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https://www.readbyqxmd.com/read/28346881/heparin-and-homogeneous-model-heparin-oligosaccharides-form-distinct-complexes-with-protamine-light-scattering-and-zeta-potential-analysis
#1
Cynthia D Sommers, Hongping Ye, Jian Liu, Robert J Linhardt, David A Keire
Large multimolecular complexes of heparin with positively charged proteins such as platelet factor 4 (PF4) or protamine can initiate immune responses associated with heparin use in patients, including the most significant adverse event, heparin-induced thrombocytopenia (HIT). Current evidence suggests that platelet-activating antibodies that recognize large multi-molecular complexes (300-700kDa) of PF4 bound to heparin cause HIT [1] and in very rare cases anti-protamine-heparin antibodies can induce thrombocytopenia [2]...
March 14, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28346821/structure-activity-relationships-on-cynnamoyl-derivatives-as-inhibitors-of-p300-histone-acetyltransferase
#2
Valentina Noemi Madia, Rosaria Benedetti, Maria Letizia Barreca, Liza Ngo, Luca Pescatori, Antonella Messore, Giovanni Pupo, Francesco Saccoliti, Sergio Valente, Antonello Mai, Luigi Scipione, Yujun George Zheng, Cristina Tintori, Maurizio Botta, Violetta Cecchetti, Lucia Altucci, Roberto Di Santo, Roberta Costi
Human p300 is a polyhedric transcriptional coactivator, playing a crucial role by acetylating histones on specific lysine residues. A great deal of evidences shows that p300 is involved in several diseases as leukemia, tumors and viral infection. Its involvement in pleiotropic biological roles and connections to diseases provide the rationale as to how its modulation could represent an amenable drug target. Several p300 inhibitors (HATi) have been described so far, but all suffer from low potency, lack of specificity or low cell-permeability, highlighting the need to find more effective inhibitors...
March 27, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28346812/identification-of-a-novel-benzimidazole-pyrazolone-scaffold-that-inhibits-kdm4-lysine-demethylases-and-reduces-proliferation-of-prostate-cancer-cells
#3
David M Carter, Edgar Specker, Jessica Przygodda, Martin Neuenschwander, Jens Peter von Kries, Udo Heinemann, Marc Nazaré, Ulrich Gohlke
Human lysine demethylase (KDM) enzymes (KDM1-7) constitute an emerging class of therapeutic targets, with activities that support growth and development of metastatic disease. By interacting with and co-activating the androgen receptor, the KDM4 subfamily (KDM4A-E) promotes aggressive phenotypes of prostate cancer (PCa). Knockdown of KDM4 expression or inhibition of KDM4 enzyme activity reduces the proliferation of PCa cell lines and highlights inhibition of lysine demethylation as a possible therapeutic method for PCa treatment...
March 1, 2017: SLAS Discov
https://www.readbyqxmd.com/read/28346540/fragment-library-screening-identifies-hits-that-bind-to-the-non-catalytic-surface-of-pseudomonas-aeruginosa-dsba1
#4
Biswaranjan Mohanty, Kieran Rimmer, Róisín M McMahon, Stephen J Headey, Mansha Vazirani, Stephen R Shouldice, Mathieu Coinçon, Stephanie Tay, Craig J Morton, Jamie S Simpson, Jennifer L Martin, Martin J Scanlon
At a time when the antibiotic drug discovery pipeline has stalled, antibiotic resistance is accelerating with catastrophic implications for our ability to treat bacterial infections. Globally we face the prospect of a future when common infections can once again kill. Anti-virulence approaches that target the capacity of the bacterium to cause disease rather than the growth or survival of the bacterium itself offer a tantalizing prospect of novel antimicrobials. They may also reduce the propensity to induce resistance by removing the strong selection pressure imparted by bactericidal or bacteriostatic agents...
2017: PloS One
https://www.readbyqxmd.com/read/28346484/a-neighborhood-wide-association-study-nwas-example-of-prostate-cancer-aggressiveness
#5
Shannon M Lynch, Nandita Mitra, Michelle Ross, Craig Newcomb, Karl Dailey, Tara Jackson, Charnita M Zeigler-Johnson, Harold Riethman, Charles C Branas, Timothy R Rebbeck
PURPOSE: Cancer results from complex interactions of multiple variables at the biologic, individual, and social levels. Compared to other levels, social effects that occur geospatially in neighborhoods are not as well-studied, and empiric methods to assess these effects are limited. We propose a novel Neighborhood-Wide Association Study(NWAS), analogous to genome-wide association studies(GWAS), that utilizes high-dimensional computing approaches from biology to comprehensively and empirically identify neighborhood factors associated with disease...
2017: PloS One
https://www.readbyqxmd.com/read/28346236/current-concepts-in-ischemic-hepatitis
#6
Joseph M Lightsey, Don C Rockey
PURPOSE OF REVIEW: The current review seeks to define ischemic hepatitis and its associated comorbidities. It means to review the pathophysiology, clinical presentation, clinical course, outcomes, and any potential therapies. RECENT FINDINGS: Ischemic hepatitis has long been associated with cardiovascular disease; recent reports have found a substantial link between preexisting cardiovascular disease and the risk for developing ischemic hepatitis. A proposed mechanism by which hepatic congestion predisposes the liver to hemodynamic injury further defines this link...
March 24, 2017: Current Opinion in Gastroenterology
https://www.readbyqxmd.com/read/28346089/a-chemogenomic-screening-platform-used-to-identify-chemotypes-perturbing-hsp90-pathways
#7
Fiona M Thomas, Kourtney M Goode, Bartek Rajwa, Andrew B Bieberich, Larisa V Avramova, Tony R Hazbun, V Jo Davisson
Compounds that modulate the heat shock protein (HSP) network have potential in a broad range of research applications and diseases. A yeast-based liquid culture assay that measured time-dependent turbidity enabled the high-throughput screening of different Saccharomyces cerevisae strains to identify HSP modulators with unique molecular mechanisms. A focused set of four strains, with differing sensitivities to Hsp90 inhibitors, was used to screen a compound library of 3680 compounds. Computed turbidity curve functions were used to classify strain responses and sensitivity to chemical effects across the compound library...
January 1, 2017: SLAS Discov
https://www.readbyqxmd.com/read/28345007/partial-occupancy-binders-identified-by-the-pan-dataset-density-analysis-method-offer-new-chemical-opportunities-and-reveal-cryptic-binding-sites
#8
Nicholas M Pearce, Anthony R Bradley, Tobias Krojer, Brian D Marsden, Charlotte M Deane, Frank von Delft
Crystallographic fragment screening uses low molecular weight compounds to probe the protein surface and although individual protein-fragment interactions are high quality, fragments commonly bind at low occupancy, historically making identification difficult. However, our new Pan-Dataset Density Analysis method readily identifies binders missed by conventional analysis: for fragment screening data of lysine-specific demethylase 4D (KDM4D), the hit rate increased from 0.9% to 10.6%. Previously unidentified fragments reveal multiple binding sites and demonstrate: the versatility of crystallographic fragment screening; that surprisingly large conformational changes are possible in crystals; and that low crystallographic occupancy does not by itself reflect a protein-ligand complex's significance...
May 2017: Structural Dynamics (Melville, N.Y.)
https://www.readbyqxmd.com/read/28344030/antibacterial-activity-of-medicinal-plants-from-the-physicians-of-myddvai-a-13-th-century-welsh-medical-manuscript
#9
Charles Wagner, Jillian De Gezelle, Maureen Robertson, Keith Robertson, Mickey Wilson, Slavko Komarnytsky
ETHNOPHARMACOLOGICAL RELEVANCE: Antimicrobial drug resistance is a growing threat to global public health. Historical records and herbal texts relating to traditional Celtic medicine indicate an extensive pharmacopeia of plants for treating infections likely caused by microbes. However, a major barrier for successful integration of these remedies into mainstream practice is the current lack of accurate interpretation and scientific validation. MATERIALS AND METHODS: We applied Mobile Discovery approach to the Isle of Arran, Scotland, for in situ targeted screening of 83 out of 138 plants identified in Meddygion Myddvai (a 13(th) century Welsh manuscript) to treat conditions related to microbial infections, and an additional 18 plants from modern ethnobotanical knowledge on the island...
March 24, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28343875/discovery-and-structure-activity-relationship-studies-of-n-substituted-indole-derivatives-as-novel-mcl-1-inhibitors
#10
Shenglin Luan, Qi Ge, Yedong Chen, Mingyang Dai, Jinyu Yang, Kun Li, Dan Liu, Linxiang Zhao
Myeloid cell leukemia-1 (Mcl-1) is an important antiapoptotic protein functioning through protein-protein interactions. We discovered LSL-A6 (2-((2-carbamoyl-1-(3-(4-methoxyphenoxy)propyl)-1H-indol-6-yl)oxy)acetic acid) with a novel N-substituted indole scaffold to interfere Mcl-1 binding as a novel Mcl-1 inhibitor. Molecular modeling indicated that this compound binds with Mcl-1 by interaction with P2 and R263 hot-spots. Structure modification focused on several moieties including indole core, hydrophobic tail and acidic chain were conducted and structure-activity relationship was analyzed...
March 16, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28343446/responding-to-aggression-and-reactive-behaviours-in-the-home
#11
Rachel V Herron, Mark W Rosenberg
Behaviours such as hitting, spitting, swearing and kicking can be a common response to personal, social and environmental challenges experienced by people with dementia. Little attention, however, has been given to how partners in care experience and respond to these behaviours in the home. This paper examines the emerging theme of 'aggression,' in seven interviews with nine former partners in care of people with dementia in Ontario, Canada. We explore how partners in care talk about, interpret and respond to these behaviours drawing on recent conceptualizations of structural and interpersonal violence in health and social geography and contributing to the growing body of research on relational care...
January 1, 2017: Dementia
https://www.readbyqxmd.com/read/28343116/health-and-weight-gender-specific-linkages-under-heterogeneity-interdependence-and-resilience-factors
#12
Olaf Hübler
Many studies have shown that obesity is a serious health problem for our society. Empirical analyses often neglect a number of methodological issues and relevant influences on health. This paper investigates empirically whether neglecting these items leads to systematically different estimates. Based on data from the German Socio-Economic Panel, this study derives the following results. (1) Many combinations of weight and height lead to the same health status. (2) The relationship between health and body mass index is nonlinear...
March 11, 2017: Economics and Human Biology
https://www.readbyqxmd.com/read/28342383/own-attractiveness-and-perceived-relationship-quality-shape-sensitivity-in-women-s-memory-for-other-men-on-the-attractiveness-dimension
#13
Christopher D Watkins, Mike J Nicholls, Carlota Batres, Dengke Xiao, Sean Talamas, David I Perrett
Although recent work suggests that opposite-sex facial attractiveness is less salient in memory when individuals are in a committed romantic relationship, romantic relationship quality can vary over time. In light of this, we tested whether activating concerns about romantic relationship quality strengthens memory for attractive faces. Partnered women were exposed briefly to faces manipulated in shape cues to attractiveness before either being asked to think about a moment of emotional closeness or distance in their current relationship...
March 22, 2017: Cognition
https://www.readbyqxmd.com/read/28341402/inhibitors-of-protein-arginine-deiminases-and-their-efficacy-in-animal-models-of-multiple-sclerosis
#14
Amit Sarswat, Ewa Wasilewski, Sai K Chakka, Angelica M Bello, Andrew V Caprariello, Chithra M Muthuramu, Peter K Stys, Shannon E Dunn, Lakshmi P Kotra
Protein arginine deiminases (PAD) are implicated in a variety of inflammatory and neurodegenerative diseases including multiple sclerosis (MS). Following the discovery of an in silico hit containing hydantoin and a piperidine moiety, we hypothesized that a 2-carbon linker on the hydantoin would be necessary for a 5-membered heterocycle for optimal PAD inhibitory activity. We designed thirteen compounds as potential inhibitors of PAD2 and PAD4 enzymes-two important PAD enzymes implicated in MS. Two compounds, one with an imidazole moiety (22) and the other with a tetrazole moiety (24) showed good inhibition of PAD isozymes in vitro and in the EAE mouse model of MS in vivo...
March 6, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28340400/pharmacoinformatics-exploration-of-polyphenol-oxidases-leading-to-novel-inhibitors-by-virtual-screening-and-molecular-dynamic-simulation-study
#15
Mubashir Hassan, Qamar Abbas, Zaman Ashraf, Ahmed A Moustafa, Sung-Yum Seo
Polyphenol oxidases (PPOs)/tyrosinases are metal-dependent enzymes and known as important targets for melanogenesis. Although considerable attempts have been conducted to control the melanin-associated diseases by using various inhibitors. However, the exploration of the best anti-melanin inhibitor without side effect still remains a challenge in drug discovery. In present study, protein structure prediction, ligand-based pharmacophore modeling, virtual screening, molecular docking and dynamic simulation study were used to screen the strong novel inhibitor to cure melanogenesis...
March 15, 2017: Computational Biology and Chemistry
https://www.readbyqxmd.com/read/28340238/cigarette-smoke-exposure-worsens-endotoxin-induced-lung-injury-and-pulmonary-edema-in-mice
#16
Jeffrey E Gotts, Jason Abbott, Xiaohui Fang, Haru Yanagisawa, Naoki Takasaka, Stephen L Nishimura, Carolyn S Calfee, Michael A Matthay
Introduction: Cigarette smoking (CS) remains a major public health concern and has recently been associated with an increased risk of developing acute respiratory distress syndrome (ARDS). Bronchoalveolar lavage (BAL) experiments in human volunteers have demonstrated that active smokers develop increased alveolar-epithelial barrier permeability to protein after inhaling lipopolysaccharide (LPS). Here we tested the hypothesis that short-term whole-body CS exposure would increase LPS-induced lung edema in mice...
March 9, 2017: Nicotine & Tobacco Research: Official Journal of the Society for Research on Nicotine and Tobacco
https://www.readbyqxmd.com/read/28339199/structure-based-discovery-of-new-antagonist-and-biased-agonist-chemotypes-for-the-kappa-opioid-receptor
#17
Zhong Zheng, Xi-Ping Huang, Thomas J Mangano, Rodger Zou, Xin Chen, Saheem Zaidi, Bryan L Roth, Raymond C Stevens, Vsevolod Katritch
The ongoing epidemics of opioid overdose raises an urgent need for effective anti-addiction therapies and addiction-free painkillers. The κ-opioid receptor (KOR) has emerged as a promising target for both indications, raising demand for new chemotypes of KOR antagonists, as well as G-protein-biased agonists. We employed the crystal structure of the KOR-JDTic complex and ligand-optimized structural templates to perform virtual screening of available compound libraries for new KOR ligands. The prospective virtual screening campaign yielded a high 32% hit rate, identifying novel fragment-like and lead-like chemotypes of KOR ligands...
March 24, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28338323/shape-dependent-radiosensitization-effect-of-gold-nanostructures-in-cancer-radiotherapy-comparison-of-gold-nanoparticles-nanospikes-and-nanorods
#18
Ningning Ma, Fu-Gen Wu, Xiaodong Zhang, Yao-Wen Jiang, Hao-Ran Jia, Hong-Yin Wang, Yan-Hong Li, Peidang Liu, Ning Gu, Zhan Chen
The shape effect of gold (Au) nanomaterials on the efficiency of cancer radiotherapy has not been fully elucidated. To address this issue, Au nanomaterials with different shapes but similar average size (~50 nm) including gold nanoparticles (GNPs), gold nanospikes (GNSs), and gold nanorods (GNRs) were synthesized and functionalized with poly(ethylene glycol) (PEG) molecules. Although all these Au nanostructures were coated with the same PEG molecules, their cellular uptake behavior differed significantly. The GNPs showed the highest cellular responses compared to the GNSs and the GNRs (based on the same gold mass) after incubation with KB cancer cells for 24 h...
March 24, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28338290/identification-of-natural-inhibitors-of-bcr-abl-for-the-treatment-of-chronic-myeloid-leukemia
#19
Phani Krishna, Sailu Sarvagalla, Bindu Madhuri, Sankar Pajaniradje, Vinitha Baskaran, Mohane Selvaraj Coumar, R Baskaran
Chronic myeloid leukemia (CML) is a clonal myeloproliferative disorder of the hematopoietic stem cells, characterized at the molecular level by the bcr/abl gene rearrangement. Even though targeting the fusion gene product Bcr-Abl protein is a successful strategy, development of drug resistance and drug intolerance are currently the limitations for Bcr-Abl targeted CML therapy. With an aim to develop natural Bcr-Abl inhibitors, we performed virtual screening (VS) of ZINC natural compound database by docking with Abl kinase using Glide software...
March 24, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28337675/an-ontology-based-search-engine-for-digital-reconstructions-of-neuronal-morphology
#20
Sridevi Polavaram, Giorgio A Ascoli
Neuronal morphology is extremely diverse across and within animal species, developmental stages, brain regions, and cell types. This diversity is functionally important because neuronal structure strongly affects synaptic integration, spiking dynamics, and network connectivity. Digital reconstructions of axonal and dendritic arbors are thus essential to quantify and model information processing in the nervous system. NeuroMorpho.Org is an established repository containing tens of thousands of digitally reconstructed neurons shared by several hundred laboratories worldwide...
March 23, 2017: Brain Informatics
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