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https://www.readbyqxmd.com/read/28535045/bet-bromodomain-inhibitors-with-one-step-synthesis-discovered-from-virtual-screen
#1
Alex M Ayoub, Laura M L Hawk, Ryan J Herzig, Jiewei Jiang, Andrea J Wisniewski, Clifford T Gee, Peiliang Zhao, Jin-Yi Zhu, Norbert Berndt, Nana K Offei-Addo, Thomas G Scott, Jun Qi, James E Bradner, Timothy R Ward, Ernst Schönbrunn, Gunda I Georg, William C K Pomerantz
Chemical inhibition of epigenetic regulatory proteins BrdT and Brd4 is emerging as a promising therapeutic strategy in contraception, cancer, and heart disease. We report an easily synthesized dihydropyridopyrmidine pan-BET inhibitor scaffold, which was uncovered via a virtual screen followed by testing in a fluorescence anisotropy assay. Dihydropyridpyimidine 3 was subjected to further characterization and is highly selective for the BET family of bromodomains. Structure-activity relationship data and ligand deconstruction highlight the importance of the substitution of the uracil moiety for potency and selectivity...
May 23, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28534698/effect-of-parathyroid-hormone-on-healing-in-osteoporotic-fractures-via-a-phospholipase-c-independent-pathway
#2
Wei-Long Li, Xiao Yu, Zhi-Ping Huang, Qing-Jiang Pang
Objective This study was performed to investigate the effect of parathyroid hormone (PTH) on healing in osteoporotic fractures via a phospholipase C (PLC)-independent pathway and explore the mechanism of PTH-mediated bone formation. Methods Ninety-six 12-week-old C57BL/6J female mice underwent bilateral ovariectomy. One month later, the lower third of the femur was fractured and the mice were treated using saline, PTH(1-28), PTH(1-34), zoledronic acid (ZA), PTH(1-28)+ZA, and PTH(1-34)+ZA. The mice were killed at weeks 2 and 4 in each group...
January 1, 2017: Journal of International Medical Research
https://www.readbyqxmd.com/read/28532408/bone-turnover-and-periprosthetic-bone-loss-after-cementless-total-hip-arthroplasty-can-be-restored-by-zoledronic-acid-a-prospective-randomized-open-label-controlled-trial
#3
Tsan-Wen Huang, Chao-Jan Wang, Hsin-Nung Shih, Yuhan Chang, Kuo-Chin Huang, Kuo-Ti Peng, Mel S Lee
BACKGROUND: Although the loss of bone mineral density (BMD) after total hip arthroplasty (THA) is a known problem, it remains unresolved. This study prospectively examined the effect of zoledronic acid (ZA) on bone turnover and BMD after cementless THA. METHODS: Between January 2010 and August 2011, 60 patients who underwent cementless THA were randomly assigned to receive either ZA infusion or placebo (0.9% normal saline only) postoperatively. ZA was administered at 2 day and 1 year postoperatively...
May 22, 2017: BMC Musculoskeletal Disorders
https://www.readbyqxmd.com/read/28530646/the-relevance-of-the-age-of-transfused-blood-for-prognosis-after-transcatheter-aortic-valve-implantation-tavi
#4
Katarzyna Czerwińska-Jelonkiewicz, Magdalena Łętowska, Adam Witkowski, Walerian Piotrowski, Marta Załęska-Kocięcka, Janina Stępińska
INTRODUCTION    Blood transfusion after transcatheter aortic valve implantation (TAVI) is frequently required due to the high vulnerability of TAVI population and procedure related bleeding.  OBJECTIVES    We quantified the impact of post-procedural blood transfusion and the age of transfused red blood cells (RBC) units on prognosis after TAVI.  PATIENTS AND METHODS    This was a single-center, observational analysis conducted between 2009-2014. The adopted end points were early and long-term mortality after TAVI...
May 22, 2017: Polish Archives of Internal Medicine
https://www.readbyqxmd.com/read/28529150/preventive-effect-of-phosphodiesterase-inhibitor-pentoxifylline-against-medication-related-osteonecrosis-of-the-jaw-an-animal-study
#5
Gül Merve Yalcin-Ulker, Alev Cumbul, Gonca Duygu-Capar, Ünal Uslu, Kemal Sencift
PURPOSE: The aim of this experimental study was to investigate the prophylactic effect of pentoxifylline (PTX) on medication-related osteonecrosis of the jaw (MRONJ). MATERIALS AND METHODS: Female Sprague-Dawley rats (n = 33) received zoledronic acid (ZA) for 8 weeks to create an osteonecrosis model. The left mandibular second molars were extracted and the recovery period lasted 8 weeks before sacrifice. PTX was intraperitoneally administered to prevent MRONJ...
April 26, 2017: Journal of Oral and Maxillofacial Surgery
https://www.readbyqxmd.com/read/28501938/zoledronic-acid-renders-human-m1-and-m2-macrophages-susceptible-to-v%C3%AE-2-%C3%AE-%C3%AE-t-cell-cytotoxicity-in-a-perforin-dependent-manner
#6
Daniel W Fowler, John Copier, Angus G Dalgleish, Mark D Bodman-Smith
Vδ2(+) T cells are a subpopulation of γδ T cells in humans that are cytotoxic towards cells which accumulate isopentenyl pyrophosphate. The nitrogen-containing bisphosphonate, zoledronic acid (ZA), can induce tumour cell lines to accumulate isopentenyl pyrophosphate, thus rendering them more susceptible to Vδ2(+) T cell cytotoxicity. However, little is known about whether ZA renders other, non-malignant cell types susceptible. In this study we focussed on macrophages (Mϕs), as these cells have been shown to take up ZA...
May 13, 2017: Cancer Immunology, Immunotherapy: CII
https://www.readbyqxmd.com/read/28492229/imaging-of-ph-in-vivo-using-hyperpolarized-13-c-labelled-zymonic-acid
#7
Stephan Düwel, Christian Hundshammer, Malte Gersch, Benedikt Feuerecker, Katja Steiger, Achim Buck, Axel Walch, Axel Haase, Steffen J Glaser, Markus Schwaiger, Franz Schilling
Natural pH regulatory mechanisms can be overruled during several pathologies such as cancer, inflammation and ischaemia, leading to local pH changes in the human body. Here we demonstrate that (13)C-labelled zymonic acid (ZA) can be used as hyperpolarized magnetic resonance pH imaging sensor. ZA is synthesized from [1-(13)C]pyruvic acid and its (13)C resonance frequencies shift up to 3.0 p.p.m. per pH unit in the physiological pH range. The long lifetime of the hyperpolarized signal enhancement enables monitoring of pH, independent of concentration, temperature, ionic strength and protein concentration...
May 11, 2017: Nature Communications
https://www.readbyqxmd.com/read/28477013/self-assembling-nanoparticles-encapsulating-zoledronic-acid-inhibit-mesenchymal-stromal-cells-differentiation-migration-and-secretion-of-proangiogenic-factors-and-their-interactions-with-prostate-cancer-cells
#8
Cinzia Borghese, Naike Casagrande, Eliana Pivetta, Alfonso Colombatti, Mariarosaria Boccellino, Ezven Amler, Nicola Normanno, Michele Caraglia, Giuseppe De Rosa, Donatella Aldinucci
Zoledronic Acid (ZA) rapidly concentrates into the bone and reduces skeletal-related events and pain in bone metastatic prostate cancer (PCa), but exerts only a limited or absent impact as anti-cancer activity. Recently, we developed self-assembling nanoparticles (NPS) encapsulating zoledronic acid (NZ) that allowed a higher intratumor delivery of the drug compared with free zoledronic acid (ZA) in in vivo cancer models of PCa. Increasing evidence suggests that Bone Marrow (BM) Mesenchymal stromal cells (BM-MSCs) are recruited into the stroma of developing tumors where they contribute to progression by enhancing tumor growth and metastasis...
April 19, 2017: Oncotarget
https://www.readbyqxmd.com/read/28466681/a-computational-insight-into-binding-modes-of-inhibitors-xd29-xd35-and-xd28-to-bromodomain-containing-protein-4-based-on-molecular-dynamics-simulations
#9
Jing Su, Xinguo Liu, Shaolong Zhang, Fangfang Yan, Qinggang Zhang, Jianzhong Chen
In the current work, conformational changes of bromodomain-containing protein 4 (1) (BRD4-1) induced by bindings of inhibitors XD29 (57G), XD35 (57F), and XD28 (L28) were investigated using molecular dynamics (MD) simulations and principal component analysis. The results demonstrate that inhibitor bindings produce significant effect on the motion of ZA loop in BRD4-1. Moreover, to further study binding modes of three inhibitors to BRD4-1, binding free energies of inhibitors to BRD4-1 were also calculated using molecular mechanics Poisson-Boltzmann surface area (MM-PBSA) method...
May 3, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/28461254/combination-sclerostin-antibody-and-zoledronic-acid-treatment-outperforms-either-treatment-alone-in-a-mouse-model-of-osteogenesis-imperfecta
#10
David G Little, Lauren Peacock, Kathy Mikulec, Michaela Kneissel, Ina Kramer, Tegan L Cheng, Aaron Schindeler, Craig Munns
In this study, we examined the therapeutic potential of anti-Sclerostin Antibody (Scl-Ab) and bisphosphonate treatments for the bone fragility disorder Osteogenesis Imperfecta (OI). Mice with the Amish OI mutation (Col1a2 G610C mice) and control wild type littermates (WT) were treated from week 5 to week 9 of life with (1) saline (control), (2) zoledronic acid given 0.025mg/kg s.c. weekly (ZA), (3) Scl-Ab given 50mg/kg IV weekly (Scl-Ab), or (4) a combination of both (Scl-Ab/ZA). Functional outcomes were prioritized and included bone mineral density (BMD), bone microarchitecture, long bone bending strength, and vertebral compression strength...
April 29, 2017: Bone
https://www.readbyqxmd.com/read/28458102/ivabradine-attenuates-the-anticonvulsant-potency-of-lamotrigine-but-not-that-of-lacosamide-pregabalin-and-topiramate-in-the-tonic-clonic-seizure-model-in-mice
#11
Katarzyna M Sawicka, Katarzyna Załuska, Agnieszka Wawryniuk, Karolina Załuska-Patel, Michał Szczyrek, Bartłomiej Drop, Jadwiga Daniluk, Monika Szpringer, Dorota Żółkowska, Jarogniew J Łuszczki
Hyperpolarization-activated cyclic nucleotide-gated (HCN) channels are involved not only in synaptic transmission and neuronal excitability under physiological conditions, but also in seizure activity. To determine the influence of ivabradine (an HCN channel inhibitor) on the anticonvulsant potency of four novel antiepileptic drugs (AEDs: lacosamide, lamotrigine, pregabalin and topiramate) in the mouse maximal electroshock-induced seizure (MES) model. Adult male albino Swiss mice were challenged with maximal electroconvulsions (electric current of 25mA delivered via auricular electrodes)...
April 22, 2017: Epilepsy Research
https://www.readbyqxmd.com/read/28433475/targeted-population-screening-of-late-onset-pompe-disease-in-unspecified-myopathy-patients-for-korean-population
#12
Jung Hwan Lee, Jin-Hong Shin, Hyung Jun Park, Sook Za Kim, Young Mi Jeon, Hye Kyoung Kim, Dae-Seong Kim, Young-Chul Choi
We performed targeted population screening of late onset Pompe disease (LOPD) in unspecified myopathy patients, because early diagnosis is difficult due to its heterogeneous clinical features. We prospectively enrolled 90 unrelated myopathic patients who had one or more signs out of five LOPD-like clinical findings (proximal weakness, axial weakness, lingual weakness, respiratory difficulty, idiopathic hyperCKemia). Acid alpha glucosidase activity was evaluated with dried blood spot and mixed leukocyte simultaneously...
June 2017: Neuromuscular Disorders: NMD
https://www.readbyqxmd.com/read/28430124/association-between-serum-selenium-concentrations-and-levels-of-proinflammatory-and-profibrotic-cytokines-interleukin-6-and-growth-differentiation-factor-15-in-patients-with-alcoholic-liver-cirrhosis
#13
Andrzej Prystupa, Paweł Kiciński, Dorota Luchowska-Kocot, Anna Błażewicz, Jarosław Niedziałek, Grzegorz Mizerski, Mariusz Jojczuk, Andrzej Ochal, Jarosław J Sak, Wojciech Załuska
According to some authors, serum selenium levels are strongly associated with the severity of liver diseases, including liver cirrhosis. The aim of this study was to determine the relationship between the concentration of selenium and pro-inflammatory and profibrotic cytokines-interleukin-6 (IL-6) and growth differentiation factor 15 (GDF-15) in patients with alcoholic liver cirrhosis. The parameters studied were determined in the serum of 99 patients with alcoholic liver cirrhosis divided based on the severity of disease according to the Child-Turcotte-Pugh criteria...
April 21, 2017: International Journal of Environmental Research and Public Health
https://www.readbyqxmd.com/read/28422387/should-we-be-putting-our-scalpel-down-is-hifu-the-answer-to-fertility-sparing-fibroid-treatment
#14
Nicola Tempest, Dharani Hapangama
Despite HIFU being a fertility sparing, outpatient procedure reported to be safe and effective in treating patients with fibroids for 15 years (Wang et al. Zhonghua Chao Sheng Ying Xiang Xue Za Zhi 2002; 11:161-63); approved by the FDA in America in 2004; and seen to have similar cost-effectiveness as all other uterine preserving treatments; it is currently only available in two private treatment centers and on a case by case basis on the NHS in the UK and not consistently covered by any major US insurance company...
April 19, 2017: BJOG: An International Journal of Obstetrics and Gynaecology
https://www.readbyqxmd.com/read/28412244/a-central-role-for-cadherin-signaling-in-cancer
#15
REVIEW
Antonis Kourtidis, Ruifeng Lu, Lindy J Pence, Panos Z Anastasiadis
Cadherins are homophilic adhesion molecules with important functions in cell-cell adhesion, tissue morphogenesis, and cancer. In epithelial cells, E-cadherin accumulates at areas of cell-cell contact, coalesces into macromolecular complexes to form the adherens junctions (AJs), and associates via accessory partners with a subcortical ring of actin to form the apical zonula adherens (ZA). As a master regulator of the epithelial phenotype, E-cadherin is essential for the overall maintenance and homeostasis of polarized epithelial monolayers...
April 12, 2017: Experimental Cell Research
https://www.readbyqxmd.com/read/28392837/denosumab-treatment-in-the-management-of-patients-with-advanced-prostate-cancer-clinical-evidence-and-experience
#16
REVIEW
Miriam Hegemann, Jens Bedke, Arnulf Stenzl, Tilman Todenhöfer
Osteoprotective therapies have become an essential component in the management of advanced prostate cancer (PC) patients as bone metastases (BMs) have a major impact on morbidity and mortality. Denosumab is a fully humanized antibody targeting the receptor activator of nuclear factor κB ligand (RANKL), which has been approved by the European Medicines Agency (EMA) in Europe and the United States (US) Food and Drug Administration (FDA) in the US for prevention of skeletal-related events (SREs) in patients with solid tumors and BMs, including PC...
March 2017: Therapeutic Advances in Urology
https://www.readbyqxmd.com/read/28390132/a-5-year-retrospective-longitudinal-study-on-the-incidence-and-the-risk-factors-of-osteonecrosis-of-the-jaws-in-patients-treated-with-zoledronic-acid-for-bone-metastases-from-solid-tumors
#17
M Manfredi, G Mergoni, M Goldoni, S Salvagni, E Merigo, M Meleti, P Vescovi
BACKGROUND: The aim of this study was to evaluate the incidence and the risk factors of osteonecrosis of the jaw (ONJ) in a group of patients treated with zoledronic acid (ZA) for bone metastases from solid tumors and enrolled in a preventive dental program. MATERIAL AND METHODS: This 5-year retrospective longitudinal study included all consecutive oncological patients who underwent at least one infusion with ZA between 2004 and 2011 for bone metastases due to solid neoplasms...
May 1, 2017: Medicina Oral, Patología Oral y Cirugía Bucal
https://www.readbyqxmd.com/read/28387418/delineating-the-role-of-ripples-on-the-thermal-expansion-of-2d-honeycomb-materials-graphene-2d-h-bn-and-monolayer-ml-mos2
#18
P Anees, M C Valsakumar, B K Panigrahi
We delineated the role of thermally excited ripples on the thermal expansion properties of 2D honeycomb materials (free-standing graphene, 2D h-BN, and ML-MoS2), by explicitly carrying out three-dimensional (3D) and two-dimensional (2D) molecular dynamics simulations. In 3D simulations, the in-plane lattice parameter (a-lattice) of graphene and 2D h-BN shows thermal contraction over a wide range of temperatures and exhibits a strong system size dependence. The 2D simulations of the very same system show a reverse trend, where the a-lattice expands in the whole computed temperature range...
April 19, 2017: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/28349704/lc-esi-ms-ms-profiling-of-phenolics-in-the-leaves-of-eleutherococcus-senticosus-cultivated-in-the-west-europe-and-anti-hyaluronidase-and-anti-acetylcholinestarase-activities
#19
Rafał Kuźniewski, Daniel Załuski, Marta Olech, Piotr Banaszczak, Renata Nowak
Neither secondary metabolites of the spring leaves nor the autumn leaves of Eleutherococcus senticosus species cultivated in Poland, or the bioactivity are known. The richest in polyphenols was the autumn leaves (171.1 mg/g DE), while in flavonoids the spring leaves (107.9 mg/g DE). Using LC-ESI-MS/MS, protocatechuic acid has been identified as the most abundant compound in the spring and autumn leaves (200 and 70 μg/g DE, respectively). Amongst flavonoids, naringenin 7-O-glucoside occurred in the largest amount (20 and 10 mg/g DE in the spring and autumn leaves, respectively)...
March 28, 2017: Natural Product Research
https://www.readbyqxmd.com/read/28345127/zoledronate-promotes-bone-formation-by-blocking-osteocyte-osteoblast-communication-during-bone-defect-healing
#20
Pingping Cui, Hongrui Liu, Jing Sun, Norio Amizuka, Qinfeng Sun, Minqi Li
Nitrogen-containing bisphosphonates (N-BPs) are potent antiresorptive drugs and their actions on osteoclasts have been studied extensively. Recent studies have suggested that N-BPs also target bone-forming cells. However, the precise mechanism of N-BPs in osteoblasts is paradoxical, and the specific role of osteocytes is worthy of in-depth study. Here, we investigated the cellular mechanisms of N-BPs regulating bone defect healing by zoledronate (ZA). Bone histomorphometry confirmed an increase in new bone formation by systemic ZA administration...
March 27, 2017: Histology and Histopathology
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