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https://www.readbyqxmd.com/read/27922978/significance-of-monocyte-counts-at-recurrence-on-survival-outcome-of-women-with-endometrial-cancer
#1
Hiroko Machida, Madushka Yohan De Zoysa, Tsuyoshi Takiuchi, Marianne S Hom, Katherine E Tierney, Koji Matsuo
OBJECTIVE: Tumor-associated macrophages (TAMs) are known to have adverse effects on the survival of women with endometrial cancer. Because monocytes function as progenitors of macrophages, this study examined the association between monocyte count at the first recurrence/progression of endometrial cancer and survival time after recurrence/progression (SAR). METHODS: This is a retrospective study evaluating 141 consecutive cases of recurrent endometrial cancer after surgical staging (n = 114) and progression after nonsurgical management (n = 27)...
December 3, 2016: International Journal of Gynecological Cancer
https://www.readbyqxmd.com/read/27922185/relaxin-family-peptides-structure-activity-relationship-studies
#2
REVIEW
Nitin A Patil, K Johan Rosengren, Frances Separovic, John D Wade, Ross A D Bathgate, Mohammed Akhter Hossain
The human relaxin peptide family consists of seven cystine-rich peptides, four of which are known to signal through relaxin family peptide receptors, RXFP1-4. Considering the vital roles these peptides play in physiology and various diseases, they are of considerable importance for drug discovery and development. Detailed structure-activity relationship (SAR) studies towards understanding the role of important residues in each of these peptides have been reported over the years and utilised for design of antagonists and minimised agonist variants...
December 6, 2016: British Journal of Pharmacology
https://www.readbyqxmd.com/read/27921386/cytotoxicity-of-a-series-of-norcantharidin-inspired-tetrahydroepoxyisoindole-carboxamides
#3
Christopher Peter Gordon, Lawson K Spare, Pasquale Falsetta, Jayne Gilbert, David G Harman, Mark A Baker, Feng Li, Adam McCluskey, Jack K Clegg, Jennette A Sakoff, Janice R Aldrich-Wright
A series of 28 norcantharidin (NorC) inspired analogues were accessed via a robust two-step Ugi intramolecular Diels-Alder (IMDA) sequence. Four analogues displayed equipotent whole cell cytotoxicity to NorC and cisplatin against a number of cancer cell lines and a normal breast cell line (MCF10A). Notably (3S,3aS,6R)-2-benzyl-7-methyl-N-(naphthalen-2-yl)-1-oxo-1,2,3,6-tetrahydro-3a,6-epoxyisoindole-3-carboxamide (trans-27) displayed superior whole cell activity against breast (MCF-7, GI50 = 2.9 µM) and colon (HT29, GI50 = 6...
December 6, 2016: ChemMedChem
https://www.readbyqxmd.com/read/27920896/assessing-the-hyperthermic-properties-of-magnetic-heterostructures-the-case-of-gold-iron-oxide-composites
#4
Elvira Fantechi, Paula M Castillo, Erika Conca, Francesca Cugia, Claudio Sangregorio, Maria Francesca Casula
Gold-iron oxide composites were obtained by in situ reduction of an Au(III) precursor by an organic reductant (either potassium citrate or tiopronin) in a dispersion of preformed iron oxide ultrasmall magnetic (USM) nanoparticles. X-ray diffraction, transmission electron microscopy, chemical analysis and mid-infrared spectroscopy show the successful deposition of gold domains on the preformed magnetic nanoparticles, and the occurrence of either citrate or tiopronin as surface coating. The potential of the USM@Au nanoheterostructures as heat mediators for therapy through magnetic fluid hyperthermia was determined by calorimetric measurements under sample irradiation by an alternating magnetic field with intensity and frequency within the safe values for biomedical use...
December 6, 2016: Interface Focus
https://www.readbyqxmd.com/read/27920722/a-new-structure-activity-relationship-sar-model-for-predicting-drug-induced-liver-injury-based-on-statistical-and-expert-based-structural-alerts
#5
Fabiola Pizzo, Anna Lombardo, Alberto Manganaro, Emilio Benfenati
The prompt identification of chemical molecules with potential effects on liver may help in drug discovery and in raising the levels of protection for human health. Besides in vitro approaches, computational methods in toxicology are drawing attention. We built a structure-activity relationship (SAR) model for evaluating hepatotoxicity. After compiling a data set of 950 compounds using data from the literature, we randomly split it into training (80%) and test sets (20%). We also compiled an external validation set (101 compounds) for evaluating the performance of the model...
2016: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/27919659/synthesis-and-sar-study-of-novel-sarsasapogenin-derivatives-as-potent-neuroprotective-agents-and-no-production-inhibitors
#6
Hui Pan, Pham Van Khang, Dong Dong, Rui Wang, Lei Ma
Sarsasapogenin, isolated from rhizomes of Anemarrhena asphodeloides, was found to be able to enhance memory. On the basis of the structure of Sarsasapogenin, a series of derivatives were synthesized and evaluated for their neuroprotective activity in PC12 cells and NO production inhibitory activity in RAW264.7 cell lines. The preliminary structure-activity relationship of them indicated that introduction of carbamate groups at the 3-hydroxyl position of sarsasapogenin might improve neuroprotective activity...
November 24, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27919315/implication-of-alternative-minimal-clinically-important-difference-threshold-estimation-methods-on-technology-assessment
#7
Diana Brixner, Eli O Meltzer, Kellie Morland, Cathryn A Carroll, Ullrich Munzel, Brian J Lipworth
OBJECTIVES: Various minimal clinically important difference (MCID) threshold estimation techniques have been applied to seasonal allergic rhinitis (SAR). The objectives of this study are to (i) assess the difference in magnitude of alternative SAR MCID threshold estimates and (ii) evaluate the impact of alternative MCID estimates on health technology assessment (HTA). METHODS: Data describing change from baseline of the reflective Total Nasal Symptom Score (rTNSS) for four intranasal SAR treatments were obtained from United States Food and Drug Administration-approved prescribing information...
December 6, 2016: International Journal of Technology Assessment in Health Care
https://www.readbyqxmd.com/read/27919211/development-of-mlr-and-svm-aided-qsar-models-to-identify-common-sar-of-gaba-uptake-herbal-inhibitors-used-in-the-treatment-of-schizophrenia
#8
Sahila Mohammed Marunnan, Babitha Pallikkara Pulikka, V K Gopalakrishnan, Srinivas Bandaru, Mukesh Yadav, Anuraj Nayarisseri, Victor Arokia Doss
Deficits in GABAnergic system is implicated in the pathophysiology of schizophrenia. Available antipsychotics that target GABA receptor form a desirable therapeutic strategy in the treatment regimen of schizophrenia but, unfortunately, suffers serious setback due to their prolonged side effects. The present investigation focuses on developing QSAR models from the biological activity of herbal compounds and their derivatives that promise to be alternative candidates to GABA uptake inhibitors. Three sets of compounds were undertaken in the study to develop the QSAR models...
December 5, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/27918876/awareness-of-identity-alteration-and-diagnostic-preference-between-borderline-personality-disorder-and-dissociative-disorders
#9
Vedat Sar, Firdevs Alioğlu, Gamze Akyuz, Emre Tayakısı, Ezgi F Öğülmüş, Doğuş Sönmez
AIM: This study inquires into identity alteration among college students and its relationship to borderline personality disorder (BPD) and/or dissociative disorders (DDs). METHODS: Steinberg Identity Alteration Questionnaire (SIAQ), Childhood Trauma Questionnaire (CTQ), and self-report screening tool of the BPD section of the Structured Clinical Interview for DSM-IV (SCID-BPD) were administered to 1301 college students. Participants who fit the diagnostic criteria of BPD (n = 80) according to the clinician-administered SCID-BPD and 111 non-BPD controls were evaluated using the Structured Clinical Interview for DSM-IV DDs (SCID-D) by two psychiatrists blind to the group membership and scale scores...
December 5, 2016: Journal of Trauma & Dissociation
https://www.readbyqxmd.com/read/27917181/nitric-oxide-responsive-heavy-metal-associated-gene-athmad1-contributes-to-development-and-disease-resistance-in-arabidopsis-thaliana
#10
Q Muhammad Imran, Noreen Falak, Adil Hussain, Bong-Gyu Mun, Arti Sharma, Sang-Uk Lee, Kyung-Min Kim, Byung-Wook Yun
Exposure of plants to different biotic and abiotic stress condition instigates significant change in the cellular redox status; resulting in the elevation of reactive nitrogen species that play signaling role in mediating defense responses. Heavy metal associated (HMA) domain containing genes are required for spatio-temporal transportation of metal ions that bind with various enzymes and co-factors within the cell. To uncover the underlying mechanisms mediated by AtHMA genes, we identified 14 Arabidopsis HMA genes that were differentially expressed in response to nitrosative stress through RNA-seq analysis...
2016: Frontiers in Plant Science
https://www.readbyqxmd.com/read/27915171/progress-in-the-development-of-%C3%AE-lactams-as-n-acylethanolamine-acid-amidase-naaa-inhibitors-synthesis-and-sar-study-of-new-potent-n-o-substituted-derivatives
#11
R Petracca, S Ponzano, S M Bertozzi, O Sasso, D Piomelli, T Bandiera, F Bertozzi
The anti-inflammatory effects resulting from raising the levels of palmitoylethanolamide (PEA), an endogenous bioactive lipid, led to envisage N-Acylethanolamine Acid Amidase (NAAA), the cysteine hydrolase mainly responsible for PEA degradation, as an attractive target for small molecule inhibitors. Previous work in our group identified serine-derived β-lactams as potent and systemically active inhibitors of NAAA activity. Aiming to expand the SAR study around this class of compounds, we investigated the effect of the substitution on the endocyclic nitrogen by designing and synthesizing a series of N-substituted β-lactams...
November 23, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27914946/design-synthesis-and-biological-evaluation-of-alkylamino-biphenylamides-as-hsp90-c-terminal-inhibitors
#12
Gaurav Garg, Huiping Zhao, Brian S J Blagg
Hsp90 is a promising therapeutic target for the development of anti-cancer agents due to its integral role in the stability and function of proteins associated with all ten hallmarks of cancer. Novobiocin, a coumarin antibiotic, was the first natural product identified that targeted the Hsp90 C-terminal domain and manifested anti-proliferative activity (SKBr3 IC50∼700μM). Subsequent structural investigations on novobiocin led to analogues with significantly improved anti-proliferative activity against multiple cancer cell lines...
November 19, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27914363/new-insights-into-the-sar-and-drug-combination-synergy-of-2-quinolin-4-yloxy-acetamides-against-mycobacterium-tuberculosis
#13
Bruno Couto Giacobbo, Kenia Pissinate, Valnês Rodrigues-Junior, Anne Drumond Villela, Estêvão Silveira Grams, Bruno Lopes Abbadi, Fernanda Teixeira Subtil, Nathalia Sperotto, Rogério Valim Trindade, Davi Fernando Back, Maria Martha Campos, Luiz Augusto Basso, Pablo Machado, Diógenes Santiago Santos
2-(Quinolin-4-yloxy)acetamides have been described as potent and selective in vitro inhibitors of Mycobacterium tuberculosis (Mtb) growth. Herein, a new series of optimized compounds were found to demonstrate highly potent antitubercular activity, with minimum inhibitory concentration (MIC) values against drug-susceptible and drug-resistant Mycobacterium tuberculosis strains in the submicromolar range. Furthermore, the most active compounds had no apparent toxicity to mammalian cells, and they showed intracellular activities similar to those of isoniazid and rifampin in a macrophage model of Mtb infection...
November 23, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27914003/n-terminal-pro-b-type-natriuretic-peptide-levels-are-linked-with-modified-child-pugh-classification-in-patients-with-nonalcoholic-cirrhosis-nt-probnp-and-liver-cirrhosis
#14
Abdulbaki Kumbasar, Mehtap Navdar, Esra Ataoglu, Isil Uzunhasan, Kadir Ergen, Sule Poturoglu, Filiz Basinoglu, Fatih Yilmaz, Mustafa Yenigun, Fuat Sar, Ozgur Tanriverdi
Excess N-terminal pro-brain natriuretic peptide secretion has been linked to cirrhosis in previously studies. The relationship of plasma N-terminal pro-brain natriuretic peptide levels and cardiac dysfunction determined by echocardiography were investigated in patients with nonalcoholic cirrhosis and a control group of chronic hepatitis. This study was designed as a cross-sectional study. Thirty-two men and thirty-three women who gave informed consent who were followed-up for chronic liver failure were enrolled...
December 2, 2016: Cell Biochemistry and Biophysics
https://www.readbyqxmd.com/read/27913739/structure-activity-relation-of-amor-sugar-molecule-that-activates-pollen-tubes-for-ovular-guidance
#15
Jiao Jiao, Akane G Mizukami, Subramanian Sankaranarayanan, Junichiro Yamguchi, Kenichiro Itami, Tetsuya Higashiyama
Successful fertilization in flowering plants depends on the precise directional growth control of pollen tube through the female pistil tissue, towards the female gametophyte contained in the ovule for delivery of non-motile sperm cells. Cysteine-rich peptides LUREs secreted from the synergid cells on either side of the egg cell act as ovular attractants of pollen tubes. Competency control by the pistil is crucial for the response of pollen tubes to these ovular attractants. We recently reported that ovular 4-O-methyl-glucuronosyl arabinogalactan AMOR induces competency of the pollen tube to respond to ovular attractant LURE peptides in Torenia fournieri...
December 2, 2016: Plant Physiology
https://www.readbyqxmd.com/read/27908761/discovery-of-dual-positive-allosteric-modulators-pams-of-the-metabotropic-glutamate-2-receptor-and-cyslt1-antagonists-for-treating-migraine-headache
#16
Maria-Jesus Blanco, Dana R Benesh, James A Knobelsdorf, Albert Khilevich, Guillermo S Cortez, Fese Mokube, Thomas D Aicher, Todd M Groendyke, Fredrik P Marmsater, Tony P Tang, Kirk W Johnson, Amy Clemens-Smith, Mark A Muhlhauser, Steven Swanson, John Catlow, Renee Emkey, Michael P Johnson, Jeffrey M Schkeryantz
Pyridylmethylsulfonamide series were the first reported example of positive allosteric modulators (PAM) of the mGlu2 receptor. The hydroxyacetophenone scaffold is a second series of mGlu2 PAMs we have identified. This series of molecules are potent mGlu2 potentiators and possess significant CysLT1 (cysteinyl leukotriene receptor 1) antagonist activity, showing in vivo efficacy in a dural plasma protein extravasation (PPE) model of migraine. In this paper, we describe the dual SAR, pharmacokinetics and preclinical in vivo efficacy data for a tetrazole containing hydroxyacetophenone scaffold...
November 18, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27907876/rational-design-and-synthesis-of-1-5-disubstituted-tetrazoles-as-potent-inhibitors-of-the-mdm2-p53-interaction
#17
Ewa Surmiak, Constantinos G Neochoritis, Bogdan Musielak, Aleksandra Twarda-Clapa, Katarzyna Kurpiewska, Grzegorz Dubin, Carlos Camacho, Tad A Holak, Alexander Dömling
Using the computational pharmacophore-based ANCHOR.QUERY platform a new scaffold was discovered. Potent compounds evolved inhibiting the protein-protein interaction p53-MDM2. An extensive SAR study was performed based on our four-point pharmacophore model, yielding derivatives with affinity to MDM2 in the nanomolar range. Their binding affinity with MDM2 was evaluated using both fluorescence polarization (FP) assay and 2D-NMR-HSQC experiments.
November 16, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27903454/effects-of-frequently-used-pharmaceutical-excipients-on-the-organic-cation-transporters-1-3-and-peptide-transporters-1-2-stably-expressed-in-mdckii-cells
#18
Marcus Otter, Stefan Oswald, Werner Siegmund, Markus Keiser
There is ample evidence that pharmaceutical excipients, which are supposed to be pharmacologically inactive, have an impact on drug metabolism and efflux transport. So far, little is known whether they also modulate uptake transporter proteins. We have recently shown that commonly used solubilizing agents exert significant effects on the function of organic anion uptake transporting polypeptides. Therefore, we investigated in this study the influence of frequently used pharmaceutical excipients on the transport activity of organic cation transporters OCT1, OCT2 and OCT3 and the peptide transporters PEPT1 and PEPT2...
November 26, 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/27903218/structure-activity-relationship-studies-of-new-marine-anticancer-agents-and-their-synthetic-analogues
#19
Sergey N Fedorov, Valentin A Stonik, Friedemann Honecker, Sergey Dyshlovoy
This review addresses in depth recent structure-activity relationship (SAR) studies of new marine compounds and their synthetic analogues with potential or established anticancer activity, published in 2015.
November 21, 2016: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/27898005/validation-and-parameter-sensitivity-tests-for-reconstructing-swell-field-based-on-an-ensemble-kalman-filter
#20
Xuan Wang, Pierre Tandeo, Ronan Fablet, Romain Husson, Lei Guan, Ge Chen
The swell propagation model built on geometric optics is known to work well when simulating radiated swells from a far located storm. Based on this simple approximation, satellites have acquired plenty of large samples on basin-traversing swells induced by fierce storms situated in mid-latitudes. How to routinely reconstruct swell fields with these irregularly sampled observations from space via known swell propagation principle requires more examination. In this study, we apply 3-h interval pseudo SAR observations in the ensemble Kalman filter (EnKF) to reconstruct a swell field in ocean basin, and compare it with buoy swell partitions and polynomial regression results...
November 25, 2016: Sensors
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