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halofuginone

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https://www.readbyqxmd.com/read/28501621/discovery-of-a-novel-prolyl-trna-synthetase-inhibitor-and-elucidation-of-its-binding-mode-to-the-atp-site-in-complex-with-l-proline
#1
Ryutaro Adachi, Kengo Okada, Robert Skene, Kazumasa Ogawa, Masanori Miwa, Kazuhiro Tsuchinaga, Shoichi Ohkubo, Tsutomu Henta, Tomohiro Kawamoto
Prolyl-tRNA synthetase (PRS) is a member of the aminoacyl-tRNA synthetase family of enzymes and catalyzes the synthesis of prolyl-tRNA(Pro) using ATP, l-proline, and tRNA(Pro) as substrates. An ATP-dependent PRS inhibitor, halofuginone, was shown to suppress autoimmune responses, suggesting that the inhibition of PRS is a potential therapeutic approach for inflammatory diseases. Although a few PRS inhibitors have been derivatized from natural sources or substrate mimetics, small-molecule PRS inhibitors have not been reported...
May 10, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28492544/halofuginone-dually-regulates-autophagic-flux-through-nutrient-sensing-pathways-in-colorectal-cancer
#2
Guo-Qing Chen, Rui-Hong Gong, Da-Jian Yang, Ge Zhang, Ai-Ping Lu, Siu-Cheong Yan, Shu-Hai Lin, Zhao-Xiang Bian
Autophagy has a key role in metabolism and impacts on tumorigenesis. Our previous study found that halofuginone (HF) exerts anticancer activity in colorectal cancer (CRC) by downregulating Akt/mTORC1 (mechanistic target of rapamycin complex 1) signaling pathway. But whether and how HF regulates autophagy and metabolism to inhibit cancer growth remains an open question. Here, we unveil that HF activates ULK1 by downregulation of its phosphorylation site at Ser757 through Akt/mTORC1 signaling pathway, resulting in induction of autophagic flux under nutrient-rich condition...
May 11, 2017: Cell Death & Disease
https://www.readbyqxmd.com/read/28487390/activation-of-the-amino-acid-response-pathway-blunts-the-effects-of-cardiac-stress
#3
Pu Qin, Pelin Arabacilar, Roberta E Bernard, Weike Bao, Alan R Olzinski, Yuanjun Guo, Hind Lal, Stephen H Eisennagel, Michael C Platchek, Wensheng Xie, Julius Del Rosario, Mohamad Nayal, Quinn Lu, Theresa Roethke, Christine G Schnackenberg, Fe Wright, Michael P Quaile, Wendy S Halsey, Ashley M Hughes, Ganesh M Sathe, George P Livi, Robert B Kirkpatrick, Xiaoyan A Qu, Deepak K Rajpal, Maria Faelth Savitski, Marcus Bantscheff, Gerard Joberty, Giovanna Bergamini, Thomas L Force, Gregory J Gatto, Erding Hu, Robert N Willette
BACKGROUND: The amino acid response (AAR) is an evolutionarily conserved protective mechanism activated by amino acid deficiency through a key kinase, general control nonderepressible 2. In addition to mobilizing amino acids, the AAR broadly affects gene and protein expression in a variety of pathways and elicits antifibrotic, autophagic, and anti-inflammatory activities. However, little is known regarding its role in cardiac stress. Our aim was to investigate the effects of halofuginone, a prolyl-tRNA synthetase inhibitor, on the AAR pathway in cardiac fibroblasts, cardiomyocytes, and in mouse models of cardiac stress and failure...
May 9, 2017: Journal of the American Heart Association
https://www.readbyqxmd.com/read/28440200/effect-of-halofuginone-on-the-pathogenesis-of-autoimmune-thyroid-disease-in-different-mice-models
#4
Xin Hou, Jin Zhou, Rong Yang, Shanshan Liu, Mei Bi, Tong Liu, Chenling Fan, Haixia Guan, Yushu Li, Zhongyan Shan, Weiping Teng
OBJECTIVE: Our objectives were to investigate the therapeutic effect of halofuginone (HF) in the treatment of autoimmune thyroid diseases (AITDs) and explore its underlying mechanism of action. METHODS: The Graves' disease (GD) model was generated by immunizing female BALB/c mice with adenovirus expressing the TSH receptor A subunit (Ad-TSHR289). The Ad-TSHRA+HF and Ad-TSHRA+DMSO groups were injected intraperitoneally with HF or the vehicle control (DMSO), respectively...
April 23, 2017: Endocrine, Metabolic & Immune Disorders Drug Targets
https://www.readbyqxmd.com/read/28339722/prevalence-and-drug-resistance-of-avian-eimeria-species-in-broiler-chicken-farms-of-zhejiang-province-china
#5
L-H Lan, B-B Sun, B-X-Z Zuo, X-Q Chen, A-F Du
In this study, coccidia were isolated and identified from 5 main poultry farms located in Zhejiang province, eastern China. The overall prevalence of Eimeria spp. was 30.7% (95 of 310). Five common species were observed: E. tenella, E. acervulina, E. maxima, E. necatrix, and E. mitis. Two isolates (HZ and QZ) were tested for sensitivity to 8 anticoccidial drugs using 4 indexes including anticoccidial index (ACI), percent of optimum anticoccidial activity (POAA), reduction of lesion scores (RLS), and relative oocyst production (ROP): sulfachloropyrazine, toltrazuril, diclazuril, sulfamonomethoxine/trimethoprim, and amprolium; sulfaquinoxaline/sulfadimethoxine, nicarbazin, and halofuginone...
February 22, 2017: Poultry Science
https://www.readbyqxmd.com/read/28039084/halofuginone-enhances-the-chemo-sensitivity-of-cancer-cells-by-suppressing-nrf2-accumulation
#6
Kouhei Tsuchida, Tadayuki Tsujita, Makiko Hayashi, Asaka Ojima, Nadine Keleku-Lukwete, Fumiki Katsuoka, Akihito Otsuki, Haruhisa Kikuchi, Yoshiteru Oshima, Mikiko Suzuki, Masayuki Yamamoto
The KEAP1-NRF2 system regulates the cellular defence against oxidative and xenobiotic stresses. NRF2 is a transcription factor that activates the expression of cytoprotective genes encoding antioxidative, detoxifying and metabolic enzymes as well as transporters. Under normal conditions, KEAP1 represses NRF2 activity by degrading the NRF2 protein. When cells are exposed to stresses, KEAP1 stops promoting NRF2 degradation, and NRF2 rapidly accumulates and activates the transcription of target genes. Constitutive accumulation of NRF2 via a variety of mechanisms that disrupt KEAP1-mediated NRF2 degradation has been observed in various cancer types...
December 28, 2016: Free Radical Biology & Medicine
https://www.readbyqxmd.com/read/28013187/halofuginone-inhibits-tnf-%C3%AE-induced-the-migration-and-proliferation-of-fibroblast-like-synoviocytes-from-rheumatoid-arthritis-patients
#7
Shan Zeng, Kefeng Wang, Mingcheng Huang, Qian Qiu, Youjun Xiao, Maohua Shi, Yaoyao Zou, Xiuyan Yang, Hanshi Xu, Liuqin Liang
Fibroblast-like synoviocytes (FLSs) display an aggressive phenotype that is a critical factor in cartilage destruction in rheumatoid arthritis (RA). Increased FLS migration and proliferation are essential to the pathology of RA. Halofuginone has been found to inhibit cell migration and proliferation in cancer cells. However, whether halofuginone has a role in the treatment of RA FLSs is unclear. In this study, we found that halofuginone reduced migration, invasion, cell proliferation and MMPs expression in RA FLSs...
February 2017: International Immunopharmacology
https://www.readbyqxmd.com/read/27878913/response-of-an-ovine-laryngeal-injury-model-to-a-novel-fibrosis-inhibitor
#8
Jacqueline Allen
BACKGROUND: Vocal fold injury results in severe voice alteration that limits occupational function and social interaction. An ovine model of laryngeal injury has been developed, validated and utilized to examine laryngeal wound healing and the effect of a novel collagen inhibitor (halofuginone) on surgical wound healing. The study design includes basic research and animal model. METHODS: An ovine laryngeal model was utilized to study controlled vocal fold injury and healing...
April 2017: ANZ Journal of Surgery
https://www.readbyqxmd.com/read/27798837/biochemical-and-structural-characterization-of-selective-allosteric-inhibitors-of-the-plasmodium-falciparum-drug-target-prolyl-trna-synthetase
#9
Stephen Nakazawa Hewitt, David M Dranow, Benjamin G Horst, Jan A Abendroth, Barbara Forte, Irene Hallyburton, Chimed Jansen, Beatriz Baragaña, Ryan Choi, Kasey L Rivas, Matthew A Hulverson, Mitchell Dumais, Thomas E Edwards, Donald D Lorimer, Alan H Fairlamb, David W Gray, Kevin D Read, Adele M Lehane, Kiaran Kirk, Peter J Myler, Amy Wernimont, Chris Walpole, Robin Stacy, Lynn K Barrett, Ian H Gilbert, Wesley C Van Voorhis
Plasmodium falciparum (Pf) prolyl-tRNA synthetase (ProRS) is one of the few chemical-genetically validated drug targets for malaria, yet highly selective inhibitors have not been described. In this paper, approximately 40,000 compounds were screened to identify compounds that selectively inhibit PfProRS enzyme activity versus Homo sapiens (Hs) ProRS. X-ray crystallography structures were solved for apo, as well as substrate- and inhibitor-bound forms of PfProRS. We identified two new inhibitors of PfProRS that bind outside the active site...
January 13, 2017: ACS Infectious Diseases
https://www.readbyqxmd.com/read/27769022/tadalafil-reduces-airway-hyperactivity-and-protects-against-lung-and-respiratory-airways-dysfunction-in-a-rat-model-of-silicosis
#10
Rania R Abdelaziz, Wagdi F Elkashef, Eman Said
Silicosis is a crippling respiratory disorder characterized by massive lung inflammation and fibrosis. The current study provides evidence on the protective potential of tadalafil; a specific phosphodiesterase-5 (PDE-5) inhibitor against experimentally-induced pulmonary silicosis in rats. Silicosis was induced by intranasal instillation of crystalline silica (50mg/rat). Halofuginone hydrobromide; a standard collagen-1 synthesis inhibitor was selected as a reference anti-fibrotic. Daily oral administration of tadalafil (1mg/kg) for 8weeks significantly ameliorated silica-induced pulmonary damage...
November 2016: International Immunopharmacology
https://www.readbyqxmd.com/read/27709544/evaluation-and-elucidation-studies-of-natural-aglycones-for-anticancer-potential-using-apoptosis-related-markers-an-in-silico-study
#11
Salman Akhtar, M Kalim A Khan, Jamal M Arif
Exposure to exogenous and endogenous chemicals and subsequent cellular and molecular changes has been linked to enhanced cell proliferation and restricted apoptosis phenomenon. Though in the past decades numerous anticancer drugs inducing programmed cell death in cancer cells by targeting specific apoptotic markers have reached the market, they have been allied with unwanted side effects, ranging from mild to severe toxicity. With further understanding on the functional mechanism of p53 and MDM2 in apoptosis and in our continuous search for new and potent multi-target anticancer lead compounds, we have carried out molecular docking and inhibition studies of the selected aglycones along with selected anticancer leads, against the specific apoptotic and cell cycle markers using AutoDock Tools 4...
October 5, 2016: Interdisciplinary Sciences, Computational Life Sciences
https://www.readbyqxmd.com/read/27687492/single-cell-analysis-reveals-igf-1-potentiation-of-inhibition-of-the-tgf-%C3%AE-smad-pathway-of-fibrosis-in-human-keratocytes-in-vitro
#12
Tomislav Sarenac, Martin Trapecar, Lidija Gradisnik, Marjan Slak Rupnik, Dusica Pahor
Corneal wound healing is often affected by TGF-β-mediated fibrosis and scar formation. Guided fibrosis with IGF-1 and antifibrotic substances might maintain corneal transparency. Primary human corneal keratocytes under serum-free conditions were used as a model of corneal stromal wounding, with markers of corneal fibrosis and opacity studied under TGF-β2 stimulation. Single-cell imaging flow cytometry was used to determine nuclearization of Smad3, and intracellular fluorescence intensity of Smad7 and the corneal crystallin aldehyde dehydrogenase 3A1...
September 30, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27674657/the-mechanism-study-on-the-inhibition-effect-of-halofuginone-on-lung-cancer-cell-epithelial-mesenchymal-transition-induced-by-radiation-therapy
#13
Y Chen, Y Wang, N Liu, L Zhao
No abstract text is available yet for this article.
October 1, 2016: International Journal of Radiation Oncology, Biology, Physics
https://www.readbyqxmd.com/read/27533085/halofuginone-inhibits-radiotherapy-induced-epithelial-mesenchymal-transition-in-lung-cancer
#14
Yang Chen, Weishuai Liu, Peng Wang, Hailing Hou, Ningbo Liu, Linlin Gong, Youyou Wang, Kai Ji, Lujun Zhao, Ping Wang
Radiotherapy is used to treat many different human tumors. Paradoxically, radiation can activate TGF-β1 signaling and induce the epithelial-mesenchymal transition (EMT), which is associated with enhanced tumor progression. This study investigated the inhibitory effects of halofuginone, a plant-derived alkaloid that has been shown to inhibit TGF-β1 signaling, on radiation-induced EMT and explored the underlying mechanisms using a Lewis lung carcinoma (LLC) xenograft model. The cells and animals were divided into five treatment groups: Normal Control (NC), Halofuginone alone (HF), Radiotherapy alone (RT), Radiotherapy combined with Halofuginone (RT+HF), and Radiotherapy combined with the TGF-β1 inhibitor SB431542 (RT+SB)...
November 1, 2016: Oncotarget
https://www.readbyqxmd.com/read/27518579/-clinical-epidemiology-of-cryptosporidiosis-in-calves
#15
S E Weber, C Lippuner, S Corti, P Deplazes, M Hässig
The aim of this study was to determine whether there is an association between Cryptosporidium infections in calves and immunological factors, as well as farm-related factors or the application of the anti-cryptosporidiosis drug Halofuginone. From January to June 2010, 63 cow-calf-pairs from 20 different farms near Zürich, Switzerland have been investigated. Each cowcalf- pair was visited three times within the first 6 weeks of life to collect data of the farm and animals, as well as blood, faecal, colostral and milk samples...
May 2016: Schweizer Archiv Für Tierheilkunde
https://www.readbyqxmd.com/read/27457799/amelioration-of-radiation-induced-lung-injury-by-halofuginone-an-experimental-study-in-wistar-albino-rats
#16
M Calik, G Yavas, S G Calik, C Yavas, Z E Celik, M F Sargon, H Esme
To evaluate effects of halofuginone (H) on radiation-induced lung injury (RILI), 60 rats were divided into six groups: Group (G) 1 control, G2 radiotherapy (RT) only, G3 and G4 2. 5 and 5 μg H and G5 and G6 RT + 2.5 and 5 μg H groups, respectively. A single dose of 12 Gy RT was given to both lungs. H was applied intraperitoneally with daily doses, until animals were killed at 6 and 16 weeks after RT. At 6th and 16th weeks of RT, five rats from each group were killed. Lung tissues were dissected for light and electron microscopy...
July 24, 2016: Human & Experimental Toxicology
https://www.readbyqxmd.com/read/27443201/a-multi-residue-method-for-17-anticoccidial-drugs-and-ractopamine-in-animal-tissues-by-liquid-chromatography-tandem-mass-spectrometry-and-time-of-flight-mass-spectrometry
#17
Johanna L Matus, Joe O Boison
A new and sensitive multi-residue liquid chromatography-tandem mass spectrometry (LC-MS/MS) and liquid chromatography-quadrupole time-of-flight-mass spectrometry (LC-QToF-MS) method was developed and validated for the determination and confirmation of residues of 17 anticoccidials, plus free ractopamine in poultry muscle and liver, and bovine muscle, liver, and kidney tissues. The 17 anticoccidials are lasalocid, halofuginone, narasin, monensin, semduramicin, ethopabate, robenidine, buquinolate, toltrazuril as its sulfone metabolite, maduramicin, salinomycin, diclazuril, amprolium, decoquinate, dinitolmide, clopidol, and the nicarbazin metabolite DNC (N,N1-bis(4-nitrophenyl)urea)...
May 2016: Drug Testing and Analysis
https://www.readbyqxmd.com/read/27388880/halofuginone-alleviates-burn-induced-hepatic-and-renal-damage-in-rats
#18
Kivilcim Karadeniz Cerit, Berna Karakoyun, Meral Yüksel, Feriha Ercan, Halil Tuğtepe, Tolga E Dagli, Berrak Ç Yeğen
The aim of this study was to evaluate the possible protective effects of halofuginone on burn-induced oxidative injury of the liver and kidney. For the induction of burn, backs of Wistar albino rats were shaved and exposed for 10 seconds to water bath at 90°C, whereas rats in the control group were exposed for 10 seconds at 25°C. Rats were then administered either saline (1 ml/kg) or halofuginone (100 μg/kg/day) intraperitoneally and decapitated at the 24th hour (early burn) or on the 7th day (late burn)...
January 2017: Journal of Burn Care & Research: Official Publication of the American Burn Association
https://www.readbyqxmd.com/read/27385212/halofuginone-and-artemisinin-synergistically-arrest-cancer-cells-at-the-g1-g0-phase-by-upregulating-p21cip1-and-p27kip1
#19
Guoqing Chen, Ruihong Gong, Xianli Shi, Dajian Yang, Ge Zhang, Aiping Lu, Jianbo Yue, Zhaoxiang Bian
Combinational drug therapy is one of the most promising strategies in modern anticancer research. Traditional Chinese medicine (TCM) formulas represent a wealth of complex combinations proven successful over centuries of clinical application. One such formula used to treat a variety of diseases, including cancer, contains two herbs, whose main active components are Halofuginone (HF) and Artemisinin (ATS). Here we studied the anticancer synergism of HF and ATS in various cancer cell lines and in a xenograft nude mice model...
August 2, 2016: Oncotarget
https://www.readbyqxmd.com/read/27369778/therapeutic-elimination-of-the-type-1-interferon-receptor-for-treating-psoriatic-skin-inflammation
#20
Jun Gui, Michael Gober, Xiaoping Yang, Kanstantsin V Katlinski, Christine M Marshall, Meena Sharma, Victoria P Werth, Darren P Baker, Hallgeir Rui, John T Seykora, Serge Y Fuchs
Phototherapy with UV light is a standard treatment for psoriasis, yet the mechanisms underlying the therapeutic effects are not well understood. Studies in human and mouse keratinocytes and in the skin tissues from human patients and mice showed that UV treatment triggers ubiquitination and downregulation of the type I IFN receptor chain IFNAR1, leading to suppression of IFN signaling and an ensuing decrease in the expression of inflammatory cytokines and chemokines. The severity of imiquimod-induced psoriasiform inflammation was greatly exacerbated in skin of mice deficient in IFNAR1 ubiquitination (Ifnar1(SA))...
October 2016: Journal of Investigative Dermatology
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