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https://www.readbyqxmd.com/read/29332585/new-tacrines-as-anti-alzheimer-s-disease-agents-ii-the-benzo-chromenopyranotacrines
#1
Maria J Oset-Gasque, Jose Marco-Contelles
Tacrine was the first drug approved by FDA (US) for the treatment of Alzheimer's disease suffering patients. Nowadays, this agent has been withdrawn from the clinics due to secondary effects, among them, and the most important, its hepatotoxicity. However, the research on new tacrine analogues devoid of these therapeutically undesirable effects, but benefiting of their high and well known positive cholinergic power, has produced a number of new non-hepatotoxic tacrines. In this context, in our laboratory, in the last years we have prepared a new heterocyclic tacrines by changing the benzene ring present in tacrine by appropriate heterocyclic motifs...
January 12, 2018: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/29331692/memory-performance-predicts-response-to-psychotherapy-for-depression-in-bipolar-disorder-a-pilot-randomized-controlled-trial-with-exploratory-functional-magnetic-resonance-imaging
#2
Thilo Deckersbach, Amy T Peters, Conor Shea, Aishwarya Gosai, Jonathan P Stange, Andrew D Peckham, Kristen K Ellard, Michael W Otto, Scott L Rauch, Darin D Dougherty, Andrew A Nierenberg
OBJECTIVE: This pilot randomized controlled trial compared Cognitive Behavior Therapy (CBT) and Supportive Psychotherapy (SP) for the treatment of depression in bipolar I disorder. We also examined whether exploratory verbal memory, executive functioning, and neural correlates of verbal memory during functional magnetic resonance imaging (fMRI) predicted change in depression severity. METHODS: Thirty-two adults (ages 18-65) with DSM-IV bipolar I disorder meeting current criteria for a major depressive episode were randomized to 18 weeks of CBT or SP...
December 27, 2017: Journal of Affective Disorders
https://www.readbyqxmd.com/read/29329002/integration-of-multi-scale-molecular-modeling-approaches-with-experiments-for-the-in-silico-guided-design-and-discovery-of-novel-herg-neutral-antihypertensive-oxazalone-and-imidazolone-derivatives-and-analysis-of-their-potential-restrictive-effects-on-cell
#3
Serdar Durdagi, Busecan Aksoydan, Ismail Erol, Isik Kantarcioglu, Yavuz Ergun, Gulay Bulut, Melih Acar, Timucin Avsar, George Liapakis, Vlasios Karageorgos, Ramin E Salmas, Barış Sergi, Sara Alkhatib, Gizem Turan, Berfu Nur Yigit, Kutay Cantasir, Bahar Kurt, Turker Kilic
AT1 antagonists is the most recent drug class of molecules against hypertension and they mediate their actions through blocking detrimental effects of angiotensin II (A-II) when acts on type I (AT1) A-II receptor. The effects of AT1 antagonists are not limited to cardiovascular diseases. AT1 receptor blockers may be used as potential anti-cancer agents - due to the inhibition of cell proliferation stimulated by A-II. Therefore, AT1 receptors and the A-II biosynthesis mechanisms are targets for the development of new synthetic drugs and therapeutic treatment of various cardiovascular and other diseases...
December 11, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29327813/computational-tools-for-the-identification-and-interpretation-of-sequence-motifs-in-immunopeptidomes
#4
REVIEW
Bruno Alvarez, Carolina Barra, Morten Nielsen, Massimo Andreatta
Recent advances in proteomics and mass-spectrometry have widely expanded the detectable peptide repertoire presented by major histocompatibility complex (MHC) molecules on the cell surface, collectively known as the immunopeptidome. Finely characterizing the immunopeptidome brings about important basic insights into the mechanisms of antigen presentation, but can also reveal promising targets for vaccine development and cancer immunotherapy. In this report, we describe a number of practical and efficient approaches to analyze immunopeptidomics data, discussing the identification of meaningful sequence motifs in various scenarios and considering current limitations...
January 12, 2018: Proteomics
https://www.readbyqxmd.com/read/29320178/novel-k-ras-g12c-switch-ii-covalent-binders-destabilize-ras-and-accelerate-nucleotide-exchange
#5
Chimno Ihuoma Nnadi, Meredith L Jenkins, Daniel R Gentile, Leslie A Bateman, Daniel Zaidman, Trent E Balius, Daniel K Nomura, John E Burke, Kevan M Shokat, Nir London
The success of targeted covalent inhibitors in the global pharmaceutical industry has led to a resurgence of covalent drug discovery. However, covalent inhibitor design for flexible binding sites remains a difficult task due to lack of methodological development. Here, we compared covalent docking to empirical electrophile screening, against the highly dynamic target K-RasG12C. While the overall hit-rate of both methods was comparable, we were able to rapidly progress a docking hit to a potent irreversible covalent inhibitor that modifies the inactive, GDP-bound state of K-RasG12C...
January 10, 2018: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/29316128/ranking-power-of-the-sqm-cosmo-scoring-function-on-carbonic-anhydrase-ii-inhibitor-complexes
#6
Adam Pecina, Jiri Brynda, Lukas Vrzal, Ramachandran Gnanasekaran, Magdalena Horejsi, Saltuk Eyrilmez, Jan Rezac, Martin Lepsik, Pavlina Rezacova, Pavel Hobza, Pavel Majer, Vaclav Veverka, Jindrich Fanfrlik
Accurate prediction of protein-ligand binding affinities is essential for hit-to-lead optimization and virtual screening. The reliability of scoring functions can be improved by implementing of quantum effects. Here, we demonstrate the ranking power of the semiempirical quantum mechanics (SQM)/implicit solvent (COSMO) scoring function using a challenging set of 10 inhibitors binding to carbonic anhydrase II via Zn2+ in the active site. This new dataset consists of the high-resolution (1.1 - 1.4 Å) crystal structures and experimentally determined Ki values...
January 8, 2018: Chemphyschem: a European Journal of Chemical Physics and Physical Chemistry
https://www.readbyqxmd.com/read/29289882/efficacy-of-2-hydroxy-3-phenylsulfanylmethyl-1-4-naphthoquinone-derivatives-against-different-trypanosoma-cruzi-discrete-type-units-identification-of-a-promising-hit-compound
#7
L S Lara, C S Moreira, C M Calvet, G C Lechuga, R S Souza, S C Bourguignon, V F Ferreira, D Rocha, M C S Pereira
The limited efficacy of benznidazole (Bz) indicated by failures of current Phase II clinical trials emphasizes the urgent need to identify new drugs with improved safety and efficacy for treatment of Chagas disease (CD). Herein, we analyzed the efficacy of a series of 2-hydroxy-3-phenylsulfanylmethyl-[1,4]-naphthoquinones against different Trypanosoma cruzi discrete type units (DTUs) of relevant clinical forms of CD. Cytotoxic and trypanocidal effect of naphthoquinone derivatives were assessed in mammalian cells, trypomastigotes and intracellular amastigotes using, luminescent assays (CellTiter-Glo and T...
December 16, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29283307/using-the-california-verbal-learning-test-second-edition-as-an-embedded-performance-validity-measure-among-individuals-with-tbi-and-individuals-with-psychiatric-disorders
#8
Virginia C Persinger, Douglas M Whiteside, Lyuba Bobova, Seema D Saigal, Marla J Vannucci, Michael R Basso
OBJECTIVE: Among embedded performance validity tests (PVTs), little research addresses the use of Total Hits and Total False Positives from the California Verbal Learning Test, Second Edition (CVLT-II) in spite of low sensitivity, particularly in psychiatric samples. METHOD: This study examined the classification accuracy of these two measures in individuals with psychiatric disorders or mild traumatic brain injury (MTBI). These samples were separated into two groups using the criteria of passing all PVTs versus failing 2 or more PVTs...
December 28, 2017: Clinical Neuropsychologist
https://www.readbyqxmd.com/read/29277148/prostacyclins-in-cardiac-surgery-coming-of-age
#9
Seema P Deshpande, Michael A Mazzeffi, Erik Strauss, Allison Hollis, Kenichi A Tanaka
Prostacyclin (prostaglandin I2 [PGI2]) is an eicosanoid lipid mediator produced by the endothelial cells. It plays pivotal roles in vascular homeostasis by virtue of its potent vasodilatory and antithrombotic effects. Stable pharmacological analogues of PGI2 are used for treatment of pulmonary hypertension and right ventricular failure. PGI2 dose dependently inhibits platelet activation induced by adenosine-5'-diphosphate, arachidonic acid, collagen, and low-dose thrombin. This property has led to its use as an alternative to direct thrombin inhibitors in patients with type II heparin-induced thrombocytopenia (HIT) undergoing cardiac surgery...
December 1, 2017: Seminars in Cardiothoracic and Vascular Anesthesia
https://www.readbyqxmd.com/read/29248145/renal-replacement-therapy-and-anticoagulation
#10
REVIEW
Timo Brandenburger, Thomas Dimski, Torsten Slowinski, Detlef Kindgen-Milles
Today, up to 20% of all intensive care unit patients require renal replacement therapy (RRT), and continuous renal replacement therapies (CRRT) are the preferred technique. In CRRT, effective anticoagulation of the extracorporeal circuit is mandatory to prevent clotting of the circuit or filter and to maintain filter performance. At present, a variety of systemic and regional anticoagulation modes for CRRT are available. Worldwide, unfractionated heparin is the most widely used anticoagulant. All systemic techniques are associated with significant adverse effects...
September 2017: Best Practice & Research. Clinical Anaesthesiology
https://www.readbyqxmd.com/read/29234922/pharmacokinetically-targeted-dosed-everolimus-maintenance-therapy-in-lymphoma-patients
#11
L K Schoch, A Asiama, M Zahurak, S Shanbhag, J Hurtt, K Sawyer, L J Swinnen, N Wagner-Johnston, R J Jones, R F Ambinder, Douglas E Gladstone
BACKGROUND: Everolimus, an mTOR inhibitor, is active in refractory lymphomas. However, toxicity with flat dosing limits its usage. Speculatively, pharmacokinetically-targeted dosing could improve tolerability. Therefore, we studied serum-trough dosing with rituximab as maintenance after high-dose cyclophosphamide (HDC) consolidation in lymphoma patients. PATIENTS/METHODS: After HDC, everolimus was dosed to serum trough levels (goal 3-15 ng/mL), with quarterly rituximab infusions for 1 year while maintaining < grade II non-hematologic and < grade III hematologic toxicities...
December 13, 2017: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/29215417/muramyl-dipeptide-enhances-thermal-injury-induced-autophagy-and-inflammatory-cytokine-response-of-lungs-via-activation-of-nod2-rick-signaling-pathway-in-rats
#12
Xiao-Jing Wu, Hui Liang, Ying Zhang, Xu-Ming Yang, Hong-Yu Wang, Hui Li, Xin-Yi Li, Kai Chen, Yan-Lin Wang, Jian-Guo Li, Zong-Ze Zhang, Xue-Min Song
OBJECTIVE: Nucleotide-binding oligomerization domain 2 (NOD2) is the innate receptor of muramyl dipeptide (MDP). Our previous study revealed that MDP could enhance thermal injury-induced inflammatory cytokine production and organ function injury in rats. The present study was to determine the effect of MDP on autophagy and NOD2/receptor-interacting serine/threonine protein kinases (RICK) signaling pathway of lung injury after thermal injury. METHODS: Forty male Sprague-Dawlay rats were randomly divided into four groups: normal control (NC) group, MDP group, Scald group and MDP + Scald group...
December 6, 2017: Shock
https://www.readbyqxmd.com/read/29206593/glioma-grade-discrimination-with-mr-diffusion-kurtosis-imaging-a-meta-analysis-of-diagnostic-accuracy
#13
Anna Falk Delgado, Markus Nilsson, Danielle van Westen, Alberto Falk Delgado
Purpose To assess the diagnostic test accuracy and sources of heterogeneity for the discriminative potential of diffusion kurtosis imaging (DKI) to differentiate low-grade glioma (LGG) (World Health Organization [WHO] grade II) from high-grade glioma (HGG) (WHO grade III or IV). Materials and Methods The Cochrane Library, Embase, Medline, and the Web of Science Core Collection were systematically searched by two librarians. Retrieved hits were screened for inclusion and were evaluated with the revised tool for quality assessment for diagnostic accuracy studies (commonly known as QUADAS-2) by two researchers...
December 4, 2017: Radiology
https://www.readbyqxmd.com/read/29169470/use-of-fondaparinux-off-label-or-approved-anticoagulants-for-management-of-heparin-induced-thrombocytopenia
#14
MULTICENTER STUDY
Marc Schindewolf, Julia Steindl, Jan Beyer-Westendorf, Sebastian Schellong, Pascal Maria Dohmen, Johannes Brachmann, Katharina Madlener, Bernd Pötzsch, Robert Klamroth, Johannes Hankowitz, Norbert Banik, Sonja Eberle, Markus Michael Müller, Stefan Kropff, Edelgard Lindhoff-Last
BACKGROUND: Life-threatening heparin-induced thrombocytopenia (HIT) is treated with the alternative nonheparin anticoagulants argatroban, lepirudin, or danaparoid. Frequently, the pentasaccharide fondaparinux is used off-label. OBJECTIVES: The authors sought to investigate the safety and efficacy of the different anticoagulants for treating HIT. METHODS: In a national, multicenter registry study, hospitalized patients who were diagnosed with HIT, an at least intermediate clinical HIT-risk (4Ts score ≥4 points), and received treatment with ≥1 dose of the aforementioned anticoagulants were included...
November 28, 2017: Journal of the American College of Cardiology
https://www.readbyqxmd.com/read/29156380/structure-based-design-of-herg-neutral-antihypertensive-oxazalone-and-imidazolone-derivatives
#15
Busecan Aksoydan, Isik Kantarcioglu, Ismail Erol, Ramin Ekhteiari Salmas, Serdar Durdagi
Angiotensin II receptor type 1 (AT1) antagonists are the most recent drug class against hypertension. Recently first crystal structure of AT1 receptor is deposited to the protein data bank (PDB ID: 4YAY). In this work, several molecular screening methods such as molecular docking and de novo design studies were performed and it is found that oxazolone and imidazolone derivatives reveal similar/better interaction energy profiles compared to the FDA approved sartan molecules at the binding site of the AT1 receptor...
October 18, 2017: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/29148434/the-cutting-away-of-potential-secondary-electron-tracks-explains-the-effects-of-beam-size-and-detector-wall-density-in-small-field-photon-dosimetry
#16
Hui Khee Looe, Bjoern Delfs, Daniela Poppinga, Ping Jiang, Dietrich Harder, Bjoern Poppe
The well-known field-size dependent overresponse in small-field photon-beam dosimetry of solid-state detectors equipped with very thin sensitive volumes, such as the PTW microDiamond, cannot be caused by the photon and electron interactions within these sensitive layers because they are only a few micrometers thick. The alternative explanation is that their overresponse is caused by the combination of two effects, the modification of the secondary electron fluence profile i) by a field size too small to warrant lateral secondary electron equilibrium and ii) by the density-dependent electron ranges in the structural detector materials placed in front of or backing the sensitive layer...
November 17, 2017: Physics in Medicine and Biology
https://www.readbyqxmd.com/read/29131822/impact-of-the-ebola-outbreak-on-trypanosoma-brucei-gambiense-infection-medical-activities-in-coastal-guinea-2014-2015-a-retrospective-analysis-from-the-guinean-national-human-african-trypanosomiasis-control-program
#17
Mariame Camara, Eric Ouattara, Alexandre Duvignaud, René Migliani, Oumou Camara, Mamadou Leno, Philippe Solano, Bruno Bucheton, Mamadou Camara, Denis Malvy
BACKGROUND: The 2014-2015 Ebola outbreak massively hit Guinea. The coastal districts of Boffa, Dubreka and Forecariah, three major foci of Human African Trypanosomiasis (HAT), were particularly affected. We aimed to assess the impact of this epidemic on sleeping sickness screening and caring activities. METHODOLOGY/PRINCIPAL FINDINGS: We used preexisting data from the Guinean sleeping sickness control program, collected between 2012 and 2015. We described monthly: the number of persons (i) screened actively; (ii) or passively; (iii) treated for HAT; (iv) attending post-treatment follow-up visits...
November 13, 2017: PLoS Neglected Tropical Diseases
https://www.readbyqxmd.com/read/29098714/a-potential-new-form-of-jail-diversion-and-reconnection-to-mental-health-services-ii-demonstration-of-feasibility
#18
Michael T Compton, Simone Anderson, Beth Broussard, Samantha Ellis, Brooke Halpern, Luca Pauselli, Marsha O'Neal, Benjamin G Druss, Mark Johnson
Given fragmentation between mental health and criminal justice systems, we tested the feasibility of implementing a potential new form of pre-booking jail diversion. Our "linkage system" consists of three steps: (i) individuals with serious mental illnesses and an arrest history give special consent to be enrolled in a statewide database; (ii) if an officer has an encounter with an enrolled patient and runs a routine background check, he or she receives an electronic message to call; and (iii) the "linkage specialist" provides brief telephonic assistance to the officer...
November 2, 2017: Behavioral Sciences & the Law
https://www.readbyqxmd.com/read/29069510/lnc2meth-a-manually-curated-database-of-regulatory-relationships-between-long-non-coding-rnas-and-dna-methylation-associated-with-human-disease
#19
Hui Zhi, Xin Li, Peng Wang, Yue Gao, Baoqing Gao, Dianshuang Zhou, Yan Zhang, Maoni Guo, Ming Yue, Weitao Shen, Shangwei Ning, Lianhong Jin, Xia Li
Lnc2Meth ( http://www.bio-bigdata.com/Lnc2Meth/ ), an interactive resource to identify regulatory relationships between human long non-coding RNAs (lncRNAs) and DNA methylation, is not only a manually curated collection and annotation of experimentally supported lncRNAs-DNA methylation associations but also a platform that effectively integrates tools for calculating and identifying the differentially methylated lncRNAs and protein-coding genes (PCGs) in diverse human diseases. The resource provides: (i) advanced search possibilities, e...
October 23, 2017: Nucleic Acids Research
https://www.readbyqxmd.com/read/29063542/are-we-there-yet-human-factors-knowledge-and-health-information-technology-the-challenges-of-implementation-and-impact
#20
P Turner, A Kushniruk, C Nohr
Objective: To review the developments in human factors (HF) research on the challenges of health information technology (HIT) implementation and impact given the continuing incidence of usability problems and unintended consequences from HIT development and use. Methods: A search of PubMed/Medline and Web of Science® identified HF research published in 2015 and 2016. Electronic health records (EHRs) and patient-centred HIT emerged as significant foci of recent HF research. The authors selected prominent papers highlighting ongoing HF and usability challenges in these areas...
August 2017: Yearbook of Medical Informatics
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