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https://www.readbyqxmd.com/read/28642838/adaptive-pathways-and-emerging-strategies-overcoming-treatment-resistance-in-castration-resistant-prostate-cancer
#1
Cameron M Armstrong, Allen C Gao
The therapies available for prostate cancer patients whom progress from hormone-sensitive to castration resistant prostate cancer include both systemic drugs, including docetaxel and cabazitaxel, and drugs that inhibit androgen signaling such as enzalutamide and abiraterone. Unfortunately, it is estimated that up to 30% of patients have primary resistance to these treatments and over time even those who initially respond to therapy will eventually develop resistance and their disease will continue to progress regardless of the presence of the drug...
October 2016: Asian Journal of Urology
https://www.readbyqxmd.com/read/28634145/taeniasis-caused-by-taenia-saginata-in-gianyar-townand-taenia-solium-in-karangasem-villagesof-bali-indonesia-2011-2016-how-to-detect-tapeworm-carriers-anamnesis-or-microscopy
#2
Kadek Swastika, Toni Wandra, Nyoman Sadra Dharmawan, I Made Sudarmaja, John Master Saragih, Luh Putu Eka Diarthini, Luh Ariwati, Putu Ayu Asri Damayanti, Dewa Ayu Agus Sri Laksemi, Nengah Kapti, Putu Sutisna, Tetsuya Yanagida, Akira Ito
From January 2011 until September 2016, screening of taeniasis carriers was carried out in a town in Gianyar District (Taenia saginata) and in villages which consisted of several Banjars (the smallest community units) on the eastern slope of Mt. Agung, Karangasem District (Taenia solium) in Bali, Indonesia. Fecal samples from all community members who chose to participate were examined microscopically for detection of taeniid eggs each person completedwith a questionnaire to determine if they had seen whitish, noodle-like proglottids (anamnesis) in their feces...
June 17, 2017: Acta Tropica
https://www.readbyqxmd.com/read/28632878/identification-of-novel-g-protein-coupled-receptor-143-ligands-as-pharmacologic-tools-for-investigating-x-linked-ocular-albinism
#3
Elisabetta De Filippo, Prashiela Manga, Anke C Schiedel
Purpose: GPR143 regulates melanosome biogenesis and organelle size in pigment cells. The mechanisms underlying receptor function remain unclear. G protein-coupled receptors (GPCRs) are excellent pharmacologic targets; thus, we developed and applied a screening approach to identify potential GPR143 ligands and chemical modulators. Methods: GPR143 interacts with β-arrestin; we therefore established a β-arrestin recruitment assay to screen for compounds that modulate activity...
June 1, 2017: Investigative Ophthalmology & Visual Science
https://www.readbyqxmd.com/read/28627643/niclosamide-attenuates-inflammatory-cytokines-via-the-autophagy-pathway-leading-to-improved-outcomes-in-renal-ischemia-reperfusion-injury
#4
Lin-Xia Zhang, Hui-Juan Zhao, Dong-Li Sun, Shan-Lin Gao, Hong-Mei Zhang, Xin-Guo Ding
Renal ischemia/reperfusion (I/R) injury is a debilitating condition that leads to loss renal function and damage to kidney tissue in the majority of patients with acute kidney disease. Previous studies have indicated that autophagy serves a protective function in renal I/R injury. In the present study, the effect of the anthelmintic niclosamide in the regulation of inflammatory responses in kidney I/R was investigated. A total of 40 Sprague-Dawley rats were randomly divided into the following 5 groups (n=8 in each group): Sham group; renal I/R injury; renal I/R injury plus 3‑methyladenine (3‑MA) treatment (15 mg/kg); renal I/R injury plus niclosamide (25 mg/kg); and renal I/R injury plus rapamycin (10 mg/kg)...
June 14, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28622697/vitamin-c-and-doxycycline-a-synthetic-lethal-combination-therapy-targeting-metabolic-flexibility-in-cancer-stem-cells-cscs
#5
Ernestina Marianna De Francesco, Gloria Bonuccelli, Marcello Maggiolini, Federica Sotgia, Michael P Lisanti
Here, we developed a new synthetic lethal strategy for further optimizing the eradication of cancer stem cells (CSCs). Briefly, we show that chronic treatment with the FDA-approved antibiotic Doxycycline effectively reduces cellular respiration, by targeting mitochondrial protein translation. The expression of four mitochondrial DNA encoded proteins (MT-ND3, MT-CO2, MT-ATP6 and MT-ATP8) is suppressed, by up to 35-fold. This high selection pressure metabolically synchronizes the surviving cancer cell sub-population towards a predominantly glycolytic phenotype, resulting in metabolic inflexibility...
June 9, 2017: Oncotarget
https://www.readbyqxmd.com/read/28606189/therapeutic-efficacy-of-artemisia-absinthium-against-hymenolepis-nana-in-vitro-and-in-vivo-studies-in-comparison-with-the-anthelmintic-praziquantel
#6
E V N Beshay
Hymenolepis nana is a common intestinal tapeworm that affects humans. Drugs are available for the treatment of this infection, including praziquantel (PZQ), nitazoxanide and niclosamide. Although the drug of choice is praziquantel, due to its high cure rates, indicators of the development of PZQ resistance by different parasites have begun to appear over recent decades. Therefore, this study was a trial to find an alternative to PZQ by assessing the activity of the crude aqueous extract of the medicinal herb Artemisia absinthium against H...
June 13, 2017: Journal of Helminthology
https://www.readbyqxmd.com/read/28596138/preparation-characterization-and-cytotoxicity-studies-of-niclosamide-loaded-mesoporous-drug-delivery-systems
#7
Vishwas Pardhi, Rahul B Chavan, Rajesh Thipparaboina, Sowjanya Thatikonda, Vgm Naidu, Nalini R Shastri
Recent reports on the anticancer potential of niclosamide have opened new avenues for anticancer treatment. Niclosamide belongs to the BCS class II, which is indicative of poor solubility and dissolution rate limited absorption. The aim of this study was to improve the dissolution rate of the drug by mesoporous drug delivery system. Porous silica grades (ordered and nonordered) with different pore size, pore volume and surface area were used in the study. The drug was loaded on silica carriers by the solvent evaporation method and characterized by BET surface area analysis, SEM, P-XRD, DSC, and FTIR...
June 5, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28575805/niclosamide-induces-apoptosis-through-mitochondrial-intrinsic-pathway-and-inhibits-migration-and-invasion-in-human-thyroid-cancer-in-vitro
#8
Kai Yu, Tingting Wang, Yujue Li, Chun Wang, Xia Wang, Mei Zhang, Yongmei Xie, Shuangqing Li, Zhenmei An, Tinghong Ye
The morbidity of thyroid cancer has been rising obviously throughout the world during the past years. Classic treatment procedure is generally curable for low risk differentiated thyroid cancer, but may lead to many postoperative complications. And low-level of thyroid stimulating hormone after surgery has side effects on both cardiovascular system and skeletal system. Furthermore effective treatment approaches for more aggressive differentiated thyroid cancer, poorly differentiated thyroid cancer and anaplastic thyroid cancer are absent, thus new candidates that can inhibit tumor growth and metastasis are urgently needed...
May 29, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28561092/a-field-analysis-of-lampricide-photodegradation-in-great-lakes-tributaries
#9
Megan B McConville, Natan M Cohen, Shawn M Nowicki, Stephen R Lantz, Jase L Hixson, Adam S Ward, Christina K Remucal
The lampricides 3-trifluoromethyl-4-nitrophenol (TFM) and 2',5-dichloro-4'-nitrosalicylanilide (niclosamide) are added to Great Lakes tributaries to target the sea lamprey, an invasive parasitic fish. This study examines the photochemical behavior of the lampricides in Carpenter Creek, Sullivan Creek, and the Manistique River. The observed loss of TFM in Carpenter and Sullivan Creeks (i.e., 34 and 19%) was similar to the loss of bromide in parallel time of passage studies (i.e., 30 and 29%), demonstrating that TFM photodegradation was minimal in both tributaries during the lampricide application...
May 31, 2017: Environmental Science. Processes & Impacts
https://www.readbyqxmd.com/read/28551619/structure-activity-relationship-of-niclosamide-derivatives
#10
Zhonghai Tang, Ulyana Muñoz Acuña, Nelson Freitas Fernandes, Somsundaram Chettiar, Pui-Kai Li, Esperanza Carcache DE Blanco
BACKGROUND/AIM: Cancer is a leading cause of death. Hence, this study aimed at the optimization of niclosamide derivatives for the development of new potential anticancer agents. MATERIALS AND METHODS: Niclosamide derivatives were synthesized and tested against a panel of human cancer cells: MDA and MCF7 breast cancer cells, PC3 and DU-145 prostate cancer cells, Hela cervical cancer cells, and HL-60 acute promyelocytic leukemia cells. They were also tested in nuclear factor-ĸappa B (NFĸB), V-Ki-ras2 Kirsten rat sarcoma viral oncogene (KRAS), and mitochondria transmembrane potential (MTP) assays...
June 2017: Anticancer Research
https://www.readbyqxmd.com/read/28532040/design-synthesis-and-characterization-of-poly-methacrylic-acid-niclosamide-and-its-effect-on-arterial-function
#11
Rui Ma, Zhen-Gang Ma, Chang-Lin Zhen, Xin Shen, Shan-Liang Li, Li Li, Yu-Feng Zheng, De-Li Dong, Zhi-Jie Sun
We have found that niclosamide induced relaxation of constricted artery. However, niclosamide is insoluble, the low bioavailability and the resultant low plasma concentration limit its potential exertion in vivo. The aim of the present study is to synthesize a soluble poly (methacrylic acid-niclosamide) polymer (PMAN) and study the effects of PMAN on arterial function in vitro and the blood pressure and heart rate of rats in vivo. We synthesized the poly (methacrylic acid-niclosamide) polymer (PMAN), the chemical structure of which was identified by FTIR and (1)H NMR spectra...
August 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/28531943/recent-trends-in-zikv-research-a-step-away-from-cure
#12
REVIEW
Aftab Alam, Nikhat Imam, Anam Farooqui, Shahnawaz Ali, Md Zubbair Malik, Romana Ishrat
Zika virus (ZikV) is a member of the Flaviviridae virus family, genus Flavivirus has emerged as a potential threat to human health worldwide. Consequences of vertical infections includes microcephaly with brain and eye anomalies, and adult infections includes Guillain-Barrésyndrome (GBS), brain ischemia, myelitis and meningoencephalitis. To develop a better treatment, many efforts are being made, like drug-repurposing concept for FDA-approved drugs for antiviral activity are screened against ZikV infection and emerging as a promising alternative to expedite drug development and various vaccines like DNA, ZPIV, LAIV, mRNA and AGS-v vaccines have been designed and in under clinical trial phases...
July 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28529629/the-antihelminthic-drug-niclosamide-effectively-inhibits-the-malignant-phenotypes-of-uveal-melanoma-in-vitro-and-in-vivo
#13
Jingfeng Zhou, Bei Jin, Yanli Jin, Yizhi Liu, Jingxuan Pan
Uveal melanoma (UM) is a lethal intraocular malignancy with an average survival of only 2~8 months in patients with hepatic metastasis. Currently, there is no effective therapy for metastatic UM. Here, we reported that niclosamide, an effective repellence of tapeworm that has been approved for use in patients for approximately 50 years, exhibited strong antitumor activity in UM cells in vitro and in vivo. We showed that niclosamide potently inhibited UM cell proliferation, induced apoptosis and reduced migration and invasion...
2017: Theranostics
https://www.readbyqxmd.com/read/28515572/a-family-of-fe-n-c-oxygen-reduction-electrocatalysts-for-microbial-fuel-cell-mfc-application-relationships-between-surface-chemistry-and-performances
#14
Carlo Santoro, Alexey Serov, Rohan Gokhale, Santiago Rojas-Carbonell, Lydia Stariha, Jonathan Gordon, Kateryna Artyushkova, Plamen Atanassov
Different iron-based cathode catalysts have been studied for oxygen reduction reaction (ORR) in neutral media and then applied into microbial fuel cells (MFC). The catalysts have been synthesized using sacrificial support method (SSM) using eight different organic precursors named Niclosamide, Ricobendazole, Guanosine, Succinylsulfathiazole, Sulfacetamide, Quinine, Sulfadiazine and Pyrazinamide. Linear Sweep Voltammetry (LSV) curves were obtained for the catalysts using a O2 saturated in 0.1 M potassium phosphate buffer and 0...
May 15, 2017: Applied Catalysis. B, Environmental
https://www.readbyqxmd.com/read/28500234/niclosamide-and-bicalutamide-combination-treatment-overcomes-enzalutamide-and-bicalutamide-resistant-prostate-cancer
#15
Chengfei Liu, Cameron M Armstrong, Wei Lou, Alan P Lombard, Vito Cucchiara, Xinwei Gu, Joy C Yang, Nagalakshmi Nadiminty, Chong-Xian Pan, Christopher P Evans, Allen C Gao
Activation of the androgen receptor (AR) and its splice variants is linked to advanced prostate cancer and drives resistance to antiandrogens. The roles of AR and AR variants in the development of resistance to androgen deprivation therapy (ADT) and bicalutamide treatment, however, are still incompletely understood. To determine whether AR variants play a role in bicalutamide resistance, we developed bicalutamide resistant LNCaP cells (LNCaP-BicR) and found that these resistant cells express significantly increased levels of AR variants, particularly AR-V7, both at the mRNA and protein levels...
May 12, 2017: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/28493830/ing5-knockdown-enhances-migration-and-invasion-of-lung-cancer-cells-by-inducing-emt-via-egfr-pi3k-akt-and-il-6-stat3-signaling-pathways
#16
Xin-Li Liu, Xu-Tao Zhang, Jin Meng, Hong-Fei Zhang, Yong Zhao, Chen Li, Yang Sun, Qi-Bing Mei, Feng Zhang, Tao Zhang
ING5 belongs to the Inhibitor of Growth (ING) candidate tumor suppressor family, whose functions have been involved in the regulation of chromatin remodeling, cell cycle progression, proliferation and apoptosis. Our previous study has shown that ING5 overexpression inhibits lung cancer aggressiveness via suppressing epithelial to mesenchymal transition (EMT). However, the mechanisms remain largely unknown. In the current study, by Phospho-Kinase array and western blot, we have defined significantly upregulated EGFR/PI3K/Akt and IL-6/STAT3 oncogenic signaling pathways in ING5 knockdown A549 cells, which could be downregulated by ING5 overexpression...
April 21, 2017: Oncotarget
https://www.readbyqxmd.com/read/28471351/repurposing-niclosamide-as-a-versatile-antimicrobial-surface-coating-against-device-associated-hospital-acquired-bacterial-infections
#17
Tinotenda Gwisai, Nisha Hollingsworth, Sarah Cowles, Nagendran Tharmalingam, Eleftherios Mylonakis, Beth Fuchs, Anita Shukla
Device-associated and hospital-acquired infections remain amongst the greatest challenges in regenerative medicine. Furthermore, the rapid emergence of antibiotic resistance and lack of new classes of antibiotics has made the treatment of these bacterial infections increasingly difficult. The repurposing of Food and Drug Administration (FDA) approved drugs for antimicrobial therapies is a powerful means of reducing the time and cost associated with drug discovery and development. In this work, niclosamide, a commercially available anthelmintic drug with recently identified antimicrobial properties, was found to prevent and combat existing biofilms of several relevant gram-positive bacteria, namely strains of Staphylococcus aureus, including methicillin resistant S...
May 4, 2017: Biomedical Materials
https://www.readbyqxmd.com/read/28437447/carbonic-anhydrase-iii-car3-is-not-required-for-fatty-acid-synthesis-and-does-not-protect-against-high-fat-diet-induced-obesity-in-mice
#18
Sarah W Renner, Lauren M Walker, Lawrence J Forsberg, Jonathan Z Sexton, Jay E Brenman
Carbonic anhydrases are a family of enzymes that catalyze the reversible condensation of water and carbon dioxide to carbonic acid, which spontaneously dissociates to bicarbonate. Carbonic anhydrase III (Car3) is nutritionally regulated at both the mRNA and protein level. It is highly enriched in tissues that synthesize and/or store fat: liver, white adipose tissue, brown adipose tissue, and skeletal muscle. Previous characterization of Car3 knockout mice focused on mice fed standard diets, not high-fat diets that significantly alter the tissues that highly express Car3...
2017: PloS One
https://www.readbyqxmd.com/read/28418865/anti-helminthic-niclosamide-inhibits-ras-driven-oncogenic-transformation-via-activation-of-gsk-3
#19
Sung Yong Ahn, Ji Hye Yang, Nam Hee Kim, Kyungro Lee, Yong Hoon Cha, Jun Seop Yun, Hee Eun Kang, Yoonmi Lee, Jiwon Choi, Hyun Sil Kim, Jong In Yook
Despite the importance of Ras oncogenes as a therapeutic target in human cancer, their 'undruggable' tertiary structures limit the effectiveness of anti-Ras drugs. Canonical Wnt signaling contributes to Ras activity by glycogen synthase kinase 3 (GSK-3)-dependent phosphorylation at the C-terminus and subsequent degradation. In the accompanying report, we show that the anti-helminthic niclosamide directly binds to GSK-3 and inhibits Axin functions in colon cancer cells, with reversion of Snail-mediated epithelial-mesenchymal transition...
May 9, 2017: Oncotarget
https://www.readbyqxmd.com/read/28418862/niclosamide-is-a-potential-therapeutic-for-familial-adenomatosis-polyposis-by-disrupting-axin-gsk3-interaction
#20
Sung Yong Ahn, Nam Hee Kim, Kyungro Lee, Yong Hoon Cha, Ji Hye Yang, So Young Cha, Eunae Sandra Cho, Yoonmi Lee, Jeong Seok Cha, Hyun Soo Cho, Yoon Jeon, Young-Su Yuk, Suebean Cho, Kyoung Tai No, Hyun Sil Kim, Ho Lee, Jiwon Choi, Jong In Yook
The epithelial-mesenchymal transition (EMT) is implicated in tumorigenesis and cancer progression, and canonical Wnt signaling tightly controls Snail, a key transcriptional repressor of EMT. While the suppression of canonical Wnt signaling and EMT comprises an attractive therapeutic strategy, molecular targets for small molecules reverting Wnt and EMT have not been widely studied. Meanwhile, the anti-helminthic niclosamide has been identified as a potent inhibitor of many oncogenic signaling pathways although its molecular targets have not yet been clearly identified...
May 9, 2017: Oncotarget
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