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https://www.readbyqxmd.com/read/28437766/cyanobacterial-lectins-characteristics-and-their-role-as-antiviral-agents
#1
REVIEW
Ram Sarup Singh, Amandeep Kaur Walia, Jasvirinder Singh Khattar, Davinder Pal Singh, John F Kennedy
Lectins are ubiquitous proteins/glycoproteins of non-immune origin that bind reversibly to carbohydrates in non-covalent and highly specific manner. These lectin-glycan interactions could be exploited for establishment of novel therapeutics, targeting the adherence stage of viruses and thus helpful in eliminating wide spread viral infections. Here the review focuses on the haemagglutination activity, carbohydrate specificity and characteristics of cyanobacterial lectins. Cyanobacterial lectins exhibiting high specificity towards mannose or complex glycans have potential role as anti-viral agents...
April 21, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28437591/fluorofenidone-attenuates-il-1%C3%AE-production-by-interacting-with-nlrp3-inflammasome-in-unilateral-ureteral-obstruction
#2
Linfeng Zheng, Jin Zhang, Xiangning Yuan, Juan Tang, Sisi Qiu, Zhangzhe Peng, Qiongjing Yuan, Yanyun Xie, Wenjuan Mei, Yiting Tang, Jie Meng, Gaoyun Hu, Lijian Tao
AIM: We explored whether Fluorofenidone reduced IL-1β production by interacting with NLRP3 inflammasome in unilateral ureteral obstruction (UUO). METHODS: UUO rats were treated with Fluorofenidone (500 mg · kg · d) for 3, 7 days. Morphologic analysis and leukocytes infiltration were assessed in ligated kidneys. Furthermore, plasmids of NLRP3, ASC, pro-Caspase-1, pro-IL-1β were co-transfected into 293 T cells, and then treated with Fluorofenidone (2 mM)...
April 24, 2017: Nephrology
https://www.readbyqxmd.com/read/28436902/learning-to-predict-consequences-as-a-method-of-knowledge-transfer-in-reinforcement-learning
#3
Eric Chalmers, Edgar Bermudez Contreras, Brandon Robertson, Artur Luczak, Aaron Gruber
The reinforcement learning (RL) paradigm allows agents to solve tasks through trial-and-error learning. To be capable of efficient, long-term learning, RL agents should be able to apply knowledge gained in the past to new tasks they may encounter in the future. The ability to predict actions' consequences may facilitate such knowledge transfer. We consider here domains where an RL agent has access to two kinds of information: agent-centric information with constant semantics across tasks, and environment-centric information, which is necessary to solve the task, but with semantics that differ between tasks...
April 17, 2017: IEEE Transactions on Neural Networks and Learning Systems
https://www.readbyqxmd.com/read/28436880/a-human-robot-co-manipulation-approach-based-on-human-sensorimotor-information
#4
Luka Peternel, Nikos Tsagarakis, Arash Ajoudani
This paper aims to improve the interaction and coordination between the human and the robot in cooperative execution of complex, powerful and dynamic tasks. We propose a novel approach that integrates online information about the human motor function and manipulability properties into the hybrid controller of the assistive robot. Through this human-inthe- loop framework, the robot can adapt to the human motor behaviour and provide the appropriate assistive response in different phases of the cooperative task...
April 17, 2017: IEEE Transactions on Neural Systems and Rehabilitation Engineering
https://www.readbyqxmd.com/read/28436713/modified-dextran-heparin-based-triggered-release-microspheres-for-cardiovascular-delivery-of-therapeutic-drugs-using-protamine-as-a-stimulus
#5
Hoai X Nguyen, Edgar A O'Rear
In this study, we describe the synthesis of an amine-modified acetalated dextran polymer which is combined with heparin (HP) as the basis for a novel controlled release system. Dextran-amine (DEXAM) conjugates, synthesized using reductive amination, were incorporated into DEXAM/HP microspheres. HP binds to positively charged ammonium ions of the DEXAM conjugates, contributing to the structural integrity of the microspheres. Crystal violet (CV) was encapsulated inside DEXAM/HP microspheres as a model drug to test the system...
April 24, 2017: Journal of Microencapsulation
https://www.readbyqxmd.com/read/28436514/cpg-loaded-mos2-nanosheets-as-multifunctional-agents-for-photothermal-enhanced-cancer-immunotherapy
#6
Qiusen Han, Xinhuan Wang, Xinghang Jia, Shuangfei Cai, Wei Liang, Yan Qin, Rong Yang, Chen Wang
Single or few-layered MoS2 nanosheets, as a novel class of 2D nanomaterials, have received tremendous attention due to their fantastic physical and chemical properties. Here, we fabricated MoS2-PEG-CpG with a small and uniform size as a multifunctional platform for photothermal enhanced immunotherapy. MoS2 nanosheets were fabricated by chemical exfoliation and further probe sonication. To realize MoS2-based adjuvant delivery, MoS2 nanosheets were functionalized with cytosine-phosphate-guanine (CpG) and polyethylene glycol (PEG) to form MoS2-PEG-CpG nanoconjugates...
April 24, 2017: Nanoscale
https://www.readbyqxmd.com/read/28436453/functional-thermodynamics-structural-and-biological-studies-of-in-silico-identified-inhibitors-of-mycobacterium-tuberculosis-enoyl-acp-coa-reductase-enzyme
#7
Leonardo K B Martinelli, Mariane Rotta, Anne D Villela, Valnês S Rodrigues-Junior, Bruno L Abbadi, Rogério V Trindade, Guilherme O Petersen, Giuliano M Danesi, Laura R Nery, Ivani Pauli, Maria M Campos, Carla D Bonan, Osmar Norberto de Souza, Luiz A Basso, Diogenes S Santos
Novel chemotherapeutics agents are needed to kill Mycobacterium tuberculosis, the main causative agent of tuberculosis (TB). The M. tuberculosis 2-trans-enoyl-ACP(CoA) reductase enzyme (MtInhA) is the druggable bona fide target of isoniazid. New chemotypes were previously identified by two in silico approaches as potential ligands to MtInhA. The inhibition mode was determined by steady-state kinetics for seven compounds that inhibited MtInhA activity. Dissociation constant values at different temperatures were determined by protein fluorescence spectroscopy...
April 24, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28436443/curcumol-allosterically-modulates-gaba-a-receptors-in-a-manner-distinct-from-benzodiazepines
#8
Yan-Mei Liu, Hui-Ran Fan, Jing Ding, Chen Huang, Shining Deng, Tailin Zhu, Tian-Le Xu, Wei-Hong Ge, Wei-Guang Li, Fei Li
Inhibitory A type γ-aminobutyric acid receptors (GABAARs) play a pivotal role in orchestrating various brain functions and represent an important molecular target in neurological and psychiatric diseases, necessitating the need for the discovery and development of novel modulators. Here, we show that a natural compound curcumol, acts as an allosteric enhancer of GABAARs in a manner distinct from benzodiazepines. Curcumol markedly facilitated GABA-activated currents and shifted the GABA concentration-response curve to the left in cultured hippocampal neurons...
April 24, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28436320/antibacterial-activity-of-desert-truffles-from-saudi-arabia-against-staphylococcus-aureus-and-pseudomonas-aeruginosa
#9
Domenico Schillaci, Maria Grazia Cusimano, Stella Maria Cascioferro, Vita Di Stefano, Vincenzo Arizza, Marco Chiaramonte, Luigi Inguglia, Abdulhakim Bawadekji, Salvatore Davino, Maria Letizia Gargano, Giuseppe Venturella
Medicinal mushrooms represent an unlimited source of polysaccharides with nutritional, antitumoral, antibacterial, and immune-stimulating properties. Traditional studies of epigeous higher Basidiomycetes have recently been joined by studies of hypogeous fungi and, in particular, of so-called desert truffles. With the aim to obtain novel agents against bacteria of clinical importance, we focused on the edible desert truffle mushrooms Tirmania pinoyi, Terfezia claveryi, and Picoa juniperi as sources of new antimicrobial agents...
2017: International Journal of Medicinal Mushrooms
https://www.readbyqxmd.com/read/28436164/synthesis-and-sar-study-of-novel-anticancer-protoflavone-derivatives-investigation-of-cytotoxicity-and-interaction-with-the-abcb1-and-abcg2-multidrug-efflux-transporters
#10
Balázs Dankó, Szilárd Tóth, Ana Martins, Vágvölgyi Máté, Norbert Kúsz, Joseph Molnár, Fang-Rong Chang, Yang-Chang Wu, Gergely Szakács, Attila Hunyadi
There is a constant need for new therapies against multidrug resistant (MDR) cancer. Natural compounds represent a promising class of novel anticancer agents. Recently, we have shown that protoflavones display activity in multidrug resistant cancer cell lines overexpressing the drug efflux pump P-glycoprotein. In the present study, 52 protoflavones, including 22 new derivatives were synthesized and tested against a panel of sensitive parental cells and their MDR derivatives obtained by transfection with the human ABCB1 or ABCG2 genes, or by adaptation to chemotherapeutics...
April 23, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28435985/elucidating-the-a%C3%AE-42-anti-aggregation-mechanism-of-action-of-tramiprosate-in-alzheimer-s-disease-integrating-molecular-analytical-methods-pharmacokinetic-and-clinical-data
#11
Petr Kocis, Martin Tolar, Jeremy Yu, William Sinko, Soumya Ray, Kaj Blennow, Howard Fillit, John A Hey
BACKGROUND: Amyloid beta (Aβ) oligomers play a critical role in the pathogenesis of Alzheimer's disease (AD) and represent a promising target for drug development. Tramiprosate is a small-molecule Aβ anti-aggregation agent that was evaluated in phase III clinical trials for AD but did not meet the primary efficacy endpoints; however, a pre-specified subgroup analysis revealed robust, sustained, and clinically meaningful cognitive and functional effects in patients with AD homozygous for the ε4 allele of apolipoprotein E4 (APOE4/4 homozygotes), who carry an increased risk for the disease...
April 24, 2017: CNS Drugs
https://www.readbyqxmd.com/read/28435886/discovery-of-a-novel-antifungal-agent-in-the-pathogen-box
#12
François L Mayer, James W Kronstad
Human fungal pathogens cause over 2 million infections per year and are major drivers of morbidity and mortality. Cryptococcus neoformans and Candida albicans are two of the most common fungal pathogens of humans, together accounting for a staggering 1.4 million infections annually, with very high mortality rates. Patients with dysfunctional immune systems, such as individuals with HIV/AIDS, are particularly susceptible to fungal infections. Unfortunately, relatively few antifungal drugs are currently available and fungi frequently develop resistance, further complicating treatment approaches...
March 2017: MSphere
https://www.readbyqxmd.com/read/28435533/discovery-of-antimalarial-azetidine-2-carbonitriles-that-inhibit-p-falciparum-dihydroorotate-dehydrogenase
#13
Micah Maetani, Nobutaka Kato, Valquiria A P Jabor, Felipe A Calil, Maria Cristina Nonato, Christina A Scherer, Stuart L Schreiber
Dihydroorotate dehydrogenase (DHODH) is an enzyme necessary for pyrimidine biosynthesis in protozoan parasites of the genus Plasmodium, the causative agents of malaria. We recently reported the identification of novel compounds derived from diversity-oriented synthesis with activity in multiple stages of the malaria parasite life cycle. Here, we report the optimization of a potent series of antimalarial inhibitors consisting of azetidine-2-carbonitriles, which we had previously shown to target P. falciparum DHODH in a biochemical assay...
April 13, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28435525/development-and-biological-evaluation-of-a-photoactivatable-small-molecule-microtubule-targeting-agent
#14
Alexander Döbber, Athena F Phoa, Ramzi H Abbassi, Brett W Stringer, Bryan W Day, Terrance G Johns, Mohammed Abadleh, Christian Peifer, Lenka Munoz
Photoremovable protecting groups added to bioactive molecules provide spatial and temporal control of the biological effects. We present synthesis and characterization of the first photoactivatable small-molecule tubulin inhibitor. By blocking the pharmacophoric OH group on compound 1 with photoremovable 4,5-dimethoxy-2-nitrobenzyl moiety we developed the photocaged prodrug 2 that had no effect in biological assays. Short UV light exposure of the derivative 2 or UV-irradiation of cells treated with 2 resulted in fast and potent inhibition of tubulin polymerization, attenuation of cell viability, and apoptotic cell death, implicating release of the parent active compound...
April 13, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28435454/dual-somatostatin-receptor-fdg-pet-ct-imaging-in-metastatic-neuroendocrine-tumours-proposal-for-a-novel-grading-scheme-with-prognostic-significance
#15
David Lh Chan, Nick Pavlakis, Geoffrey P Schembri, Elizabeth J Bernard, Edward Hsiao, Aimee Hayes, Tristan Barnes, Connie Diakos, Mustafa Khasraw, Jaswinder Samra, Enid Eslick, Paul J Roach, Alexander Engel, Stephen J Clarke, Dale L Bailey
Background: PET scans using FDG and somatostatin receptor imaging agents have both been used to study neuroendocrine tumours. Most reports have documented the sensitivity and specificity of each radiopharmaceutical independently, and even suggested the superiority of one over the other for different grades of disease. Aim: The aim of this work was to develop a grading scheme that describes the joint results of both the FDG and somatostatin receptor imaging PET scans in staging subjects with neuroendocrine tumours in a single combined parameter...
2017: Theranostics
https://www.readbyqxmd.com/read/28435450/exome-sequencing-of-oral-squamous-cell-carcinoma-reveals-molecular-subgroups-and-novel-therapeutic-opportunities
#16
Shih-Chi Su, Chiao-Wen Lin, Yu-Fan Liu, Wen-Lang Fan, Mu-Kuan Chen, Chun-Ping Yu, Wei-En Yang, Chun-Wen Su, Chun-Yi Chuang, Wen-Hsiung Li, Wen-Hung Chung, Shun-Fa Yang
Oral squamous cell carcinoma (OSCC), an epithelial malignancy affecting a variety of subsites in the oral cavity, is prevalent in Asia. The survival rate of OSCC patients has not improved over the past decades due to its heterogeneous etiology, genetic aberrations, and treatment outcomes. Improvement in therapeutic strategies and tailored treatment options is an unmet need. To unveil the mutational spectrum, whole-exome sequencing of 120 OSCC from male individuals in Taiwan was conducted. Analyzing the contributions of the five mutational signatures extracted from the dataset of somatic variations identified four groups of tumors that were significantly associated with demographic and clinical features...
2017: Theranostics
https://www.readbyqxmd.com/read/28435427/novel-4-thiazolidinone-derivatives-as-agonists-of-benzodiazepine-receptors-design-synthesis-and-pharmacological-evaluation
#17
Mehrdad Faizi, Reza Jahani, Seyed Abbas Ebadi, Sayyed Abbas Tabatabai, Elham Rezaee, Mehrnaz Lotfaliei, Mohsen Amini, Ali Almasirad
A new series of 4-chloro-N-(2-(substitutedphenyl)-4-oxothiazolidin-3-yl)-2-phenoxybenzamide derivatives were designed, synthesized and biologically evaluated as anticonvulsant agents. The designed compounds have the main essential functional groups for binding to the benzodiazepine receptors and 4-thiazolidinone ring as an anticonvulsant pharmacophore. Some of the new synthesized compounds showed considerable anticonvulsant activity in electroshock and pentylenetetrazole-induced lethal convulsion tests. Compound 5i, 4-chloro-N-(2-(4-methoxyphenyl)-4-oxothiazolidin-3-yl)-2-phenoxybenzamide, with the best activity was selected for evaluation of other benzodiazepine pharmacological effects...
2017: EXCLI journal
https://www.readbyqxmd.com/read/28435277/role-of-pirfenidone-in-the-management-of-pulmonary-fibrosis
#18
REVIEW
Keith C Meyer, Catherine A Decker
Pulmonary fibrosis is associated with a number of specific forms of interstitial lung disease (ILD) and can lead to progressive decline in lung function, poor quality of life, and, ultimately, early death. Idiopathic pulmonary fibrosis (IPF), the most common fibrotic ILD, affects up to 1 in 200 elderly individuals and has a median survival that ranges from 3 to 5 years following initial diagnosis. IPF has not been shown to respond to immunomodulatory therapies, but recent trials with novel antifibrotic agents have demonstrated lessening of lung function decline over time...
2017: Therapeutics and Clinical Risk Management
https://www.readbyqxmd.com/read/28435269/efficacy-of-silk-fibroin-nano-silver-against-staphylococcus-aureus-biofilms-in-a-rabbit-model-of-sinusitis
#19
Minghui Jia, Zhongchun Chen, Yongwei Guo, Xin Chen, Xia Zhao
BACKGROUND: Staphylococcus aureus biofilms contribute significantly to the recalcitrant nature of chronic rhinosinusitis. In previous studies, it has been shown that silk fibroin-nano silver solution can eliminate S. aureus biofilms in vitro, which suggests a potential role of this novel agent in the treatment of biofilm-associated diseases, such as sinusitis. OBJECTIVE: The aim of this study was to investigate the efficacy of silk fibroin-nano silver solution as a topical anti-biofilm agent in a rabbit model of sinusitis...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28435261/ph-sensitive-au-bsa-dox-fa-nanocomposites-for-combined-ct-imaging-and-targeted-drug-delivery
#20
He Huang, Da-Peng Yang, Minghuan Liu, Xiangsheng Wang, Zhiyong Zhang, Guangdong Zhou, Wei Liu, Yilin Cao, Wen Jie Zhang, Xiansong Wang
Albumin-based nanoparticles (NPs) as a drug delivery system have attracted much attention owing to their nontoxicity, non-immunogenicity, great stability and ability to bind to many therapeutic drugs. Herein, bovine serum albumin (BSA) was utilized as a template to prepare Au-BSA core/shell NPs. The outer layer BSA was subsequently conjugated with cis-aconityl doxorubicin (DOX) and folic acid (FA) to create Au-BSA-DOX-FA nanocomposites. A list of characterizations was undertaken to identify the successful conjugation of drug molecules and targeted agents...
2017: International Journal of Nanomedicine
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