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https://www.readbyqxmd.com/read/28454094/proteolytic-cleavages-in-the-extracellular-domain-of-receptor-tyrosine-kinases-by-membrane-associated-serine-proteases
#1
Li-Mei Chen, Karl X Chai
The epithelial extracellular membrane-associated serine proteases matriptase, hepsin, and prostasin are proteolytic modifying enzymes of the extracellular domain (ECD) of the epidermal growth factor receptor (EGFR). Matriptase also cleaves the ECD of the vascular endothelial growth factor receptor 2 (VEGFR2) and the angiopoietin receptor Tie2. In this study we tested the hypothesis that these serine proteases may cleave the ECD of additional receptor tyrosine kinases (RTKs). We co-expressed the proteases in an epithelial cell line with Her2, Her3, Her4, insulin receptor (INSR), insulin-like growth factor I receptor (IGF-1R), the platelet-derived growth factor receptors (PDGFRs) α and β, or nerve growth factor receptor A (TrkA)...
April 10, 2017: Oncotarget
https://www.readbyqxmd.com/read/28454093/hsp90-inhibitor-17-dmag-exerts-anticancer-effects-against-gastric-cancer-cells-principally-by-altering-oxidant-antioxidant-balance
#2
Jeong Goo Kim, Sang Chul Lee, Ok-Hee Kim, Kee-Hwan Kim, Kyo Young Song, Sang Kuon Lee, Byung Jo Choi, Wonjun Jeong, Say-June Kim
Heat shock protein 90 (HSP90) stabilizes numerous oncoproteins and, therefore, its inhibition has emerged as a promising antineoplastic strategy for diverse malignancies. In this study, we determined the therapeutic effects and mechanisms of action of a specific HSP90 inhibitor, 17-dimethylamino-ethylamino-17-demethoxygeldanamycin (17-DMAG), in gastric cancer cell lines (AGS, SNU-1, and KATO-III), patient-derived tissues, and a mouse xenograft model. 17-DMAG exerted anticancer effects against gastric cancer cells, manifested by significantly decreased proliferation rates (P < 0...
April 10, 2017: Oncotarget
https://www.readbyqxmd.com/read/28454090/peroxiredoxin-6-overexpression-attenuates-lipopolysaccharide-induced-acute-kidney-injury
#3
Dong Hun Lee, Ju Ho Park, Sang Bae Han, Do Young Yoon, Yu Yeon Jung, Jin Tae Hong
Peroxiredoxin 6 (PRDX6) is a member of the PRDX family of antioxidant enzymes and correlated with inflammatory response. Therefore, we investigated the role of PRDX6 during lipopolysaccharide (LPS)-induced acute kidney injury. Both 3 months aged PRDX6-overexpressing transgenic mice (PRDX6 mice) and wild type (WT) mice had acute renal injury induced by intraperitoneal injection of LPS (10 mg/kg)., PRDX6 mice showed decreased mortality and renal injury following LPS challenge compared to WT mice. Furthermore, infiltration of macrophages, T-cells and neutrophils, and the number of apoptotic cells were more decreased by LPS treatment in PRDX6 mice than in WT mice...
April 10, 2017: Oncotarget
https://www.readbyqxmd.com/read/28453984/functional-and-genetic-evidence-that-nucleoside-transport-is-highly-conserved-in-leishmania-species-implications-for-pyrimidine-based-chemotherapy
#4
Khalid J H Alzahrani, Juma A M Ali, Anthonius A Eze, Wan Limm Looi, Daniel N A Tagoe, Darren J Creek, Michael P Barrett, Harry P de Koning
Leishmania pyrimidine salvage is replete with opportunities for therapeutic intervention with enzyme inhibitors or antimetabolites. Their uptake into cells depends upon specific transporters; therefore it is essential to establish whether various Leishmania species possess similar pyrimidine transporters capable of drug uptake. Here, we report a comprehensive characterization of pyrimidine transport in L. major and L. mexicana. In both species, two transporters for uridine/adenosine were detected, one of which also transported uracil and the antimetabolites 5-fluoruracil (5-FU) and 5F,2'deoxyuridine (5F,2'dUrd), and was designated uridine-uracil transporter 1 (UUT1); the other transporter mediated uptake of adenosine, uridine, 5F,2'dUrd and thymidine and was designated Nucleoside Transporter 1 (NT1)...
April 20, 2017: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/28453850/a-novel-ligand-of-toll-like-receptor-4-from-the-sheath-of-wuchereria-bancrofti-microfilaria-induces-proinflammatory-response-in-macrophages
#5
Suprabhat Mukherjee, Sandip Mukherjee, Tushar K Maiti, Samir Bhattacharya, Santi P Sinha Babu
Background.: Lymphatic filariasis, frequently caused from Wuchereria bancrofti infection, is endemic in several parts of the globe and responsible for human health problems and socioeconomic loss to a large extent. Inflammatory consequences originating from host-parasite interaction play a major role in the disease pathology and allied complications. The identity of the key mediator of this process is yet unknown in filarial research. Methods.: Microfilarial protein (MfP) was isolated from the sheath of W...
March 15, 2017: Journal of Infectious Diseases
https://www.readbyqxmd.com/read/28449557/wnt-and-gsk3-signaling-pathways-in-bipolar-disorder-clinical-and-therapeutic-implications
#6
REVIEW
Ather Muneer
The neurobiology of bipolar disorder, a chronic and systemic ailment is not completely understood. The bipolar phenotype manifests in myriad ways, and psychopharmacological agents like lithium have long term beneficial effects. The enzyme glycogen synthase kinase 3 (GSK3) has come into focus, as lithium and several other mood stabilizing medications inhibit its activity. This kinase and its key upstream modulator, Wnt are dysregulated in mood disorders and there is a growing impetus to delineate the chief substrates involved in the development of these illnesses...
May 31, 2017: Clinical Psychopharmacology and Neuroscience: the Official Scientific Journal of the Korean College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28449367/metoprolol-pridopidine-drug-drug-interaction-and-food-effect-assessments-of-pridopidine-a-new-drug-for-treatment-of-huntington-disease
#7
Laura Rabinovich-Guilatt, Lilach Steiner, Hussein Hallak, Gina Pastino, Pierandrea Muglia, Ofer Spiegelstein
AIM: Pridopidine is an oral drug in clinical development for treatment of patients with Huntington disease. This study examined the interactions of pridopidine with in vitro cytochrome P450 activity and characterized the effects of pridopidine on CYP2D6 activity in healthy volunteers using metoprolol as a probe substrate. The effect of food on pridopidine exposure was assessed. METHODS: The ability of pridopidine to inhibit and/or induce in vitro activity of drug metabolising enzymes was examined in human liver microsomes and fresh hepatocytes...
April 27, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28449154/dual-raas-blockade-with-aliskiren-in-patients-with-severely-impaired-chronic-kidney-disease
#8
Franz Maximilian Rasche, Claudia Joel, Thomas Ebert, Thomas Frese, Filip Barinka, Volker Busch, Wilma Gertrud Rasche, Tom H Lindner, Jochen Schneider, Stephan Schiekofer
Dual renin-angiotensin-aldosterone blockade (dRAASb) is purposed in the prevention of the cardiorenal syndrome (CRS). However, all attempts with dRAASb even in patients with moderate impaired chronic kidney disease (CKD) were terminated due to the typical severe adverse events (SAE), e. g., hyperkalemia and rise of serum creatinine. The aim of our study with the direct renin inhibitor aliskiren was to evaluate the effect of dRAASb with a washout phase in patients with severely advanced CKD. We have studied 45 patients (G3b to 4, A2 and >A3; median glomerular filtration rate (GFR) CKD-EPI 31 (23-40) ml/min per 1...
April 27, 2017: Experimental and Clinical Endocrinology & Diabetes
https://www.readbyqxmd.com/read/28448784/a-motivational-interviewing-intervention-by-pharmacy-students-to-improve-medication-adherence
#9
Susan Abughosh, Xin Wang, Omar Serna, Tara Esse, Amanda Mann, Santhi Masilamani, Marcia McDonnell Holstad, Ekere James Essien, Marc Fleming
BACKGROUND: Diabetes mellitus (DM) patients with comorbid hypertension (HTN) are at a higher risk of developing microvascular and macrovascular DM complications. Through guideline-driven recommendations, angiotensin-converting enzyme inhibitors (ACEIs) and angiotensin II receptor blockers (ARBs) are highly recommended for these patients. Unfortunately, medication adherence to these products, though crucial to achieving therapeutic benefit, is frequently suboptimal. Motivational interviewing (MI) is a patient-centered collaborative communication style that is used to strengthen internal motivation for change that may prove effective in enhancing adherence...
May 2017: Journal of Managed Care & Specialty Pharmacy
https://www.readbyqxmd.com/read/28448588/allogeneic-pasc-transplantation-in-humanized-pigs-attenuates-cardiac-remodeling-post-myocardial-infarction
#10
Rafael Dariolli, Marcus V Naghetini, Euclydes F Marques, Celso K Takimura, Leonardo S Jensen, Bianca Kiers, Jeane M Tsutsui, Wilson Mathias, Pedro A Lemos Neto, Jose E Krieger
Cell therapy repair strategies using adult mesenchymal stromal cells have shown promising evidence to prevent cardiac deterioration in rodents even in the absence of robust differentiation of the cells into cardiomyocytes. We tested whether increasing doses of porcine adipose-tissue derived mesenchymal stem cells (pASCs) increase cardiac tissue perfusion in pigs post-myocardial infarction (MI) receiving angiotensin-converting-enzyme inhibitor (ACE inhibitors) and Beta-blockers similarly to patients. Female pigs were subjected to MI induction by sponge permanent occlusion of left circumflex coronary artery (LCx) generating approximately 10% of injured LV area with minimum hemodynamic impact...
2017: PloS One
https://www.readbyqxmd.com/read/28448568/inhibitory-effects-of-fenretinide-metabolites-n-4-methoxyphenyl-retinamide-mpr-and-4-oxo-n-4-hydroxyphenyl-retinamide-3-keto-hpr-on-fenretinide-molecular-targets-%C3%AE-carotene-oxygenase-1-stearoyl-coa-desaturase-1-and-dihydroceramide-%C3%AE-4-desaturase-1
#11
Eugenia Poliakov, William Samuel, Todd Duncan, Danielle B Gutierrez, Nathan L Mata, T Michael Redmond
The therapeutic capacity of fenretinide (N-[4-hydroxyphenyl] retinamide; 4-HPR) has been demonstrated for several conditions, including cancer, obesity, diabetes, and ocular disease. Yet, the mechanisms of action for its pleiotropic effects are still undefined. We hypothesized that investigation of two of the major physiological metabolites of fenretinide, N-[4-methoxyphenyl]retinamide (MPR) and 4-oxo-N-(4-hydroxyphenyl)retinamide (3-keto-HPR), might begin to resolve the multifaceted effects of this synthetic retinoid...
2017: PloS One
https://www.readbyqxmd.com/read/28448560/activity-of-xyloglucan-endotransglucosylases-hydrolases-suggests-a-role-during-host-invasion-by-the-parasitic-plant-cuscuta-reflexa
#12
Stian Olsen, Kirsten Krause
The parasitic vines of the genus Cuscuta form haustoria that grow into other plants and connect with their vascular system, thus allowing the parasite to feed on its host. A major obstacle that meets the infection organ as it penetrates the host tissue is the rigid plant cell wall. In the present study, we examined the activity of xyloglucan endotransglucosylases/hydrolases (XTHs) during the host-invasive growth of the haustorium. The level of xyloglucan endotransglucosylation (XET) activity was found to peak at the penetrating stage of Cuscuta reflexa on its host Pelargonium zonale...
2017: PloS One
https://www.readbyqxmd.com/read/28448534/intense-light-elicited-upregulation-of-mir-21-facilitates-glycolysis-and-cardioprotection-through-per2-dependent-mechanisms
#13
Colleen Marie Bartman, Yoshimasa Oyama, Kelley Brodsky, Ludmila Khailova, Lori Walker, Michael Koeppen, Tobias Eckle
A wide search for ischemic preconditioning (IPC) mechanisms of cardioprotection identified the light elicited circadian rhythm protein Period 2 (Per2) to be cardioprotective. Studies on cardiac metabolism found a key role for light elicited Per2 in mediating metabolic dependence on carbohydrate metabolism. To profile Per2 mediated pathways following IPC of the mouse heart, we performed a genome array and identified 352 abundantly expressed and well-characterized Per2 dependent micro RNAs. One prominent result of our in silico analysis for cardiac Per2 dependent micro RNAs revealed a selective role for miR-21 in the regulation of hypoxia and metabolic pathways...
2017: PloS One
https://www.readbyqxmd.com/read/28448188/effects-of-indomethacin-on-prostanoid-synthesis-and-vasomotor-responsiveness-in-endothelium-denuded-abdominal-and-thoracic-aortas-of-wistar-rats
#14
Ruth M López, Janette E López, Jorge S López, María C Castillo, Gustavo Guevara, José A Morales, Oscar A López, Jair Lozano, Enrique F Castillo
In endothelium-denuded abdominal (but not thoracic) aortas of rats, the nonselective cyclooxygenase (COX) inhibitor, indomethacin, suppressed contractions evoked by α-adrenergic agonists hypothetically mediated by prostanoids. We aimed to identify these non-endothelial-derived contractile prostanoids released by α-adrenergic receptors activation. Endothelium-denuded abdominal and thoracic aortas of Wistar rats were used for biochemical and functional analyses. Western blot analysis showed that COX-1 and COX-2 protein levels were respectively equivalent in endothelium-denuded abdominal and thoracic aortas...
2017: Clinical and Experimental Hypertension: CHE
https://www.readbyqxmd.com/read/28448045/fluorescence-based-neuraminidase-inhibition-assay-to-assess-the-susceptibility-of-influenza-viruses-to-the-neuraminidase-inhibitor-class-of-antivirals
#15
Sook-Kwan Leang, Aeron C Hurt
The neuraminidase (NA) inhibitors are the only class of antivirals approved for the treatment and prophylaxis of influenza that are effective against currently circulating strains. In addition to their use in treating seasonal influenza, the NA inhibitors have been stockpiled by a number of countries for use in the event of a pandemic. It is therefore important to monitor the susceptibility of circulating influenza viruses to this class of antivirals. There are different types of assays that can be used to assess the susceptibility of influenza viruses to the NA inhibitors, but the enzyme inhibition assays using either a fluorescent substrate or a chemiluminescent substrate are the most widely used and recommended...
April 15, 2017: Journal of Visualized Experiments: JoVE
https://www.readbyqxmd.com/read/28447754/inhibition-of-heat-shock-protein-70-intensifies-heat-stressed-damage-and-apoptosis-of-chicken-primary-myocardial-cells-in%C3%A2-vitro
#16
Jiao Xu, Shu Tang, Erbao Song, Bin Yin, Endong Bao
To investigate the potential protective effect of heat shock protein 70 (Hsp70) during heat stress (HS) in chicken primary myocardial cells (CPMC), a cellular model of low expression of Hsp70 was established using 200 µM quercetin, a specific inhibitor of Hsp70. Comparative analyses were done among a HS group, Hsp70 low expression (HS+Quercetin) group and quercetin treated only group (Quercetin) during different durations of HS (0, 1, 2, 3 and 5 h). Inhibition of Hsp70 expression in quercetin treatment groups was detected, and suggested that Hsp70 expression was inhibited significantly...
March 16, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28447739/neural-precursor-cell-expressed-developmentally-downregulated-8%C3%A2-activating-enzyme-inhibitor-mln4924-sensitizes-colorectal-cancer-cells-to-oxaliplatin-by-inducing-dna-damage-g2-cell-cycle-arrest-and-apoptosis
#17
Wanwei Zheng, Zhongguang Luo, Jun Zhang, Pei Min, Wenshuai Li, Diannan Xu, Ziqiang Zhang, Panpan Xiong, Hong Liang, Jie Liu
Oxaliplatin-based chemotherapy is a primary treatment for patients with metastatic colorectal cancer (CRC); however, its efficacy is limited. Therefore, novel therapeutic agents are urgently required. MLN4924 is a first‑in‑class inhibitor of neural precursor cell expressed, developmentally downregulated 8 (NEDD8)‑activating enzyme E1, and has entered various phase‑I/II clinical trials for cancer therapy due to its significant anticancer efficacy. The aim of the present study was to examine the synergistic effect and underlying mechanisms of MLN4924 and oxaliplatin combined treatment for CRC...
March 9, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28447479/autotaxin-inhibitors-a-patent-review-2012-2016
#18
Aikaterini Nikolaou, Maroula G Kokotou, Dimitris Limnios, Anastasia Psarra, George Kokotos
Autotaxin (ATX) is a secreted enzyme that hydrolyzes lysophosphatidylcholine to lysophosphatidic acid (LPA) and choline. The ATX/LPA axis has received increasing interest in recent years because both the enzyme ATX and the bioactive lipid LPA are involved in various pathological conditions such as tumor progression and metastasis, fibrotic diseases, autoimmune diseases, arthritis, chronic hepatitis, obesity and impaired glucose homeostasis. Thus, a great effort has been devoted in developing synthetic ATX inhibitors as new agents to treat various diseases including cancer and fibrotic diseases...
April 27, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28446877/exploring-the-role-of-cyp3a4-mediated-drug-metabolism-in-the-pharmacological-modulation-of-nitric-oxide-production
#19
José Pérez-Del Palacio, Caridad Díaz, Noemí Vergara, Francesca Algieri, Alba Rodríguez-Nogales, Nuria de Pedro, M Elena Rodríguez-Cabezas, Olga Genilloud, Julio Gálvez, Francisca Vicente
Nitric-oxide synthase, the enzyme responsible for mammalian nitric oxide generation, and cytochrome P450, the major enzymes involved in drug metabolism, share striking similarities. Therefore, it makes sense that cytochrome P450 drug mediated biotransformations might play an important role in the pharmacological modulation of nitric oxide synthase. In this work, we have undertaken an integrated in vitro assessment of the hepatic metabolism and nitric oxide modulation of previously described dual inhibitors (imidazoles and macrolides) of these enzymes in order assess the implication of CYP450 activities over production of nitric oxide...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28446809/blood-pressure-management-in-patients-with-type-2-diabetes-mellitus
#20
Hisashi Kai
Hypertension aggravates macrovascular and microvascular diseases and mortality in patients with type 2 diabetes mellitus (T2DM). The current Japanese Society of Hypertension Guidelines of the Management of Hypertension (JSH 2014) recommends that antihypertensive medication should be initiated concomitantly with lifestyle modification when blood pressure (BP) is ⩾130/80 mm Hg and that target levels of office and home BP should be <130/80 mm Hg and <125/75 mm Hg, respectively, in T2DM patients...
April 27, 2017: Hypertension Research: Official Journal of the Japanese Society of Hypertension
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