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Claire Beaufay, Allison Ledoux, Olivia Jansen, Annélise Bordignon, Senzhi Zhao, Christiana N Teijaro, Rodrigo B Andrade, Joëlle Quetin-Leclercq, Michel Frédérich
Strychnogucine B is a bisindole alkaloid previously isolated from Strychnos icaja that possesses promising in vitro antiplasmodial properties. This compound was synthesized in four steps from (-)-strychnine. As no acute toxicity was observed at the highest tested cumulative dose of 60 mg/kg, its in vivo antimalarial activity was determined intraperitoneally at 30 mg/kg/d in a Plasmodium berghei murine model. In the Peters's 4-d suppressive test, this alkaloid suppressed the parasitaemia by almost 36% on day 5 and 60% on day 7 compared to vehicle-treated mice...
June 21, 2018: Planta Medica
William F Porto, Isabel C M Fensterseifer, Suzana M Ribeiro, Octavio L Franco
The rise of bacterial resistance makes it necessary to find innovative alternatives to control bacterial infections. Antimicrobial peptides (AMPs) have been considered as the new generation of antimicrobial agents. Based on the fact that AMPs are sequence-dependent, a linguistic model for designing AMPs was previously developed. That model considers AMPs as a formal language with a grammar (patterns or motifs) and a vocabulary (amino acids). Albeit promising, that model has been poorly exploited mainly because it generates thousands of sequences, and the outcome has high similarity to already known AMPs...
June 18, 2018: Biochimica et Biophysica Acta
Davina C M Simoes, Ioannis Vogiatzis
Patients with stable chronic obstructive pulmonary disease (COPD) frequently exhibit unintentional accentuated peripheral muscle loss and dysfunction. Skeletal muscle mass in these patients is a strong independent predictor of morbidity and mortality. Factors including protein anabolism/catabolism imbalance, hypoxia, physical inactivity, inflammation, and oxidative stress are involved in the initiation and progression of muscle wasting in these patients. Exercise training remains the most powerful intervention for reversing, in part, muscle wasting in COPD...
May 2018: Journal of Thoracic Disease
Xudong Shen, Guilian Cheng, Liming Xu, Wei Wu, Zhengrong Chen, Peng Du
Jumonji AT-rich interactive domain 1B (JARID1B) has been revealed to remove methyl residues from methylated lysine 4 on histone H3 (H3K4) and has also been reported to be associated with the progression of numerous types of tumor. However, its roles and mechanisms in pancreatic cancer (PC) remain unknown. The present study demonstrated that JARID1B is elevated in PC and is associated with the growth of pancreatic tumors. Overexpression of JARID1B significantly promoted the proliferation in vitro and tumor formation in vivo of PC cells...
July 2018: Oncology Letters
Thomas N Kakuda, Jeysen Yogaratnam, Jennifer Rito, Malcolm Boyce, Toni Mitchell, Kusum Gupta, Julian A Symons, Sushmita Chanda, Pieter Van Remoortere, John Fry
BACKGROUND: This double-blind, first-in-human phase 1 study evaluated pharmacokinetics, safety and tolerability of AL-794 (prodrug of ALS-033719), a potent endonuclease inhibitor of influenza A and B in healthy volunteers. METHODS: Healthy adult volunteers were randomized to AL-794 (50-2000 mg single ascending doses, fasting) or placebo (5 cohorts, n=6:2 AL-794: placebo/cohort) in part 1, and AL-794 (50-600 mg multiple ascending doses, twice-daily, fed or fasted) or placebo (3 cohorts, n=8:2 AL-794: placebo/cohort) for 7 days in part 2...
June 21, 2018: Antiviral Therapy
Petr Popov, Yao Peng, Ling Shen, Raymond C Stevens, Vadim Cherezov, Zhi-Jie Liu, Vsevolod Katritch
Engineering of GPCR constructs with improved thermostability is a key for successful structural and biochemical studies of this transmembrane protein family, targeted by 40% of all therapeutic drugs. Here we introduce a comprehensive computational approach to effective prediction of stabilizing mutations in GPCRs, named CompoMug, which employs sequence-based analysis, structural information, and a derived machine learning predictor. Tested experimentally on the serotonin 5-HT2C receptor target, CompoMug predictions resulted in 10 new stabilizing mutations, with an apparent thermostability gain ~8...
June 21, 2018: ELife
Akshay Moharir, Lincoln Gay, Daniel Appadurai, James Keener, Markus Babst
Eisosomes are lipid domains of the yeast plasma membrane that share similarities to caveolae of higher eukaryotes. Eisosomes harbor APC-type nutrient transporters for reasons which are poorly understood. Our analyses support the model that eisosomes function as storage compartments, keeping APC transporters in a stable, inactive state. By regulating eisosomes, yeast is able to balance the number of proton-driven APC transporters with the proton pumping activity of Pma1, thereby maintaining the plasma membrane proton gradient...
June 21, 2018: Molecular Biology of the Cell
Kent Pekel, Eugene C Roehlkepartain, Amy K Syvertsen, Peter C Scales, Theresa K Sullivan, Jenna Sethi
Comments on an article by Megan M. Julian & Junlei Li (see record 2012-10324-001). Junlei Li and Megan Julian argued that a major and under appreciated factor in the success and failure of interventions intended to improve the lives of children and youth at risk is the degree to which those interventions promote what the authors called developmental relationships . They asserted that "developmental interventions produce desirable outcomes if and only if such interventions enhanced developmental relationships"...
June 21, 2018: American Journal of Orthopsychiatry
Charlotte B Thorup, Mette Hougaard, Pernille F Blindum, Erik E Sørensen
Surgical site infections that develop after vascular and cardiac surgery are often treated with Negative Pressure Wound Therapy (NPWT). Due to the severity of the infection and risk of bleeding, this NPWT often requires hospitalisation. Fourteen patients were selected for qualitative interviews to investigate their experiences and the meaning of patient participation during hospitalisation with NPWT. Results show that hospitalisation induces tension between an intrusion of privacy and being part of a community...
June 21, 2018: International Wound Journal
Frederik Rainer Ehrmann, Jorna Kalim, Toni Pfaffeneder, Bruno Bernet, Christoph Hohn, Elisabeth Schäfer, Thomas Botzanowski, Sarah Cianférani Cianférani, Andreas Heine, Klaus Reuter, François Diederich, Gerhard Klebe
The enzyme tRNA guanine transglycosylase, a target to fight Shigellosis, recognizes tRNA only as a homodimer and performs full nucleobase exchange at the wobble position. Active-site inhibitors block the enzyme function by competitively replacing tRNA. In solution, the wild-type homodimer dissociates only marginally, whereas mutated variants show substantial monomerization in solution. Surprisingly, one inhibitor transforms of the protein into a twisted state, whereby one monomer unit rotates by approximately 130°...
June 21, 2018: Angewandte Chemie
Fay Sibley, Francesca Thompson, Andrea Carter, Michael Hurley
No abstract text is available yet for this article.
July 2018: Perspectives in Public Health
Duan Wenchao, Peina Zhang, Yujiao Xiahou, Yahui Song, Cuixia Bi, Jie Zhan, Wei Du, Lihui Huang, Helmuth Möhwald, Haibing Xia
It is well known that the activity and stability of electrocatalysts are largely dependent on their surface facets. In this work, we have successfully regulated surface facets of three-dimensional (3D) metallic Aum-n aerogels by salt-induced assembly of citrate-stabilized gold nanoparticles (Au NPs) of two different sizes and further size-dependent localized Ostwald ripening at controlled particle-number ratios, where m and n represent the size of Au NPs, respectively. In addition, 3D Aum-n @Pd aerogels were further synthesized on the basis of Aum-n aerogels and also bear controlled surface facets due to the formation of ultrathin Pd layers on Aum-n aerogels...
June 21, 2018: ACS Applied Materials & Interfaces
Nipun Shrestha, Katriina T Kukkonen-Harjula, Jos H Verbeek, Sharea Ijaz, Veerle Hermans, Zeljko Pedisic
BACKGROUND: A large number of people are employed in sedentary occupations. Physical inactivity and excessive sitting at workplaces have been linked to increased risk of cardiovascular disease, obesity, and all-cause mortality. OBJECTIVES: To evaluate the effectiveness of workplace interventions to reduce sitting at work compared to no intervention or alternative interventions. SEARCH METHODS: We searched the Cochrane Central Register of Controlled Trials (CENTRAL), MEDLINE, Embase, CINAHL, OSH UPDATE, PsycINFO, ClinicalTrials...
June 20, 2018: Cochrane Database of Systematic Reviews
Patrícia Guedes Garcia, Liliana Andrade Chebli, Tarsila Campanha da Rocha Ribeiro, Pedro Duarte Gaburri, Fabio Heleno de Lima Pace, Kátia Valéria Bastos Dias Barbosa, Lívia Almeida Costa, William de Almeida Cruz, Isabelle Carvalho de Assis, Bernardo Rodriguez Mendes Moraes, Alexandre Zanini, Julio Maria Fonseca Chebli
PURPOSE: The prospective assessment of Clostridium difficile infection (CDI) impact in inflammatory bowel disease (IBD) flare in outpatient setting has been poorly investigated. We aimed to evaluate the prevalence and the associated factors with CDI in IBD outpatients presenting colitis flares as well as the outcomes following treatment. METHODS: In this prospective cohort study, conducted from October, 2014, to July, 2016, 120 IBD patients (55% presenting colitis flare) and 40 non-IBD controls were assessed for CDI...
June 21, 2018: International Journal of Colorectal Disease
Christopher J Draper-Joyce, Maryam Khoshouei, David M Thal, Yi-Lynn Liang, Anh T N Nguyen, Sebastian G B Furness, Hariprasad Venugopal, Jo-Anne Baltos, Jürgen M Plitzko, Radostin Danev, Wolfgang Baumeister, Lauren T May, Denise Wootten, Patrick M Sexton, Alisa Glukhova, Arthur Christopoulos
The class A adenosine A1 receptor (A1 R) is a G-protein-coupled receptor that preferentially couples to inhibitory Gi/o heterotrimeric G proteins, has been implicated in numerous diseases, yet remains poorly targeted. Here we report the 3.6 Å structure of the human A1 R in complex with adenosine and heterotrimeric Gi2 protein determined by Volta phase plate cryo-electron microscopy. Compared to inactive A1 R, there is contraction at the extracellular surface in the orthosteric binding site mediated via movement of transmembrane domains 1 and 2...
June 20, 2018: Nature
Jin-Man Kim, Yonghwan Shin, Sunyoung Lee, Mi Yeong Kim, Vasu Punj, Hong-In Shin, Kyunghwan Kim, Jung-Min Koh, Daewon Jeong, Woojin An
Osteoclasts are multinuclear bone-resorbing cells that differentiate from hematopoietic precursor cells. Prostate cancer cells frequently spread to bone and secrete soluble signaling factors to accelerate osteoclast differentiation and bone resorption. However, processes and mechanisms that govern the expression of osteoclastogenic soluble factors secreted by prostate cancer cells are largely unknown. MacroH2A (mH2A) is a histone variant that replaces canonical H2A at designated genomic loci and establishes functionally distinct chromatin regions...
June 20, 2018: Oncogene
Martyna Korcz, Franciszek Sączewski, Patrick J Bednarski, Anita Kornicka
A small library of novel quinoline-3-carbaldehyde hydrazones (Series 1), acylhydrazones (Series 2), and arylsulfonylhydrazones (Series 3) bearing either a 1,2,4-triazole or benzotriazole ring at position 2 was prepared, characterized by elemental analyses and IR, NMR, and MS spectra, and then subjected to in vitro cytotoxicity studies on three human tumor cell lines: DAN-G, LCLC-103H, and SISO. In general, compounds 4 , 6 , and 8 substituted with a 1,2,4-triazole ring proved to be inactive, whereas the benzotriazole-containing quinolines 5 , 7 , and 9 elicited pronounced cancer cell growth inhibitory effects with IC50 values in the range of 1...
June 20, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Beth K Neilsen, Binita Chakraborty, Jamie L McCall, Danielle E Frodyma, Richard L Sleightholm, Kurt W Fisher, Robert E Lewis
BACKGROUND: KMT2/MLL proteins are commonly overexpressed or mutated in cancer and have been shown to support cancer maintenance. These proteins are responsible for methylating histone 3 at lysine 4 and promoting transcription and DNA synthesis; however, they are inactive outside of a multi-protein complex that requires WDR5. WDR5 has been implicated in cancer for its role in the COMPASS complex and its interaction with Myc; however, the role of WDR5 in colon cancer has not yet been elucidated...
June 20, 2018: BMC Cancer
William I Weis, Brian K Kobilka
G protein-coupled receptors (GPCRs) mediate the majority of cellular responses to external stimuli. Upon activation by a ligand, the receptor binds to a partner heterotrimeric G protein and promotes exchange of GTP for GDP, leading to dissociation of the G protein into α and βγ subunits that mediate downstream signals. GPCRs can also activate distinct signaling pathways through arrestins. Active states of GPCRs form by small rearrangements of the ligand-binding, or orthosteric, site that are amplified into larger conformational changes...
June 20, 2018: Annual Review of Biochemistry
Ruiwen Cao, Yongliang Liu, Qing Wang, Zhijun Dong, Dinglong Yang, Hui Liu, Wen Ran, Yi Qu, Jianmin Zhao
Mounting evidence has demonstrated the combined effects of ocean acidification (OA) and other environmental stressors on marine organisms. Although metal pollution is widely distributed in coasts and estuaries, the combined effects of OA and metal pollution have received little attention until recent years. In this study, the accumulation and subcellular distribution of cadmium (Cd) and the physiological responses of the oyster Crassostrea gigas were investigated after 31 days of exposure to OA and Cd, either alone or in combination...
June 17, 2018: Science of the Total Environment
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