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https://www.readbyqxmd.com/read/28315445/evaluation-of-pept1-transport-of-food-derived-antihypertensive-peptides-ile-pro-pro-and-leu-lys-pro-using-in-vitro-ex-vivo-and-in-vivo-transport-models
#1
John P Gleeson, David J Brayden, Sinéad M Ryan
Ile-Pro-Pro (IPP) and Leu-Lys-Pro (LKP) are food-derived antihypertensive peptides which inhibit angiotensin-converting enzyme (ACE) and may have potential to attenuate hypertension. There is debate over their mechanism of uptake across small intestinal epithelia, but paracellular and PepT1 carrier-mediated uptake are thought to be important routes. The aim of this study was to determine their routes of intestinal permeability using in vitro, ex vivo and in vivo intestinal models. The presence of an apical side pH of 6...
March 14, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28314514/structural-modifications-of-diarylpyrimidines-dapys-as-hiv-1-nnrtis-synthesis-anti-hiv-activities-and-sar
#2
Huan-Huan Lu, Ping Xue, Yuan-Yuan Zhu, Xiu-Lian Ju, Xiao-Jiao Zheng, Xun Zhang, Ting Xiao, Christophe Pannecouque, Ting-Ting Li, Shuang-Xi Gu
30 new analogues of diarylpyrimidines were synthesized for further structural modifications, involving not only the linker but also the wing α of DAPYs. The anti-HIV-1 activities of all target molecules were evaluated, and most of them exhibited potent anti-HIV-1 (WT) activities and low cytotoxicities. Among which, compound 4g showed excellent activities against WT HIV-1 with an EC50 value of 5.8nM and SI of up to 26,034. Another compound 4ab bearing a novel pyridinyl Wing α also displayed attractive activities...
March 6, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28304353/phase-error-correction-for-approximated-observation-based-compressed-sensing-radar-imaging
#3
Bo Li, Falin Liu, Chongbin Zhou, Yuanhao Lv, Jingqiu Hu
Defocus of the reconstructed image of synthetic aperture radar (SAR) occurs in the presence of the phase error. In this work, a phase error correction method is proposed for compressed sensing (CS) radar imaging based on approximated observation. The proposed method has better image focusing ability with much less memory cost, compared to the conventional approaches, due to the inherent low memory requirement of the approximated observation operator. The one-dimensional (1D) phase error correction for approximated observation-based CS-SAR imaging is first carried out and it can be conveniently applied to the cases of random-frequency waveform and linear frequency modulated (LFM) waveform without any a priori knowledge...
March 17, 2017: Sensors
https://www.readbyqxmd.com/read/28304135/transport-of-chemical-signals-in-systemic-acquired-resistance
#4
REVIEW
Archana Singh, Gah-Hyun Lim, Pradeep Kachroo
Systemic acquired resistance (SAR) is a form of broad-spectrum resistance induced in response to local infections that protects uninfected parts against subsequent secondary infections by related or unrelated pathogens. SAR signaling requires two parallel branches, one regulated by salicylic acid (SA), and the other by azelaic acid (AzA) and glycerol-3-phosphate (G3P). AzA and G3P function downstream of the free radicals nitric oxide (NO) and reactive oxygen species (ROS). During SAR, SA, AzA, and G3P accumulate in the infected leaves, but only a small portion of these is transported to distal uninfected leaves...
March 17, 2017: Journal of Integrative Plant Biology
https://www.readbyqxmd.com/read/28303965/effect-of-1-8%C3%A2-ghz-radiofrequency-electromagnetic-radiation-on-novel-object-associative-recognition-memory-in-mice
#5
Kai Wang, Jun-Mei Lu, Zhen-He Xing, Qian-Ru Zhao, Lin-Qi Hu, Lei Xue, Jie Zhang, Yan-Ai Mei
Mounting evidence suggests that exposure to radiofrequency electromagnetic radiation (RF-EMR) can influence learning and memory in rodents. In this study, we examined the effects of single exposure to 1.8 GHz RF-EMR for 30 min on subsequent recognition memory in mice, using the novel object recognition task (NORT). RF-EMR exposure at an intensity of >2.2 W/kg specific absorption rate (SAR) power density induced a significant density-dependent increase in NORT index with no corresponding changes in spontaneous locomotor activity...
March 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28303353/silicon-alleviates-simulated-acid-rain-stress-of-oryza-sativa-l-seedlings-by-adjusting-physiology-activity-and-mineral-nutrients
#6
Shuming Ju, Liping Wang, Ningning Yin, Dan Li, Yukun Wang, Cuiying Zhang
Silicon (Si) has been a modulator in plants under abiotic stresses, such as acid rain. To understand how silicon made an effect on rice (Oryza sativa L.) exposed to simulated acid rain (SAR) stress, the growth, physiologic activity, and mineral nutrient content in leaves of rice were investigated. The results showed that combined treatments with Si (1.0, 2.0, or 4.0 mM) and SAR (pH 4.0, 3.0, or 2.0) obviously improved the rice growth compared with the single treatment with SAR. Incorporation of Si into SAR treatment decreased malondialdehyde (MDA) content; increased soluble protein and proline contents; promoted CAT, POD, SOD, and APX activity; and maintained the K, Ca, Mg, Fe, Zn, Cu content balance in leaves of rice seedlings under SAR stress...
March 16, 2017: Protoplasma
https://www.readbyqxmd.com/read/28302782/genome-sequences-of-mycobacteriophages-jane-and-sneeze-new-members-of-cluster-g
#7
Catherine M Mageeney, Cimrin Bhalla, Charles A Bowman, Bhavishya Devireddy, Adrienne P Dzurick, Lee H Graham, Marina Grossi, Margaret A Kenna, Mikala A Kowal, Drew D Nielsen, Rachel A Pallay, Kaitlyn M Ruffing, Daniel A Russell, Samantha L Sarli, Adama Shaw, Joseph W Skibbens, Joseph N Teyim, Vassie C Ware
Jane and Sneeze are newly isolated phages of Mycobacterium smegmatis mc(2)155 from Hillsborough, NJ, and Palo Verde, Costa Rica, respectively. Both are cluster G, subcluster G1 mycobacteriophages. Notable nucleotide differences exist between genomes in the right half, including the presence of mycobacteriophage mobile element 1 (MPME1) in Jane.
March 16, 2017: Genome Announcements
https://www.readbyqxmd.com/read/28302010/discovery-of-hedgehog-antagonists-for-cancer-therapy
#8
Harleen Khatra, Chandra Bose, Surajit Sinha
BACKGROUND: The evolutionarily conserved Hedgehog (Hh) signaling cascade is one of the key mediators of embryonic development of many metazoans. This pathway has been extensively targeted by small molecule inhibitors as its misregulation leads to various malignancies and developmental disorders. Thus, blocking this pathway can be a novel therapeutic avenue for the treatment of Hedgehog-dependent cancers. This review covers the mechanism of hedgehog signaling in vertebrate cells, provides an overview of reported small molecule Hh pathway inhibitors, with the synthetic routes and SAR studies of some of them discussed briefly...
March 16, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28301150/discovery-of-new-sirt2-inhibitors-by-utilizing-a-consensus-docking-scoring-strategy-and-structure-activity-relationship-analysis
#9
Shen-Zhen Huang, Chun-Li Song, Xiang Wang, Guo Zhang, Yan-Lin Wang, Xiao-Juan Jiang, Qi-Zheng Sun, Lu-Yi Huang, Rong Xiang, Yi-Guo Hu, Lin-Li Li, Sheng-Yong Yang
SIRT2, which is a NAD+ (nicotinamide adenine dinucleotide)-dependent deacetylase, has been demonstrated to play an important role in the occurrence and development of a variety of diseases such as cancer, ischemia-reperfusion, and neurodegenerative diseases. Small molecule inhibitors of SIRT2 are thought as potential interfering agents for relevant diseases. Discovery of SIRT2 inhibitor has attracted much attention recently. In this investigation, we first adopted a consensus docking/scoring strategy to screen for novel SIRT2 inhibitors...
March 16, 2017: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/28300674/structure-activity-studies-on-polymyxin-derivatives-carrying-three-positive-charges-only-reveal-a-new-class-of-compounds-with-strong-antibacterial-activity
#10
Martti Vaara, Timo Vaara, Jonathan M Tyrrell
Recent years have brought in an increased interest to develop improved polymyxins. The currently used polymyxins, i.e. polymyxin B and colistin (polymyxin E) are pentacationic lipopeptides that possess a cyclic heptapeptide part with three positive charges, a linear "panhandle" part with two positive charges, and a fatty acyl tail. Unfortunately, their clinical use is shadowed by their notable nephrotoxicity. We have previously developed a polymyxin derivative NAB739 which lacks the positive charges in the linear part...
March 11, 2017: Peptides
https://www.readbyqxmd.com/read/28300398/novel-bivalent-ligands-based-on-the-sumanirole-pharmacophore-reveal-dopamine-d2-receptor-d2r-biased-agonism
#11
Alessandro Bonifazi, Hideaki Yano, Michael P Ellenberger, Ludovic Muller, Vivek Kumar, Mu-Fa Zou, Ning Sheng Cai, Adrian M Guerrero, Amina S Woods, Lei Shi, Amy Hauck Newman
The development of bivalent ligands has attracted interest as a way to potentially improve the selectivity and/or affinity for a specific receptor subtype. The ability to bind two distinct receptor binding sites simultaneously can allow the selective activation of specific G-protein dependent or β-arrestin-mediated cascade pathways. Herein, we developed an extended SAR study using sumanirole (1) as the primary pharmacophore. We found that substitutions in the N-1- and/or N-5-positions, physiochemical properties of those substituents, and secondary aromatic pharmacophores can enhance agonist efficacy for the cAMP inhibition mediated by Gi/o-proteins, while reducing or suppressing potency and efficacy toward β-arrestin recruitment...
March 16, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28300330/synthesis-and-super-potent-anticancer-activity-of-tubulysins-carrying-non-hydrolysable-n-substituents-on-tubuvaline
#12
Monica Sani, Paolo Lazzari, Marco Folini, Marco Spiga, Valentina Zuco, Michelandrea De Cesare, Ilaria Manca, Sergio Dall'Angelo, Massimo Frigerio, Igor Usai, Andrea Testa, Nadia Zaffaroni, Matteo Zanda
Synthetic tubulysins 24a-m, having non-hydrolysable N-substituents on tubuvaline (Tuv), were obtained in high purity and good overall yields using a multi-step synthesis. Key step was the formation of differently N-substituted Ile-Tuv fragments 10 via aza-Michael reaction of azido-Ile derivatives 8 with the -unsaturated oxo-thiazole 5. A SAR study using a panel of human tumor cell lines showed strong anti-proliferative activity for all compounds 24a-m, with IC50 values in the sub-nanomolar range, which were distinctly lower than those of Tubulysin A, vinorelbine, and paclitaxel...
March 16, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28294996/design-and-imaging-of-ground-based-multiple-input-multiple-output-synthetic-aperture-radar-mimo-sar-with-non-collinear-arrays
#13
Cheng Hu, Jingyang Wang, Weiming Tian, Tao Zeng, Rui Wang
Multiple-Input Multiple-Output (MIMO) radar provides much more flexibility than the traditional radar thanks to its ability to realize far more observation channels than the actual number of transmit and receive (T/R) elements. In designing the MIMO imaging radar arrays, the commonly used virtual array theory generally assumes that all elements are on the same line. However, due to the physical size of the antennas and coupling effect between T/R elements, a certain height difference between T/R arrays is essential, which will result in the defocusing of edge points of the scene...
March 15, 2017: Sensors
https://www.readbyqxmd.com/read/28294050/an-integrated-multi-qsar-modeling-approach-for-designing-knoevenagel-type-indoles-with-enhancing-cytotoxic-profiles
#14
Sk Abdul Amin, Nilanjan Adhikari, Tarun Jha, Shovanlal Gayen
BACKGROUND: Unconventional Knoevenagel-type indoles have been the topic of interest of many synthetic chemists because of its promising efficacy in different diseases including in cancer. OBJECTIVE: To explore the structural requirements of Knoevenagel-type cytotoxic indoles for higher efficacy. METHODS: Multi-QSAR modeling (MLR, ANN, SVM, Bayesian classification, HQSAR and Topomer CoMFA) was performed on these analogs. RESULTS: All these modeling techniques were validated individually and interpreted with the experimental SAR observations...
March 9, 2017: Current Computer-aided Drug Design
https://www.readbyqxmd.com/read/28291806/effects-of-silicon-on-oryza-sativa-l-seedling-roots-under-simulated-acid-rain-stress
#15
Shuming Ju, Ningning Yin, Liping Wang, Cuiying Zhang, Yukun Wang
Silicon (Si) has an important function in reducing the damage of environmental stress on plants. Acid rain is a serious abiotic stress factor, and Si can alleviate the stress induced by acid rain on plants. Based on these assumptions, we investigated the effects of silicon on the growth, root phenotype, mineral element contents, hydrogen peroxide (H2O2) and antioxidative enzymes of rice (Oryza sativa L.) seedling roots under simulated acid rain (SAR) stress. The results showed that the combined or single effects of Si and/or SAR on rice roots depend on the concentration of Si and the pH of the SAR...
2017: PloS One
https://www.readbyqxmd.com/read/28291763/wonka-and-oommppaa-analysis-of-protein-ligand-interaction-data-to-direct-structure-based-drug-design
#16
Charlotte M Deane, Ian D Wall, Darren V S Green, Brian D Marsden, Anthony R Bradley
In this work, two freely available web-based interactive computational tools that facilitate the analysis and interpretation of protein-ligand interaction data are described. Firstly, WONKA, which assists in uncovering interesting and unusual features (for example residue motions) within ensembles of protein-ligand structures and enables the facile sharing of observations between scientists. Secondly, OOMMPPAA, which incorporates protein-ligand activity data with protein-ligand structural data using three-dimensional matched molecular pairs...
March 1, 2017: Acta Crystallographica. Section D, Structural Biology
https://www.readbyqxmd.com/read/28291468/navy-en-route-care-a-3-year-review-of-428-navy-air-evacuations
#17
Benjamin Walrath, Alejandra Mora, Victoria Ganem, Stephen Harper, Elliot Ross, Chetan Kharod, Gerard Demers, Vikhyat S Bebarta
BACKGROUND: Navy medical personnel have been recording en route care (ERC) missions through Search and Rescue (SAR) reports since the 1970's. Our objective was to report clinical ERC cases treated by Navy operational assets from January 2012 to January 2015. METHODS: The Search and Rescue Model Manager office collects SAR reports for all patient transports involving Navy personnel and equipment. From these reports, descriptive statistics to include total number of patients transported, percentages of Advanced Life Support versus Basic Life Support transports, time of transport, and type of ERC provider for the transport were collected...
March 2017: Military Medicine
https://www.readbyqxmd.com/read/28291352/understanding-the-molecular-determinant-of-reversible-human-monoamine-oxidase-b-inhibitors-containing-2h-chromen-2-one-core-structure-based-and-ligand-based-derived-3-d-qsar-predictive-models
#18
Milan Mladenovic, Alexandros Patsilinakos, Adele Pirolli, Manuela Sabatino, Rino Ragno
Monoamine oxidase B (MAO B) catalyzes the oxidative deamination of aryalkylamines neurotransmitters with concomitant reduction of oxygen to hydrogen peroxide. Consequently, the enzyme's malfunction can induce oxidative damage to mitochondrial DNA and mediates development of Parkinson's disease. Thus, MAO B emerges as a promising target for developing pharmaceuticals potentially useful to treat this vicious neurodegenerative condition. Aiming to contribute to the development of drugs with the reversible mechanism of MAO B inhibition only, herein, an extended in silico-in vitro procedure for the selection of novel MAO B inhibitors is demonstrated, including: (1) definition of optimized and validated structure-based (SB) 3-D QSAR models derived from available co-crystallized inhibitor-MAO B complexes; (2) elaboration of structure-activity relationships (SAR) features for either irreversible or reversible MAO B inhibitors to characterize and improve coumarin-based inhibitor activity (Protein Data Bank ID: 2V61) as the most potent reversible lead compound; (3) definition of structure-based (SB) and ligand-based (LB) alignment rules assessments by which virtually any untested potential MAO B inhibitor might be evaluated; (4) predictive ability validation of the best 3-D QSAR model through SB/LB modeling of four coumarin-based external test sets (267 compounds); (5) design and SB/LB alignment of novel coumarin-based scaffolds experimentally validated through synthesis and biological evaluation in vitro...
March 14, 2017: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/28288318/coumarin-sulfonates-new-alkaline-phosphatase-inhibitors-in%C3%A2-vitro-and-in-silico-studies
#19
Uzma Salar, Khalid Mohammed Khan, Jamshed Iqbal, Syeda Abida Ejaz, Abdul Hameed, Mariya Al-Rashida, Shahnaz Perveen, Muhammad Nawaz Tahir
A library of coumarin derived sulfonyl esters (1-38) was synthesized by reacting various hydroxy coumarins with different alkyl and aryl sulfonyl chlorides. All compounds were evaluated for their potential to inhibit alkaline phosphatases (hTNAP and hIAP). Most of the compounds were found to be inhibitors of APs. Compound 20 was found to be the most active hIAP inhibitor (IC50 = 1.11 ± 0.15 μM), whereas, compound 13 was found to be the most active hTNAP inhibitor (IC50 = 0.58 ± 0.17 μM). Detailed structure activity relationship studies (SAR), and molecular docking studies were carried out to identify structural elements necessary for AP inhibition, in addition to rationalize most probable binding site interaction of the inhibitors with the AP enzymes...
March 6, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28287723/sulfonamides-as-selective-nav1-7-inhibitors-optimizing-potency-and-pharmacokinetics-while-mitigating-metabolic-liabilities
#20
Matthew M Weiss, Thomas A Dineen, Isaac E Marx, Steven Altmann, Alessandro A Boezio, Howard Bregman, Margaret Y Chu-Moyer, Erin F DiMauro, Elma Feric Bojic, Robert S Foti, Hua Gao, Russell F Graceffa, Hakan Gunaydin, Angel Guzman-Perez, Hongbing Huang, Liyue Huang, Michael Jarosh, Thomas Kornecook, Charles R Kreiman, Joseph Ligutti, Daniel S La, Min-Hwa Jasmine Lin, Dong Liu, Bryan D Moyer, Hanh Nho Nguyen, Emily A Peterson, Paul E Rose, Kristin Taborn, Beth D Youngblood, Violeta L Yu, Robert T Fremeau
Several reports have recently emerged regarding the identification of heteroarylsulfonamides as NaV1.7 inhibitors that demonstrate high levels of selectivity over other NaV isoforms. The optimization of a series of internal NaV1.7 leads that address a number of metabolic liabilities including bioactivation, PXR activation, as well as CYP3A4 induction and inhibition led to the identification of potent and selective inhibitors that demonstrated favorable pharmacokinetic profiles and were devoid of the aforementioned liabilities...
March 13, 2017: Journal of Medicinal Chemistry
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