring space. Evaluation against breast and prostate tumor cell lines identified 7b with DU-145 antiproliferative activity (GI50 300 nM). A preliminary structure-activity relationship afforded compounds (e...
February 8, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29200966/microencapsulation-of-low-passage-poorly-differentiated-human-mucoepidermoid-carcinoma-cells-by-alginate-microcapsules-in-vitro-profiling-of-angiogenesis-related-molecules
#16
Sen Yang, Li-Juan Guo
Background: Human mucoepidermoid carcinoma (MEC) is regarded as the most common primary salivary malignancy. High-grade MEC has a high risk of recurrence and poor prognosis. Tumor angiogenesis, induced by poorly differentiated cancer cells of high-grade MEC, contributes to tumor growth and metastasis. Therefore, elucidating molecular mechanisms underlying the pro-angiogenic ability of poorly differentiated MEC cells is critical for the understanding of high-grade MEC progression. It is well known that three-dimensional (3D) cell culture, in contrast with conventional two-dimensional (2D) culture, provides a better approach to in vitro recapitulation of in vivo characteristics of cancer cells and their surrounding microenvironment...
2017: Cancer Cell International
https://www.readbyqxmd.com/read/29193609/endogenous-hormone-2-methoxyestradiol-suppresses-venous-hypertension-induced-angiogenesis-through-up-and-down-regulating-p53-and-id-1
#17
Xiang Zou, Li Zhang, Jie Yuan, Chunjie Yang, Zehan Wu, Jianping Song, Wei Zhu, Ying Mao, Liang Chen
Brain arteriovenous malformations (AVMs) which associate with angiogenesis due to local hypertension, chronic cerebral ischaemia and tissue hypoxia usually lead to haemorrhage, however, the therapeutic medicine for the disease is still lacking. 2-methoxyestradiol (2-ME) has been shown effective in the anti-angiogenic treatment. This study was conducted to examine whether and how 2-ME could improve the vascular malformations. Intracranial venous hypertension (VH) model produced in adult male Sprague-Dawley rats and culture of human umbilical vein endothelial cells (HUVECs) at the anoxia condition were used to induce in vivo and in vitro angiogenesis, respectively...
February 2018: Journal of Cellular and Molecular Medicine
https://www.readbyqxmd.com/read/29110580/clinical-significance-of-low-2-methoxyestradiol-levels-in-serum-and-tissue-of-recurrent-juvenile-onset-laryngeal-papillomatosis
#18
Danling Liu, Jiadong Wang, Yanan Xu
Objective We aim to explore the correlation between serum and tissue 2-methoxyestradiol (2-ME-2) levels and recurrence of juvenile-onset respiratory papillomatosis (JORRP). Study Design Retrospective cohort studies. Settings Laboratory of Otolaryngology, Department of Head and Neck Surgery, Renji Hospital, School of Medicine, Shanghai Jiaotong University. Subjects and Methods Sixty-four patients diagnosed with JORRP in our department from January 2007 to December 2012 were enrolled. Patients were divided into recurrence and nonrecurrence groups, with 32 patients in each group...
March 2018: Otolaryngology—Head and Neck Surgery
https://www.readbyqxmd.com/read/29109098/2-methoxyestradiol-reverses-the-pro-carcinogenic-effect-of-l-lactate-in-osteosarcoma-143b-cells
#19
REVIEW
Magdalena Gorska-Ponikowska, Alicja Kuban-Jankowska, Agnieszka Daca, Stephan Nussberger
BACKGROUND/AIM: According to the reverse Warburg effect, tumor cells may metabolize lactate as an energy source and shuttle L-lactate to neighboring cancer cells, adjacent stroma, and vascular endothelial cells, thus inducing metabolic reprogramming. An increased tumor L-lactate level strictly correlates with increased metastasis, tumor recurrence and a poor outcome. A potent anticancer agent that may act on L-lactate activated cells is 2-metoxyestradiol. Thus, the aim of the study was to evaluate whether a potent anticancer agent, 2-methoxyestradiol, is able to reverse L-lactate-induced metabolic reprogramming in osteosarcoma 143B cells...
November 2017: Cancer Genomics & Proteomics
https://www.readbyqxmd.com/read/29054710/novel-p-carborane-containing-multitarget-anticancer-agents-inspired-by-the-metabolism-of-17%C3%AE-estradiol
#20
Asako Kaise, Kiminori Ohta, Yasuyuki Endo
The female hormone 17 β-estradiol (E2) is synthesized from estrone by steroid sulfatase (STS), and metabolized into 2-methoxyestradiol (2-ME), whereby the biological activity of the latter is substantially different from that of E2. Based on the metabolic pathways of E2, a carborane-containing 2-ME mimic (1c) and its derivatives (1 and 2) were designed and synthesized as novel multitarget anticancer agents. Bissulfamate 1f exhibited potent STS-inhibitory activity and tubulin-polymerization-inhibitory activity...
December 15, 2017: Bioorganic & Medicinal Chemistry
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