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Hif inhibitor

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https://www.readbyqxmd.com/read/28720379/inhibition-of-12-15-lox-ameliorates-cognitive-and-cholinergic-dysfunction-in-mouse-model-of-hypobaric-hypoxia-via-attenuation-of-oxidative-nitrosative-stress
#1
Richa Choudhary, Udayabanu Malairaman, Anju Katyal
12/15 Lipoxygenase has recently been described as potent propagator of oxidative stress and is closely associated with cognitive decline in neurodegenerative diseases. The mechanism/s behind 12/15 LOX involvement in cognitive deficits remain obscure. The current study has been designed to investigate the underlying role of 12/15LOX and effect of 12/15 LOX inhibition on hypobaric hypoxia induced memory impairment and cholinergic deficits. Male Balb/c mice subjected to simulated hypobaric hypoxia/reoxygenation condition for 3 days showed marked working memory impairment concomitant with hippocampal neuronal damage and malondialdehyde production which were significantly attenuated by baicalein, a specific inhibitor of 12/15LOX...
July 15, 2017: Neuroscience
https://www.readbyqxmd.com/read/28712399/-expressions-of-stem-cell-factor-and-hypoxia-inducible-factor-1-alpha-in-pancreatic-cancer-cells-and-related-mechanism
#2
Min Zhang, Yunjian Wang, Qiong Li, Qingjun Li, Nanmu Yang, Guohua You, Li Wang
Objective To study the correlation between the expressions of stem cell factor (SCF) and hypoxia inducible factor 1 alpha (HIF-1α) in pancreatic cancer, and investigate the mechanism by which SCF regulates the expression of HIF-1α. Methods Immunohistochemistry was used to detect the expressions of SCF and HIF-1α in pancreatic cancer specimens and to analyze the correlation between SCF and HIF-1α expressions. Pancreatic cancer PANC-1 cells were treated with different doses of SCF (0, 1, 10, 100 ng/mL) alone or combined with c-KIT inhibitor Gleevec (5 μmol/L)...
July 2017: Xi Bao Yu Fen Zi Mian Yi Xue za Zhi, Chinese Journal of Cellular and Molecular Immunology
https://www.readbyqxmd.com/read/28711911/human-steroid-sulfatase-induces-wnt-%C3%AE-catenin-signaling-and-epithelial-mesenchymal-transition-by-upregulating-twist1-and-hif-1%C3%AE-in-human-prostate-and-cervical-cancer-cells
#3
Sangyun Shin, Hee-Jung Im, Yeo-Jung Kwon, Dong-Jin Ye, Hyoung-Seok Baek, Donghak Kim, Hyung-Kyoon Choi, Young-Jin Chun
Steroid sulfatase (STS) catalyzes the hydrolysis of estrone sulfate and dehydroepiandrosterone sulfate (DHEAS) to their unconjugated biologically active forms. Although STS is considered a therapeutic target for estrogen-dependent diseases, the cellular functions of STS remain unclear. We found that STS induces Wnt/β-catenin s Delete ignaling in PC-3 and HeLa cells. STS increases levels of β-catenin, phospho-β-catenin, and phospho-GSK3β. Enhanced translocation of β-catenin to the nucleus by STS might activate transcription of target genes such as cyclin D1, c-myc, and MMP-7...
June 27, 2017: Oncotarget
https://www.readbyqxmd.com/read/28708594/hypoxia-favors-myosin-heavy-chain-beta-gene-expression-in-an-hif-1alpha-dependent-manner
#4
Lucia Binó, Jiřina Procházková, Katarzyna Anna Radaszkiewicz, Jan Kučera, Jana Kudová, Jiří Pacherník, Lukáš Kubala
The potentiation of the naturally limited regenerative capacity of the heart is dependent on an understanding of the mechanisms that are activated in response to pathological conditions such as hypoxia. Under these conditions, the expression of genes suggested to support cardiomyocyte survival and heart adaptation is triggered. Particularly important are changes in the expression of myosin heavy chain (MHC) isoforms. We propose here that alterations in the expression profiles of MHC genes are induced in response to hypoxia and are primarily mediated by hypoxia inducible factor (HIF)...
July 5, 2017: Oncotarget
https://www.readbyqxmd.com/read/28701475/hif-activation-causes-synthetic-lethality-between-the-vhl-tumor-suppressor-and-the-ezh1-histone-methyltransferase
#5
Abhishek A Chakraborty, Eijiro Nakamura, Jun Qi, Amanda Creech, Jacob D Jaffe, Joshiawa Paulk, Jesse S Novak, Kshithija Nagulapalli, Samuel K McBrayer, Glenn S Cowley, Javier Pineda, Jiaxi Song, Yaoyu E Wang, Steven A Carr, David E Root, Sabina Signoretti, James E Bradner, William G Kaelin
Inactivation of the von Hippel-Lindau tumor suppressor protein (pVHL) is the signature lesion in the most common form of kidney cancer, clear cell renal cell carcinoma (ccRCC). pVHL loss causes the transcriptional activation of hypoxia-inducible factor (HIF) target genes, including many genes that encode histone lysine demethylases. Moreover, chromatin regulators are frequently mutated in this disease. We found that ccRCC displays increased H3K27 acetylation and a shift toward mono- or unmethylated H3K27 caused by an HIF-dependent increase in H3K27 demethylase activity...
July 12, 2017: Science Translational Medicine
https://www.readbyqxmd.com/read/28697748/endothelial-progenitor-cells-transplantation-attenuated-blood-brain-barrier-damage-after-ischemia-in-diabetic-mice-via-hif-1%C3%AE
#6
Jieli Geng, Liping Wang, Meijie Qu, Yaying Song, Xiaojie Lin, Yajing Chen, Muyassar Mamtilahun, Shengdi Chen, Zhijun Zhang, Yongting Wang, Guo-Yuan Yang
BACKGROUND: Blood-brain barrier impairment is a major indicator of endothelial dysfunction in diabetes. Studies showed that endothelial progenitor cell (EPC) transplantation promoted angiogenesis and improved function recovery after hind limb ischemia in diabetic mice. The effect of EPC transplantation on blood-brain barrier integrity after cerebral ischemia in diabetic animals is unknown. The aim of this study is to explore the effect of EPC transplantation on the integrity of the blood-brain barrier after cerebral ischemia in diabetic mice...
July 11, 2017: Stem Cell Research & Therapy
https://www.readbyqxmd.com/read/28693255/sodium-butyrate-enhances-the-growth-inhibitory-effect-of-sunitinib-in-human-renal-cell-carcinoma-cells
#7
Hiromi Sato, Miaki Uzu, Tatsuro Kashiba, Rina Suzuki, Takuya Fujiwara, Hiroko Okuzawa, Koichi Ueno
Sunitinib (SU) is a small molecule that inhibits the receptor tyrosine kinase (RTK) signaling pathway, and has been clinically used to treat advanced renal cell carcinoma (RCC). However, SU is not always effective as RCC is a highly chemoresistant type of cancer. One of the factors that confer chemoresistance to RCC is a hypoxic condition. Lack of oxygen activates hypoxia-inducible factor (HIF) protein, which is followed by the upregulation of growth factors, including vascular endothelial growth factor and activation of the RTK signaling pathway...
July 2017: Oncology Letters
https://www.readbyqxmd.com/read/28689812/ibmx-protects-human-proximal-tubular-epithelial-cells-from-hypoxic-stress-through-suppressing-hypoxia-inducible-factor-1%C3%AE-expression
#8
Arif Ul Hasan, Wararat Kittikulsuth, Fuminori Yamaguchi, Tuba Musarrat Ansary, Asadur Rahman, Yuki Shibayama, Daisuke Nakano, Hirofumi Hitomi, Masaaki Tokuda, Akira Nishiyama
Hypoxia predisposes renal fibrosis. This study was conducted to identify novel approaches to ameliorate the pathogenic effect of hypoxia. Using human proximal tubular epithelial cells we showed that a pan-phosphodiesterase (PDE) inhibitor, 3-isobutyl-1-methylxanthine (IBMX) dose and time dependently downregulated hypoxia-inducible factor 1α (HIF-1α) mRNA expression, which was further augmented by addition of a transcriptional inhibitor, actinomycin D. IBMX also increased the cellular cyclic adenosine monophosphate (cAMP) level...
July 6, 2017: Experimental Cell Research
https://www.readbyqxmd.com/read/28689235/qsar-modeling-and-in-silico-design-of-small-molecule-inhibitors-targeting-the-interaction-between-e3-ligase-vhl-and-hif-1-formula-see-text
#9
Jing Pan, Yanmin Zhang, Ting Ran, Anyang Xu, Xin Qiao, Lingfeng Yin, Weineng Zhou, Lu Zhu, Junnan Zhao, Tao Lu, Yadong Chen, Yulei Jiang
Protein-protein interactions (PPIs) have attracted much attention recently because of their preponderant role in most biological processes. The prevention of the interaction between E3 ligase VHL and HIF-1[Formula: see text] may improve tolerance to hypoxia and ameliorate the prognosis of many diseases. To obtain novel potent inhibitors of VHL/HIF-1[Formula: see text] interaction, a series of hydroxyproline-based inhibitors were investigated for structural optimization using a combination of QSAR modeling and molecular docking...
July 8, 2017: Molecular Diversity
https://www.readbyqxmd.com/read/28686797/asiatic-acid-enhances-survival-of-human-ac16-cardiomyocytes-under-hypoxia-by-upregulating-mir-1290
#10
Kai Wu, Min Hu, Zejin Chen, Feixiang Xiang, Guojian Chen, Weihong Yan, Qing Peng, Xiaoping Chen
Asiatic acid (AA) could attenuate ischemia/reperfusion induced myocardial apoptosis through upregulating the Akt/GSK-3β/HIF-1α pathway. HIF-3α is a negative regulator of HIF-1α, whose mRNA is a potential target of miR-1290. AA could upregulate miR-1290 in non-small-cell lung cancer A549 cells. This work aimed to investigate whether AA could inhibit hypoxia induced cardiomyocyte apoptosis through regulating the miR-1290/HIF3A/HIF-1α axis. The AC16 human myocardial cell line cultured under normoxic or hypoxic conditions was treated with various doses of AA for 24 h...
July 7, 2017: IUBMB Life
https://www.readbyqxmd.com/read/28684234/roflumilast-treatment-inhibits-lung-carcinogenesis-in-benzo-a-pyrene-induced-murine-lung-cancer-model
#11
Chang Dong Yeo, Young Ae Kim, Hwa Young Lee, Jin Woo Kim, Seung Joon Kim, Sang Haak Lee, Young Kyoon Kim
Roflumilast, a potent and selective inhibitor of phosphodiesterase-4 (PDE4), has been used in treatment of COPD. PDE4 inhibitor is associated with inhibition of chronic airway inflammation, oxidative stress, and mesenchymal markers in B(a)P-induced lung tumors. The aim of this study was to assess whether roflumilast alone or added to inhaled budesonide might have dose-dependent inhibition on lung carcinogenesis induced by carcinogen B(a)P in mice. Female A/J mice were given a single dose of benzo(a)pyrene. Administration of roflumilast (1mg/kg or 5mg/kg) via oral gavage and aerosolized budesonide (2...
July 3, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28667082/new-hif2a-inhibitors-implications-for-pheochromocytomas-and-paragangliomas
#12
Rodrigo Almeida Toledo
Two recent independent studies published in Nature show robust responses of clear cell renal cell carcinoma (ccRCC) cell lines, preclinical ccRCC xenograft models and, remarkably, a patient with progressive ccRCC despite receiving multiple lines of treatment, to the long-awaited, recently developed inhibitors of hypoxia-inducible factor 2-alpha (HIF2α). This Commentary is based on the recognition of similar molecular drivers in ccRCC and the endocrine neoplasias pheochromocytomas and paragangliomas (PPGLs), ultimately leading to stabilization of HIFs...
June 30, 2017: Endocrine-related Cancer
https://www.readbyqxmd.com/read/28666461/glyceollins-trigger-anti-proliferative-effects-through-estradiol-dependent-and-independent-pathways-in-breast-cancer-cells
#13
Sylvain Lecomte, Frederic Chalmel, François Ferriere, Frederic Percevault, Nicolas Plu, Christian Saligaut, Claire Surel, Marie Lelong, Theo Efstathiou, Farzad Pakdel
BACKGROUND: Estrogen receptors (ER) α and β are found in both women and men in many tissues, where they have different functions, including having roles in cell proliferation and differentiation of the reproductive tract. In addition to estradiol (E2), a natural hormone, numerous compounds are able to bind ERs and modulate their activities. Among these compounds, phytoestrogens such as isoflavones, which are found in plants, are promising therapeutics for several pathologies. Glyceollins are second metabolites of isoflavones that are mainly produced in soybean in response to an elicitor...
June 30, 2017: Cell Communication and Signaling: CCS
https://www.readbyqxmd.com/read/28666324/xiap-upregulates-expression-of-hif-target-genes-by-targeting-hif1%C3%AE-for-lys63-linked-polyubiquitination
#14
Catherine V Park, Iglika G Ivanova, Niall S Kenneth
The cellular response to hypoxia is characterised by a switch in the transcriptional program, mediated predominantly by the hypoxia inducible factor family of transcription factors (HIF). Regulation of HIF1 is primarily controlled by post-translational modification of the HIF1α subunit, which can alter its stability and/or activity. This study identifies an unanticipated role for the X-linked inhibitor of apoptosis (XIAP) protein as a regulator of Lys63-linked polyubiquitination of HIF1α. Lys63-linked ubiquitination of HIF1α by XIAP is dependent on the activity of E2 ubiquitin conjugating enzyme Ubc13...
June 28, 2017: Nucleic Acids Research
https://www.readbyqxmd.com/read/28666189/oral-metronomic-topotecan-sensitizes-crizotinib-antitumor-activity-in-alk-f1174l-drug-resistant-neuroblastoma-preclinical-models
#15
Libo Zhang, Bing Wu, Sylvain Baruchel
BACKGROUND: Anaplastic lymphoma kinase (ALK) inhibitor crizotinib has proven to be effective in the treatment of ALK-mutated neuroblastoma, but crizotinib resistance was commonly observed in patients. We aimed to overcome crizotinib resistance by combining with the MEK inhibitor trametinib or low-dose metronomic (LDM) topotecan in preclinical neuroblastoma models. METHODS: We selected a panel of neuroblastoma cell lines carrying various ALK genetic aberrations to assess the therapeutic efficacy on cell proliferation in vitro...
June 27, 2017: Translational Oncology
https://www.readbyqxmd.com/read/28659027/eclipta-prostrata-improves-dss-induced-colitis-through-regulation-of-inflammatory-response-in-intestinal-epithelial-cells
#16
Dae-Seung Kim, Sung-Hee Kim, Ji-Ye Kee, Yo-Han Han, JinBong Park, Jeong-Geon Mun, Moon-Jung Joo, Yong-Deok Jeon, Su-Jin Kim, Sang-Hyun Park, Sung-Joo Park, Jae-Young Um, Seung-Heon Hong
Eclipta prostrata (EP) and its compounds are known to have several pharmacological effects including anti-inflammatory effects. In the present study, we demonstrated that EP improves the dextran sulfate sodium (DSS)-induced colitis symptoms such as body weight loss, colon length shortening and disease activity index. In DSS-induced colitis tissue, EP controls the protein expressions of cyclooxygenase-2 (COX-2) and hypoxia inducible factor-1[Formula: see text] (HIF-1[Formula: see text]). In addition, the release of prostaglandin E2 and vascular endothelial growth factor-A were significantly reduced by EP administration...
June 28, 2017: American Journal of Chinese Medicine
https://www.readbyqxmd.com/read/28656316/apigenin-overcomes-drug-resistance-by-blocking-the-signal-transducer-and-activator-of-transcription-3-signaling-in-breast-cancer-cells
#17
Hye-Sook Seo, Jin Mo Ku, Hyeong Sim Choi, Jong-Kyu Woo, Byung Hoon Lee, Doh Sun Kim, Hyun Jong Song, Bo-Hyoung Jang, Yong Cheol Shin, Seong-Gyu Ko
Drug resistance in chemotherapy is a serious obstacle for the successful treatment of cancer. Drug resistance is caused by various factors, including the overexpression of P‑glycoprotein (P‑gp, MDR1). The development of new, useful compounds that overcome drug resistance is urgent. Apigenin, a dietary flavonoid, has been reported as an anticancer drug in vivo and in vitro. In the present study, we investigated whether apigenin is able to reverse drug resistance using adriamycin‑resistant breast cancer cells (MCF‑7/ADR)...
June 26, 2017: Oncology Reports
https://www.readbyqxmd.com/read/28651951/prolyl-hydroxylase-domain-inhibitors-as-a-novel-therapeutic-approach-against-anemia-in-chronic-kidney-disease
#18
Mai Sugahara, Tetsuhiro Tanaka, Masaomi Nangaku
Anemia is a common complication of chronic kidney disease and is mainly caused by the inability of injured kidneys to produce adequate amounts of erythropoietin. Studies elucidating the regulation of erythropoietin production led to the identification of hypoxia-inducible factor (HIF), which activates the transcription of genes that mediate adaptive responses to hypoxia. HIF is a heterodimer that consists of an α and β subunit. While HIF-β is constitutively expressed, HIF-α is subjected to ubiquitination and proteasomal degradation under normoxic conditions...
June 24, 2017: Kidney International
https://www.readbyqxmd.com/read/28651835/andrographolide-reduced-vegfa-expression-in-hepatoma-cancer-cells-by-inactivating-hif-1%C3%AE-the-involvement-of-jnk-and-mta1-hdca
#19
Liang Shi, Guoqing Zhang, Zhiyong Zheng, Bin Lu, Lili Ji
Andrographolide (Andro) is the main active compound in medicinal herb Andrographis paniculata Nees (Acanthaceae). Vascular endothelial growth factor A (VEGFA), a key pro-angiogenic factor, contributes greatly to tumor growth. The purpose of this study is to observe the inhibition of Andro on VEGFA expression in hepatoma cancer cells and its engaged mechanism. Andro decreased mRNA and protein expression of VEGFA in hepatoma Hep3B and HepG2 cells. Andro also decreased hypoxia-inducible factor 1-alpha (HIF-1α) protein expression and its subsequent nuclear translocation...
June 23, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28651420/-effects-of-hypoxia-inducible-factor-1%C3%AE-on-p311-and-its-influence-on-the-migration-of-murine-epidermal-stem-cells
#20
Z D Xu, H S Li, S Wang, W F He, J Wu, G X Luo
Objective: To explore the effects of hypoxia inducible factor-1α (HIF-1α) on P311 and its influence on the migration of murine epidermal stem cells (ESCs) under hypoxia in vitro. Methods: Two kinds of murine ESCs were isolated and obtained from 15 neonatal wild-type C57BL/6J mice and 5 congeneric source P311 gene knock-out mice, respectively. The first passage of cells were used in the following experiments after morphologic observation and detection of expression of cell surface markers CD71 and CD49f with flow cytometer...
May 20, 2017: Zhonghua Shao Shang za Zhi, Zhonghua Shaoshang Zazhi, Chinese Journal of Burns
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