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https://www.readbyqxmd.com/read/28434203/topiramate-monotherapy-for-juvenile-myoclonic-epilepsy
#1
REVIEW
Jia Liu, Lu-Ning Wang, Yu-Ping Wang
BACKGROUND: Topiramate is a newer broad-spectrum antiepileptic drug (AED). Some studies have shown the benefits of topiramate monotherapy in the treatment of juvenile myoclonic epilepsy (JME). However, there are no current systematic reviews to determine the efficacy and tolerability of topiramate monotherapy in people with JME. This is an updated version of the original Cochrane Review published in Issue 12, 2015. OBJECTIVES: To evaluate the efficacy and tolerability of topiramate monotherapy in the treatment of JME...
April 23, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28434163/biomarkers-of-epileptogenesis-the-focus-on-glia-and-cognitive-dysfunctions
#2
Annamaria Vezzani, Rosaria Pascente, Teresa Ravizza
The need to find measures that reliably predict the onset of epilepsy after injurious events or how the patient will respond to anti-seizure drugs led to intensive pre-clinical and clinical research to discover non-invasive biomarkers that could increase the sensitivity of existing clinical indicators. The use of experimental models of epileptogenesis and of drug-resistance is instrumental to select the most promising approaches to explore such biomarkers in the pre-clinical setting for further clinical validation...
April 22, 2017: Neurochemical Research
https://www.readbyqxmd.com/read/28433941/self-assembled-dual-responsive-micelles-stabilized-with-protein-for-co-delivery-of-drug-and-sirna-in-cancer-therapy
#3
M R Aji Alex, Chetan Nehate, Srivani Veeranarayanan, D Sakthi Kumar, Ritu Kulshreshtha, Veena Koul
Design of safe and efficient vehicles for the combinatorial delivery of drugs and genetic agents is an emerging requisite for achieving enhanced therapeutic effect in cancer. Even though several nanoplatforms have been explored for the co-delivery of drugs and genetic materials the translation of these systems to clinical phase is still a challenge, mainly due to tedious synthesis procedures, lack of serum stability, inefficient scalability etc. Here in, we report development of reduction and pH sensitive polymeric graft of low molecular weight poly (styrene -alt -maleic anhydride) and evaluation of its efficacy in co-delivering drug and siRNA...
April 17, 2017: Biomaterials
https://www.readbyqxmd.com/read/28433886/controlled-release-of-metformin-from-chitosan-based-nanocomposite-films-containing-mesoporous-mcm-41-nanoparticles-as-novel-drug-delivery-systems
#4
Zahra Shariatinia, Zahra Zahraee
Biocompatible nanocomposite films based on blended chitosan and poly(ethylene glycol)-block-poly(propylene glycol)-block-poly(ethylene glycol) (BP) polymers containing metformin (MET) drug and MCM-41 or MCM-41-APS (APS=aminopropylsilane) nanoparticles (NPs) were designed and fabricated in order to prepare novel drug delivery systems which are useful for controlled drug release purposes. The total pore volume and mesopore volume of MCM-41 were measured equal to 1.08 and 1.05 cm(3)/g but those of MCM-41-APS were 0...
April 13, 2017: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/28433787/facile-encapsulation-of-hydroxycamptothecin-nanocrystals-into-zein-based-nanocomplexes-for-active-targeting-drug-delivery-and-cell-imaging
#5
Hongdi Wang, Wei Zhu, Yunna Huang, Zhixian Li, Yanbin Jiang, Qiuling Xie
Nano-drug delivery systems that integrate inorganic and organic or even bioactive components into a single nanoscale platform are playing a greatly important role in cancer treatment. Here, the fabrication of a versatile nanocarrier based on self-assembled structures of gold nanoparticles (AuNPs)-zein is reported, which displays high drug-loading efficiency for needle-shaped hydroxycamptothecin (HCPT) nanocrystals. The surface modification with folate-conjugated polydopamine (PFA) renders them stable and also facilitates their selective cellular internalization and enhancement of endocytosis...
April 19, 2017: Acta Biomaterialia
https://www.readbyqxmd.com/read/28433777/design-and-expeditious-synthesis-of-organosilanes-as-potent-antivirals-targeting-multidrug-resistant-influenza-a-viruses
#6
Yanmei Hu, Yuanxiang Wang, Fang Li, Chunlong Ma, Jun Wang
The efficacy of current influenza vaccines and small molecule antiviral drugs is curtailed by the emerging of multidrug-resistant influenza viruses. As resistance to the only FDA-approved oral influenza antiviral, oseltamivir (Tamiflu), continues to rise, there is a clear need to develop the next-generation of antiviral drugs. Since more than 95% of current circulating influenza A viruses carry the S31N mutation in their M2 genes, the AM2-S31N mutant proton channel represents an attractive target for the development of broad-spectrum antivirals...
April 19, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28433679/part-i-design-synthesis-and-biological-evaluation-of-novel-pyrazole-benzimidazole-conjugates-as-checkpoint-kinase-2-chk2-inhibitors-with-studying-their-activities-alone-and-in-combination-with-genotoxic-drugs
#7
Shadia A Galal, Ahmed S Abdelsamie, Samia A Shouman, Yasmin M Attia, Hamed I Ali, Ashraf Tabll, Reem El-Shenawy, Yasmine S El Abd, Mamdouh M Ali, Abeer E Mahmoud, Abeer H Abdel-Halim, Amal A Fyiad, Adel S Girgis, Hoda I El-Diwani
Activated checkpoint kinase 2 (Chk2) is a tumor suppressor as one of the main enzymes that affect the cell cycle. 2-Biarylbenzimidazoles are potent selective class of Chk2 inhibitors; the structure-based design was applied to synthesize a new series of this class with replacing the lateral aryl group by substituted pyrazoles. Ten pyrazole-benzimidazole conjugates from the best fifty candidates according to docking programs have been subjected to chemical synthesis in this study. The activities of the conjugates 5-14 as checkpoint kinase inhibitors and as antitumor alone and in combination with genotoxic drugs were evaluated...
April 14, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28433539/rationally-designed-pi3k%C3%AE-mutants-to-mimic-atr-and-their-use-to-understand-binding-specificity-of-atr-inhibitors
#8
Yipin Lu, Mark Knapp, Kenneth Crawford, Robert Warne, Robert Elling, Kelly Yan, Michael Doyle, Gwynn Pardee, Li Zhang, Sylvia Ma, Mulugeta Mamo, Elizabeth Ornelas, Yue Pan, Dirksen Bussiere, Johanna Jansen, Isabel Zaror, Albert Lai, Paul Barsanti, Janet Sim
ATR, a protein kinase in the PIKK family, plays a critical role in the cell DNA-damage response and is an attractive anticancer drug target. Several potent and selective inhibitors of ATR have been reported showing significant antitumor efficacy, with most advanced ones entering clinical trials. However, due to the absence of an experimental ATR structure, the determinants contributing to ATR inhibitors' potency and specificity are not well understood. Here we present the mutations in the ATP-binding site of PI3Kα to progressively transform the pocket to mimic that of ATR...
April 19, 2017: Journal of Molecular Biology
https://www.readbyqxmd.com/read/28433515/understanding-clinical-development-of-chimeric-antigen-receptor-t-cell-therapies
#9
Sofieke de Wilde, Henk-Jan Guchelaar, Maarten Laurens Zandvliet, Pauline Meij
BACKGROUND AIMS: In the past decade, many clinical trials with gene- and cell-based therapies (GCTs) have been performed. Increased interest in the development of these drug products by various stakeholders has become apparent. Despite this growth in clinical studies, the number of therapies receiving marketing authorization approval (MAA) is lagging behind. To enhance the success rate of GCT development, it is essential to better understand the clinical development of these products...
April 19, 2017: Cytotherapy
https://www.readbyqxmd.com/read/28433511/design-synthesis-and-pharmacological-evaluation-of-4-azolyl-benzamide-derivatives-as-novel-gpr52-agonists
#10
Kazuyuki Tokumaru, Yoshiteru Ito, Izumi Nomura, Takashi Nakahata, Yuji Shimizu, Emi Kurimoto, Kazunobu Aoyama, Kazuyoshi Aso
G protein-coupled receptor 52 (GPR52) agonists are expected to improve the symptoms of psychiatric disorders. During exploration for a novel class of GPR52 agonists with good pharmacokinetic profiles, we synthesized 4-(3-(3-fluoro-5-(trifluoromethyl)benzyl)-5-methyl-1H-1,2,4-triazol-1-yl)-2-methylbenzamide (4u; half maximal effective concentration (EC50)=75nM, maximal response (Emax)=122%) starting from a high-throughput screening hit 3 (EC50=470nM, Emax=56%). The structural features of a reported GPR52 agonist were applied to 3, led to design 4-azolylbenzamides as novel GPR52 agonists...
April 1, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28432957/nanoencapsulation-strategies-for-the-delivery-of-novel-bifunctional-antioxidant-%C3%AF-1-selective-ligands
#11
Claudia Carbone, Emanuela Arena, Veronica Pepe, Orazio Prezzavento, Ivana Cacciatore, Hasan Turkez, Agostino Marrazzo, Antonio Di Stefano, Giovanni Puglisi
Nowadays sigma-1 receptors are considered as new therapeutic objectives for central nervous system neurodegenerative diseases. Among different molecules, alpha lipoic acid has been identified as a natural potent antioxidant drug, whose therapeutic efficacy is limited by its many drawbacks, such as fast metabolism, poor bioavailability and high physico-chemical instability. Alfa-lipoic acid derivatives have been recently developed demonstrating their neuroprotective activity and effectiveness in different types of oxidative stress...
April 12, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28432913/spontaneously-formed-redox-and-ph-sensitive-polymersomes-by-mpeg-based-cytocompatible-random-copolymers
#12
Partha Laskar, Joykrishna Dey, Sudip Kumar Ghosh
Stimuli-sensitive polymersomes are one of the important vehicles and have been extensively studied as smart drug delivery system. Polymersomes have added advantage over the micelles because of having the ability to carry not only hydrophobic but also hydrophilic guest in their aqueous core. Among various stimuli, the change of pH and redox reaction is very important for drug delivery purpose especially for anticancer drug. Therefore, in this work, two poly(ethylene glycol) methyl ether methacrylate (mPEG) containing hydrophilic random anionic copolymers, poly[(2-hydroxyethyl methacrylate-3,3'-dithiodipropanoic acid)x-co-(poly(ethylene glycol) methyl ether methacrylate)y], poly[(HEMA-DTDPA)x-co-mPEGy] with different copolymer ratios were designed and synthesized...
April 12, 2017: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/28432761/protein-s-sulfhydration-by-hydrogen-sulfide-in-cardiovascular-system
#13
REVIEW
Guoliang Meng, Shuang Zhao, Liping Xie, Yi Han, Yong Ji
Hydrogen sulfide (H2 S), independent on any specific transporters, plays a number of biological effects on cardiovascular systems. However, the detailed mechanism of H2 S is not yet clear until now. Recently, a novel post-translational modification induced by H2 S, named S-sulfhydration, has been proposed. S-sulfhydration is a chemical modification on specific cysteine residues of target proteins by H2 S. There are several methods for S-sulfhydration detection, such as modified biotin switch assay, maleimide assay with fluorescent thiol modifying regents, tag-switch method and mass spectrometry...
April 22, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28432657/in-vitro-assay-for-measuring-real-time-topotecan-release-from-liposomes-release-kinetics-and-cellular-internalization
#14
Roger Gilabert-Oriol, Lina Chernov, Malathi Anantha, Wieslawa H Dragowska, Marcel B Bally
Topotecan is a drug that is under investigation for the treatment of neuroblastoma and has been encapsulated into liposomes to improve its therapeutic efficacy. However, liposomal formulations still need to be optimized for drug retention and new techniques to measure drug release are required to better understand this process. Here, a novel in vitro method based on fluorescence de-quenching and an automated microscopy imaging platform were developed for monitoring, in real time, the release of topotecan from a liposomal formulation...
April 21, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28432615/fabrication-physicochemical-characterization-and-performance-evaluation-of-biodegradable-polymeric-microneedle-patch-system-for-enhanced-transcutaneous-flux-of-high-molecular-weight-therapeutics
#15
Viral Shah, Bijaya Krushna Choudhury
A revolutionary paradigm shift is being observed currently, towards the use of therapeutic biologics for disease management. The present research was focused on designing an efficient dosage form for transdermal delivery of α-choriogonadotropin (high molecular weight biologic), through biodegradable polymeric microneedles. Polyvinylpyrrolidone-based biodegradable microneedle arrays loaded with high molecular weight polypeptide, α-choriogonadotropin, were fabricated for its systemic delivery via transdermal route...
April 21, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28432573/clinical-outcomes-in-trials-evaluating-lipid-lowering-drugs
#16
REVIEW
Julie Butters, Alex Brown, Liddy Griffith, Susan Kim, Stephen J Nicholls
While statins have formed the cornerstone of strategies for cardiovascular prevention, the residual risk related to low-density lipoprotein cholesterol (LDL-C) and other lipoprotein factors provides a landscape for development of new therapies. However, a number of lipid-modifying therapies have failed to reduce cardiovascular event rates in contemporary clinical trials of statin-treated patients. The factors considered in outcome measure selection for clinical trials of novel lipid-lowering therapies are reviewed...
April 21, 2017: American Journal of Cardiovascular Drugs: Drugs, Devices, and Other Interventions
https://www.readbyqxmd.com/read/28432531/effectiveness-of-nanoencapsulated-methotrexate-against-osteosarcoma-cells-in-vitro-cytotoxicity-under-dynamic-conditions
#17
O Mitxelena-Iribarren, C L Hisey, M Errazquin-Irigoyen, Y González-Fernández, E Imbuluzqueta, M Mujika, M J Blanco-Prieto, S Arana
Cancer is a leading cause of mortality in the world, with osteosarcoma being one of the most common types among children between 1 and 14 years old. Current treatments including preoperative chemotherapy, surgery and postoperative chemotherapy produce several side effects with limited effectiveness. The use of lipid nanoparticles as biodegradable shells for controlled drug delivery shows promise as a more effective and targeted tumor treatment. However, in vitro validation of these vehicles is limited due to fluid stagnation in current techniques, in which nanoparticles sediment onto the bottom of the wells killing the cells by asphyxiation...
June 2017: Biomedical Microdevices
https://www.readbyqxmd.com/read/28432265/artemida-trial-a-randomized-trial-of-efficacy-12-months-international-double-blind-actovegin-a-randomized-controlled-trial-to-assess-the-efficacy-of-actovegin-in-poststroke-cognitive-impairment
#18
Alla Guekht, Ingmar Skoog, Sally Edmundson, Vladimir Zakharov, Amos D Korczyn
BACKGROUND AND PURPOSE: Poststroke cognitive impairment is a debilitating consequence of stroke. The aim of this study was to assess whether Actovegin confers cognitive benefit in patients who have had an ischemic stroke. METHODS: This was a 12-month, parallel-group, randomized, multicenter, double-blind, placebo-controlled study. Eligible patients were ≥60 years of age with a Montreal Cognitive Assessment test score of ≤25 points. Patients were randomized into 2 groups within 1 week of acute supratentorial ischemic stroke in a 1:1 ratio: Actovegin (a deproteinized hemoderivative of calf blood, 2000 mg/d for ≤20 intravenous infusions followed by 1200 mg/d orally) or placebo for 6 months...
April 21, 2017: Stroke; a Journal of Cerebral Circulation
https://www.readbyqxmd.com/read/28432226/everolimus-plus-exemestane-in-advanced-breast-cancer-safety-results-of-the-ballet-study-on-patients-previously-treated-without-and-with-chemotherapy-in-the-metastatic-setting
#19
Daniele Generali, Filippo Montemurro, Roberto Bordonaro, Antonino Mafodda, Sante Romito, Andrea Michelotti, Pierluigi Piovano, Maria Teresa Ionta, Claudia Bighin, Donata Sartori, Antonio Frassoldati, Marina Elena Cazzaniga, Ferdinando Riccardi, Franco Testore, Patrizia Vici, Carlo Antonio Barone, Alessio Schirone, Federico Piacentini, Franco Nolè, Annamaria Molino, Luciano Latini, Edda Lucia Simoncini, Fausto Roila, Francesco Cognetti, Francesco Nuzzo, Jennifer Foglietta, Alessandro Marco Minisini, Francesca Goffredo, Giuseppe Portera, Gilda Ascione, Gabriella Mariani
BACKGROUND: The BALLET study was an open-label, multicenter, expanded access study designed to allow treatment with everolimus plus exemestane in postmenopausal women with hormone receptor-positive metastatic breast cancer progressed following prior endocrine therapy. A post hoc analysis to evaluate if previous chemotherapy in the metastatic setting affects the safety profile of the combination regimen of everolimus and exemestane was conducted on the Italian subset, as it represented the major part of the patients enrolled (54%)...
April 21, 2017: Oncologist
https://www.readbyqxmd.com/read/28432051/impact-of-study-outcome-on-submission-and-acceptance-metrics-for-peer-reviewed-medical-journals-six-year-retrospective-review-of-all-completed-glaxosmithkline-human-drug-research-studies
#20
Gary Evoniuk, Bernadette Mansi, Barbara DeCastro, Jennie Sykes
Objectives To determine whether the outcome of drug studies influenced submission and/or acceptance rates for publication in peer reviewed medical journals.Design A six year retrospective review of publication status by study outcome for all human drug research studies conducted by a single industry sponsor (GlaxoSmithKline) that completed from 1 January 2009 to 30 June 2014 and were therefore due for manuscript submission (per the sponsor's policy) to peer reviewed journals within 18 months of study completion-that is, 31 December 2015...
April 21, 2017: BMJ: British Medical Journal
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