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https://www.readbyqxmd.com/read/29786901/degradable-polymers-and-nanoparticles-built-from-salicylic-acid
#1
Saeed Akkad, Christopher J Serpell
As more evidence emerges supporting the possibility that nonsteroidal anti-inflammatory drugs, especially aspirin (acetyl salicylic acid), might have a role in the prevention and management of certain types of cancer, there have been several attempts to fabricate salicylic acid-based polymers that can be employed in the targeted therapy of tumors. The primary disadvantage so far has been in use of nontherapeutic polymeric backbones that constitute the majority of the therapeutic particle's size. The focus of this research is the creation of a biodegradable polymer consisting only of salicylic acid, and its use as the main building block in targeted nanotherapeutics that would consequently provide both high local dose and sustained release of the active moiety...
May 22, 2018: Macromolecular Rapid Communications
https://www.readbyqxmd.com/read/29786782/preclinical-impact-of-high-dose-intermittent-antiangiogenic-tyrosine-kinase-inhibitor-pazopanib-in-intrinsically-resistant-tumor-models
#2
Elaine Reguera-Nuñez, Shan Man, Ping Xu, Robert S Kerbel
Antiangiogenic tyrosine kinase inhibitors (TKIs) target vascular endothelial growth factor receptors and other receptor tyrosine kinases. As a result of toxicity, the clinical failures or the modest benefits associated with antiangiogenic TKI therapy may be related in some cases to suboptimal drug dosing and scheduling, thereby facilitating resistance. Most antiangiogenic TKIs, including pazopanib, are administered on a continuous daily basis. Here, instead, we evaluated the impact of increasing the dose and administering the drug intermittently...
May 21, 2018: Angiogenesis
https://www.readbyqxmd.com/read/29786768/risk-prediction-score-for-hiv-infection-development-and-internal-validation-with-cross-sectional-data-from-men-who-have-sex-with-men-in-china
#3
Lu Yin, Yuejuan Zhao, Meridith Blevins Peratikos, Liang Song, Xiangjun Zhang, Ruolei Xin, Zheya Sun, Yunan Xu, Li Zhang, Yifei Hu, Chun Hao, Yuhua Ruan, Yiming Shao, Sten H Vermund, Han-Zhu Qian
Receptive anal intercourse, multiple partners, condomless sex, sexually transmitted infections (STIs), and drug/alcohol addiction are familiar factors that correlate with increased human immunodeficiency virus (HIV) risk among men who have sex with men (MSM). To improve estimation to HIV acquisition, we created a composite score using questions from routine survey of 3588 MSM in Beijing, China. The HIV prevalence was 13.4%. A risk scoring tool using penalized maximum likelihood multivariable logistic regression modeling was developed, deploying backward step-down variable selection to obtain a reduced-form model...
May 21, 2018: AIDS and Behavior
https://www.readbyqxmd.com/read/29786660/molecular-targets-of-active-anticancer-compounds-derived-from-marine-sources
#4
REVIEW
Xiaoping Song, Ying Xiong, Xin Qi, Wei Tang, Jiajia Dai, Qianqun Gu, Jing Li
Over the past decades, a number of novel compounds, which are produced in the marine environment, have been found to exhibit the anticancer effects. This review focuses on molecular targets of marine-derived anticancer candidates in clinical and preclinical studies. They are kinases, transcription factors, histone deacetylase, the ubiquitin-proteasome system, and so on. Specific emphasis of this review paper is to provide information on the optimization of new target compounds for future research and development of anticancer drugs, based on the identification of structures of these target molecules and parallel compounds...
May 22, 2018: Marine Drugs
https://www.readbyqxmd.com/read/29786646/metabolic-reprogramming-by-3-iodothyronamine-t1am-a-new-perspective-to-reverse-obesity-through-co-regulation-of-sirtuin-4-and-6-expression
#5
Fariba M Assadi-Porter, Hannah Reiland, Martina Sabatini, Leonardo Lorenzini, Vittoria Carnicelli, Micheal Rogowski, Ebru S Selen Alpergin, Marco Tonelli, Sandra Ghelardoni, Alessandro Saba, Riccardo Zucchi, Grazia Chiellini
Obesity is a complex disease associated with environmental and genetic factors. 3-Iodothyronamine (T1AM) has revealed great potential as an effective weight loss drug. We used metabolomics and associated transcriptional gene and protein expression analysis to investigate the tissue specific metabolic reprogramming effects of subchronic T1AM treatment at two pharmacological daily doses (10 and 25 mg/kg) on targeted metabolic pathways. Multi-analytical results indicated that T1AM at 25 mg/kg can act as a novel master regulator of both glucose and lipid metabolism in mice through sirtuin-mediated pathways...
May 22, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29786643/controlled-deactivation-cb1-receptor-ligands-as-a-novel-strategy-to-lower-intraocular-pressure
#6
Sally Miller, Shashank Kulkarni, Alex Ciesielski, Spyros P Nikas, Ken Mackie, Alexandros Makriyannis, Alex Straiker
Nearly half a century has passed since the demonstration that cannabis and its chief psychoactive component Δ⁸-THC lowers intraocular pressure (IOP). Elevated IOP remains the chief hallmark and therapeutic target for glaucoma, a condition that places millions at risk of blindness. It is likely that Δ⁸-THC exerts much of its IOP-lowering effects via the activation of CB1 cannabinoid receptors. However, the initial promise of CB1 as a target for treating glaucoma has not thus far translated into a credible therapeutic strategy...
May 22, 2018: Pharmaceuticals
https://www.readbyqxmd.com/read/29786537/complete-two-year-follow-up-with-formal-non-inferiority-testing-on-primary-outcomes-of-the-aida-trial-comparing-the-absorb-bioresorbable-scaffold-with-the-xience-drug-eluting-metallic-stent-in-routine-pci
#7
Ruben Yannick G Tijssen, Robin P Kraak, Sjoerd H Hofma, Rene J van der Schaaf, Karin Arkenbout, Auke Weevers, Joelle Elias, Ivo M van Dongen, Karel T Koch, Jan Baan, Marije Vis, Robbert J de Winter, Jan J Piek, Jan G P Tijssen, Jose P S Henriques, Joanna J Wykrzykowska
AIMS: The aim of this report of the AIDA trial is to provide full two-year outcomes for the primary endpoint of target vessel failure (TVF) and an update on device thrombosis. METHODS AND RESULTS: AIDA was a single-blind, multicentre, investigator-initiated, non-inferiority, randomised (1:1) clinical trial. At complete two-year follow-up, the primary endpoint of TVF had occurred in 100 patients in the Absorb BVS arm versus 90 patients in the XIENCE EES arm (HR 1...
May 22, 2018: EuroIntervention
https://www.readbyqxmd.com/read/29786430/galaxygpcrloop-template-based-and-ab-initio-structure-sampling-of-the-extracellular-loops-of-g-protein-coupled-receptors
#8
Jonghun Won, Gyu Rie Lee, Hahnbeom Park, Chaok Seok
The second extracellular loops (ECL2s) of G-protein-coupled receptors (GPCRs) are often involved in GPCR functions, and their structures have important implications in drug discovery. However, structure prediction of ECL2 is difficult because of its long length and the structural diversity among different GPCRs. In this study, a new ECL2 conformational sampling method involving both template-based and ab initio sampling was developed. Inspired by observation of similar ECL2 structures of closely related GPCRs, a template-based sampling method employing loop structure templates selected from the structure database was developed...
May 22, 2018: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/29786422/mechanisms-regulating-the-association-of-protein-phosphatase-1-with-spinophilin-and-neurabin
#9
Michael C Edler, Asma B Salek, Darryl S Watkins, Harjot Kaur, Cameron W Morris, Bryan K Yamamoto, Anthony J Baucum
Protein phosphorylation is a key mediator of signal transduction, allowing for dynamic regulation of substrate activity. Whereas protein kinases obtain substrate specificity by targeting specific amino acid sequences, serine/threonine phosphatase catalytic subunits are much more promiscuous in their ability to dephosphorylate substrates. To obtain substrate specificity, serine/threonine phosphatases utilize targeting proteins to regulate phosphatase subcellular localization and catalytic activity. Spinophilin and its homolog neurabin are two of the most abundant dendritic spine-localized protein phosphatase 1 (PP1) targeting proteins...
May 22, 2018: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29785886/treatment-of-homozygous-familial-hypercholesterolaemia-in-paediatric-patients-a-monocentric-experience
#10
Paola S Buonuomo, Marina Macchiaiolo, Giovanna Leone, Paola Valente, Gerarda Mastrogiorgio, Maria Gnazzo, Ippolita Rana, Michaela V Gonfiantini, Maria G Gagliardi, Francesca Romano, Andrea Bartuli
Background Homozygous familial hypercholesterolaemia is a rare life-threatening disease characterized by markedly elevated low-density lipoprotein cholesterol (LDL-C) concentrations and accelerated atherosclerosis. The presence of double gene defects in the LDL-Receptor, either the same defect (homozygous) or two different LDL-raising mutations (compound heterozygotes) or other variants, identify the homozygous phenotype (HopFH). Apheresis is a procedure in which plasma is separated from red blood cells before the physical removal of LDL-C or the LDL-C is directly removed from whole blood...
January 1, 2018: European Journal of Preventive Cardiology
https://www.readbyqxmd.com/read/29785841/effects-of-antipsychotic-drugs-on-neurites-relevant-to-schizophrenia-treatment
#11
REVIEW
Xu-Feng Huang, Xueqin Song
Although antipsychotic drugs are mainly used for treating schizophrenia, they are widely used for treating various psychiatric diseases in adults, the elderly, adolescents and even children. Today, about 1.2% of the worldwide population suffers from psychosis and related disorders, which translates to about 7.5 million subjects potentially targeted by antipsychotic drugs. Neurites project from the cell body of neurons and connect neurons to each other to form neural networks. Deficits in neurite outgrowth and integrity are implicated in psychiatric diseases including schizophrenia...
May 22, 2018: Medicinal Research Reviews
https://www.readbyqxmd.com/read/29785837/more-patients-reach-glycaemic-control-with-fixed-ratio-combination-of-insulin-glargine-and-lixisenatide-iglarlixi-than-with-basal-insulin-at-12-weeks-of-treatment-a-post-hoc-time-to-control-analysis-of-lixilan-o-and-lixilan-l
#12
Juan Frias, Manuel Puig Domingo, Luigi Meneghini, Raffaele Napoli, Minzhi Liu, Erika Soltes Rak, Vanita R Aroda
This post hoc analysis of two 30-week clinical trials compared efficacy and hypoglycaemia outcomes at early study visits with iGlarLixi (insulin glargine U100 [iGlar] and lixisenatide) vs iGlar alone in patients with type 2 diabetes (T2D) uncontrolled on oral antidiabetic drugs (OADs; LixiLan-O) or basal insulin (LixiLan-L). Time to control, defined as days to achieve glycated haemoglobin (HbA1c) <7% or fasting plasma glucose (FPG) ≤7.2 mmol/L, was estimated using the Kaplan-Meier method. In LixiLan-O and -L, 60% and 46% of patients, respectively, reached HbA1c <7% with iGlarLixi at 12 weeks, vs 45% and 24%, respectively, with iGlar...
May 21, 2018: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/29785785/metabolism-within-the-tumor-microenvironment-and-its-implication-on-cancer-progression-an-ongoing-therapeutic-target
#13
REVIEW
Ma Carmen Ocaña, Beatriz Martínez-Poveda, Ana R Quesada, Miguel Ángel Medina
Since reprogramming energy metabolism is considered a new hallmark of cancer, tumor metabolism is again in the spotlight of cancer research. Many studies have been carried out and many possible therapies have been developed in the last years. However, tumor cells are not alone. A series of extracellular components and stromal cells, such as endothelial cells, cancer-associated fibroblasts, tumor-associated macrophages, and tumor-infiltrating T cells, surround tumor cells in the so-called tumor microenvironment (TME)...
May 22, 2018: Medicinal Research Reviews
https://www.readbyqxmd.com/read/29785773/molecular-tension-probes-to-investigate-the-mechanopharmacology-of-single-cells-a-step-toward-personalized-mechanomedicine
#14
Kornelia Galior, Victor Pui-Yan Ma, Yang Liu, Hanquan Su, Nusaiba Baker, Reynold A Panettieri, Cherry Wongtrakool, Khalid Salaita
Given that dysregulation of mechanics contributes to diseases ranging from cancer metastasis to lung disease, it is important to develop methods for screening the efficacy of drugs that target cellular forces. Here, nanoparticle-based tension sensors are used to quantify the mechanical response of individual cells upon drug treatment. As a proof-of-concept, the activity of bronchodilators is tested on human airway smooth muscle cells derived from seven donors, four of which are asthmatic. It is revealed that airway smooth muscle cells isolated from asthmatic donors exhibit greater traction forces compared to the control donors...
May 22, 2018: Advanced Healthcare Materials
https://www.readbyqxmd.com/read/29785705/association-of-gabaa-receptor-gene-with-epilepsy-syndromes
#15
Musadiq Ahmad Bhat, Sameer Ahmad Guru, Rashid Mir, Ajaz Ahmad Waza, Mariyam Zuberi, Mamta Pervin Sumi, Shaam Bodeliwala, Vinod Puri, Alpana Saxena
GABA has always been an inviting target in the etiology and treatment of epilepsy. The GABRA1, GABRG2, and GABRD genes provide instructions for making α1, ϒ2, and δ subunits of GABAA receptor protein respectively. GABAA is considered as one of the most important proteins and has found to play an important role in many neurological disorders. We explored the association of GABAA receptor gene mutation/SNPs in JME and LGS patients in Indian population. A total of 100 epilepsy syndrome patients (50 JME and 50 LGS) and 100 healthy control subjects were recruited and analyzed by AS-PCR and RFLP-PCR techniques...
May 21, 2018: Journal of Molecular Neuroscience: MN
https://www.readbyqxmd.com/read/29785683/targeted-therapies-and-adverse-drug-reactions-in-oncology-the-role-of-clinical-pharmacist-in-pharmacovigilance
#16
G Fornasier, M Taborelli, S Francescon, J Polesel, M Aliberti, P De Paoli, P Baldo
Background The majority of adverse drug reactions (ADRs) reported in the summary of product characteristics (SPCs) are based on pivotal clinical trials, performed under controlled conditions and with selected patients. Objectives (1) to observe ADRs in the real-world setting and to evaluate if the supervision of the pharmacist impacts on the management of ADRs and on the satisfaction of patients; (2) to sensitise health professionals and patients on the need to increase the reporting of ADRs, in compliance with Pharmacovigilance...
May 21, 2018: International Journal of Clinical Pharmacy
https://www.readbyqxmd.com/read/29785578/transport-of-the-pituitary-adenylate-cyclase-activating-polypeptide-across-the-blood-brain-barrier-implications-for-migraine
#17
Faisal Mohammad Amin, Henrik Winther Schytz
BACKGROUND: Pituitary adenylate cyclase-activating polypeptide (PACAP) is widely distributed in the nervous system and is involved in migraine pathophysiology. Understanding the function of the blood-brain barrier (BBB) in relation to PACAP is important to the understand the mechanisms behind PACAP-induced migraine attacks, but also to develop antimigraine drugs targeting the PACAP receptors Here, we aim to review the transport ability of PACAP across the BBB. METHODS: We performed a systematic literature search on PubMed to identify studies reporting original data on PACAP and BBB...
May 21, 2018: Journal of Headache and Pain
https://www.readbyqxmd.com/read/29785574/in-situ-nanostructured-hydrogel-of-resveratrol-for-brain-targeting-in-vitro-in-vivo-characterization
#18
Amarjitsing Rajput, Aditi Bariya, Ahmed Allam, Sarah Othman, Shital B Butani
The purpose of conducting the present research work was to develop resveratrol nanostructured in situ gel for the treatment of Alzheimer's disease. Resveratrol loaded lipid carrier was prepared by melt emulsification-probe sonication method, and the final product was evaluated for particle size (132 ± 11.90 nm), polydispersity index (0.209 ± 0.005), zeta potential (- 23 ± 3.79 mV), drug loading (9.26 ± 3.79%), and entrapment efficiency (74 ± 11.40%). Following incorporation of the resveratrol nanostructured lipid carrier in gellan gum and xanthan gum, in situ gel was formulated and characterized...
May 21, 2018: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/29785561/reptb-a-gene-ontology-based-drug-repurposing-approach-for-tuberculosis
#19
Anurag Passi, Neeraj Kumar Rajput, David J Wild, Anshu Bhardwaj
Tuberculosis (TB) is the world's leading infectious killer with 1.8 million deaths in 2015 as reported by WHO. It is therefore imperative that alternate routes of identification of novel anti-TB compounds are explored given the time and costs involved in new drug discovery process. Towards this, we have developed RepTB. This is a unique drug repurposing approach for TB that uses molecular function correlations among known drug-target pairs to predict novel drug-target interactions. In this study, we have created a Gene Ontology based network containing 26,404 edges, 6630 drug and 4083 target nodes...
May 21, 2018: Journal of Cheminformatics
https://www.readbyqxmd.com/read/29785484/challenges-in-malaria-management-and-a-glimpse-at-some-nanotechnological-approaches
#20
Adrian Najer, Cornelia G Palivan, Hans-Peter Beck, Wolfgang Meier
Malaria is a devastating infectious disease transmitted by mosquitoes, affecting millions of people and killing about half a million children each year. Despite tremendous progress in the control and elimination of malaria within the past years, there are still considerable challenges to be solved. To name a few, drug-resistant parasites, insecticide-resistant mosquitoes and the difficulty to formulate a potent malaria vaccine need to be addressed with new strategies to achieve the final goal of malaria eradication...
2018: Advances in Experimental Medicine and Biology
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