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https://www.readbyqxmd.com/read/28109167/cell-cycle-tailored-targeting-of-metastatic-melanoma-challenges-opportunities
#1
Nikolas K Haass, Brian Gabrielli
The advent of targeted therapies of metastatic melanoma, such as MAPK pathway inhibitors and immune checkpoint antagonists, has turned dermato-oncology from the 'bad guy' to the 'poster child' in oncology. Current targeted therapies are effective; although here is a clear need to develop combination therapies to delay the onset of resistance. Many anti-melanoma drugs impact on the cell cycle but are also dependent on certain cell cycle phases resulting in cell cycle phase-specific drug insensitivity. Here, we raise the question: Have combination trials been abandoned prematurely as ineffective possibly only because drug scheduling was not optimized? Firstly, if both drugs of a combination hit targets in the same melanoma cell, cell cycle-mediated drug insensitivity should be taken into account when planning combination therapies, timing of dosing schedules and choice of drug therapies in solid tumors...
January 21, 2017: Experimental Dermatology
https://www.readbyqxmd.com/read/28109089/betulinic-acid-inhibits-cell-proliferation-in-human-oral-squamous-cell-carcinoma-via-modulating-ros-regulated-p53-signaling
#2
Huan Shen, Li Liu, Yongjin Yang, Wenxing Xun, Kewen Wei, Guang Zeng
Oral squamous cell carcinoma (OSCC) is a common cancer of the head and neck. Betulinic acid (BA) is a naturally occurring pentacyclic triterpenoid. The present study was designed to explore the effects of BA on OSCC KB cell proliferation <em>in vitro</em> and implanted tumor growth <em>in vivo</em> and to examine the possible molecular mechanisms. The results showed that BA dose-dependently inhibited KB cell proliferation and decreased implanted tumor volume. In addition, BA significantly promoted mitochondrial apoptosis, as reflected by increase of TUNEL-positive cells and activities of caspase 3 and 9, increase of Bax expression and decrease of Bcl-2 expression and mitochondrial oxygen consumption rate...
January 20, 2017: Oncology Research
https://www.readbyqxmd.com/read/28109047/novel-antiplatelet-role-for-a-protein-disulfide-isomerase-targeted-peptide-evidence-of-covalent-binding-to-c-terminal-cghc-redox-motif
#3
H R Sousa, R S Gaspar, E M L Sena, S A da Silva, J L de L Fontelles, T L S Araújo, M Mastrogiovanni, D M Fries, A P S Azevedo-Santos, F R M Laurindo, A Trostchansky, A M Paes
Protein disulfide isomerase (PDI) plays a major role in platelet aggregation and its inhibitors have emerged as novel antithrombotic drugs. In previous work, we designed a peptide based on PDI redox motif (CGHC) that inhibited both PDI reductase activity and PDI-modulated superoxide generation by neutrophil Nox2. Thus, we hypothesized this peptide would also inhibit platelet aggregation by association to surface PDI. Three peptides were used: CxxC, containing the PDI redox motif; Scr, presenting a scrambled sequence of the same residues and AxxA, with cysteines replaced by alanine...
January 21, 2017: Journal of Thrombosis and Haemostasis: JTH
https://www.readbyqxmd.com/read/28108974/design-and-evaluation-of-topical-diclofenac-sodium-gel-using-hot-melt-extrusion-technology-as-a-continuous-manufacturing-process-with-kolliphor%C3%A2-p407
#4
Jaywant Pawar, Rajkiran Narkhede, Purnima Amin, Vaishali Tawde
The aim of the present context was to develop and evaluate a Kolliphor® P407-based transdermal gel formulation of diclofenac sodium by hot melt extrusion (HME) technology; central composite design was used to optimize the formulation process. In this study, we have explored first time ever HME as an industrially feasible and continuous manufacturing technology for the manufacturing of gel formulation using Kolliphor® P407 and Kollisolv® PEG400 as a gel base. Diclofenac sodium was used as a model drug. The HME parameters such as feeding rate, screw speed, and barrel temperature were crucial for the semisolid product development, and were optimized after preliminary trials...
January 20, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28108898/bioresorbable-scaffolds-for-coronary-artery-disease
#5
REVIEW
Ashwin Nathan, Taisei Kobayashi, Daniel M Kolansky, Robert L Wilensky, Jay Giri
PURPOSE OF REVIEW: The purpose of this review is to present an overview of the recent evidence regarding the use of bioresorbable scaffolds in percutaneous coronary intervention. RECENT FINDINGS: Bioresorbable scaffolds represent a potentially unique engineering solution to the problems associated with metallic stents. The Absorb everolimus-eluting bioresorbable scaffold has been the most extensively tested of this class and is currently Food and Drug Administration-approved for use in the USA...
January 2017: Current Cardiology Reports
https://www.readbyqxmd.com/read/28108896/pharmacophore-based-screening-and-drug-repurposing-exemplified-on-glycogen-synthase-kinase-3-inhibitors
#6
Luminita Crisan, Sorin Avram, Liliana Pacureanu
The current study was conducted to elaborate a novel pharmacophore model to accurately map selective glycogen synthase kinase-3 (GSK-3) inhibitors, and perform virtual screening and drug repurposing. Pharmacophore modeling was developed using PHASE on a data set of 203 maleimides. Two benchmarking validation data sets with focus on selectivity were assembled using ChEMBL and PubChem GSK-3 confirmatory assays. A drug repurposing experiment linking pharmacophore matching with drug information originating from multiple data sources was performed...
January 21, 2017: Molecular Diversity
https://www.readbyqxmd.com/read/28108595/identification-of-the-adpr-binding-pocket-in-the-nudt9-homology-domain-of-trpm2
#7
Peilin Yu, Xiwen Xue, Jianmin Zhang, Xupang Hu, Yan Wu, Lin-Hua Jiang, Hongwei Jin, Jianhong Luo, Liangren Zhang, Zhenming Liu, Wei Yang
Activation of the transient receptor potential melastatin 2 (TRPM2) channel occurs during the response to oxidative stress under physiological conditions as well as in pathological processes such as ischemia and diabetes. Accumulating evidence indicates that adenosine diphosphate ribose (ADPR) is the most important endogenous ligand of TRPM2. However, although it is known that ADPR binds to the NUDT9 homology (NUDT9-H) domain in the intracellular C-terminal region, the molecular mechanism underlying ADPR binding and activation of TRPM2 remains unknown...
January 20, 2017: Journal of General Physiology
https://www.readbyqxmd.com/read/28108380/the-taste-of-heat-how-humoral-qualities-act-as-a-cultural-filter-for-chemosensory-properties-guiding-herbal-medicine
#8
Matthias S Geck, Stefano Cabras, Laura Casu, Alberto J Reyes García, Marco Leonti
ETHNOPHARMACOLOGICAL RELEVANCE: Organoleptic properties, and more specifically chemosensory cues, have been shown to guide therapeutic applications of medicinal plants. Humoral qualities, on the other hand, are widely believed to be an abstract concept, mainly applied post hoc to validate therapy. However, the nexus between humoral qualities, chemosensory properties, and medicinal plant uses has never been systematically assessed. AIM OF THE STUDY: To systematically analyse the correlations between chemosensory properties, humoral qualities, and medicinal uses of selected botanical drugs...
January 17, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28108249/synthesis-and-biological-evaluation-of-thiazole-derivatives-as-novel-usp7-inhibitors
#9
Chao Chen, Jiemei Song, Jinzheng Wang, Chang Xu, Caiping Chen, Wei Gu, Hongbin Sun, Xiaoan Wen
Herpesvirus-associated Ubiquitin-Specific Protease (HAUSP, also called USP7) interacts with and stabilizes Mdm2, and represents one of the first examples that deubiquitinases oncogenic proteins. USP7 has been regarded as a potential drug target for cancer therapy. Inhibitors of USP7 have been recently shown to suppress tumor cell growth in vitro and in vivo. Based on leading USP7 inhibitors P5091 and P22077, we designed and synthesized a series of thiazole derivatives. The results of in vitro assays showed that the thiazole compounds exhibited low micromolar inhibition activity against both USP7 enzyme and cancer cell lines...
January 10, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28108242/evaluation-of-the-antimicrobial-activity-of-the-mastoparan-polybia-mpii-isolated-from-venom-of-the-social-wasp-pseudopolybia-vespiceps-testacea-vespidae-hymenoptera
#10
Juliana C Silva, Lázaro M Neto, Rogério C Neves, Jaqueline C Gonçalves, Monalisa M Trentini, Ricardo Mucury-Filho, Karina S Smidt, Isabel C Fensterseifer, Osmar N Silva, Lilian D Lima, Patricia B Clissa, Nathália Vilela, Fernanda Guilhelmelli, Luciano P Silva, Marisa Rangel, André Kipnis, Ildinete Silva-Pereira, Octavio L Franco, Ana P Junqueira-Kipnis, Anamelia L Bocca, Márcia R Mortari
Mastoparans, a class of peptides found in wasp venom, have significant effects following a sting as well as useful applications in clinical practice. Among these is their potential use in the control of micro-organisms that cause infectious diseases with a significant impact on society. Thus, the present study describes the isolation and identification of a mastoparan peptide from the venom of the social wasp Pseudopolybia vespiceps and evaluated its antimicrobial profile against bacteria (Staphylococcus aureus and Mycobacterium abscessus subsp...
January 9, 2017: International Journal of Antimicrobial Agents
https://www.readbyqxmd.com/read/28108211/user-centered-design-improves-the-usability-of-drug-drug-interaction-alerts-experimental-comparison-of-interfaces
#11
Daniel R Luna, Daniel A Rizzato Lede, Carlos M Otero, Marcelo R Risk, Fernán González Bernaldo de Quirós
Clinical Decision Support Systems can alert health professionals about drug interactions when they prescribe medications. The Hospital Italiano de Buenos Aires in Argentina developed an electronic health record with drug-drug interaction alerts, using traditional software engineering techniques and requirements. Despite enhancing the drug-drug interaction knowledge database, the alert override rate of this system was very high. We redesigned the alert system using user-centered design (UCD) and participatory design techniques to enhance the drug-drug interaction alert interface...
January 17, 2017: Journal of Biomedical Informatics
https://www.readbyqxmd.com/read/28108176/differential-housing-and-novelty-response-protection-and-risk-from-locomotor-sensitization
#12
Erik J Garcia, Tara N Haddon, Donald A Saucier, Mary E Cain
: High novelty seeking increases the risk for drug experimentation and locomotor sensitization. Locomotor sensitization to psychostimulants is thought to reflect neurological adaptations that promote the transition to compulsive drug taking. Rats reared in enrichment (EC) show less locomotor sensitization when compared to rats reared in isolation (IC) or standard conditions (SC). The current research study was designed to test if novelty response contributed locomotor sensitization and more importantly, if the different housing environments could change the novelty response to protect against the development of locomotor sensitization in both adolescence and adulthood...
January 17, 2017: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/28108125/interventions-to-support-risk-and-benefit-understanding-of-disease-modifying-drugs-in-multiple-sclerosis-patients-a-systematic-review
#13
REVIEW
Gurpreet K Reen, Eli Silber, Dawn W Langdon
OBJECTIVE: The present review evaluates interventions that have been designed to improve understanding of the complex risk-benefit profiles of disease-modifying drugs (DMDs) in patients with Multiple Sclerosis (MS). METHODS: A systematic search conducted using PubMed, Embase, Google Scholar and PsycINFO identified 15 studies. Interventions which provided treatment information were present across a range of study designs. A narrative synthesis was conducted due to heterogeneity of research findings...
December 28, 2016: Patient Education and Counseling
https://www.readbyqxmd.com/read/28108082/analysis-of-drugs-of-abuse-in-human-plasma-using-microextraction-by-packed-sorbents-and-ultra-high-performance-liquid-chromatography
#14
P Fernández, M González, M Regenjo, A M Ares, A M Fernández, R A Lorenzo, A M Carro
A miniaturized and simple method based on digitally programmed microextraction by packed sorbent (eVol(®)-MEPS) coupled to ultra-performance liquid chromatography (UPLC) has been developed for quantitative determination of three synthetic cathinones and seven conventional drugs of abuse and metabolites. The influence of several extraction parameters, such as washing and elution solvents were tested. In addition important variables affecting MEPS performance, namely sample volume, sorbent drying time, washing solvent volume, elution volume, number of extraction cycles, sorbent phase and pH, were evaluated using an asymmetrical screening design...
January 16, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28107913/quantitative-structure-retention-relationship-model-for-the-determination-of-naratriptan-hydrochloride-and-its-impurities-based-on-artificial-neural-networks-coupled-with-genetic-algorithm
#15
Mikołaj Mizera, Anna Krause, Przemysław Zalewski, Robert Skibiński, Judyta Cielecka-Piontek
Mathematical modeling of Quantitative Structure - Property Relationships met great interest in fields of in silico drug design and more recently, pharmaceutical analysis. In our approach we proposed automated method of creation Quantitative Structure-Retention Relationship (QSRR) for analysis of triptans, selective serotonin 5-HT1 receptor agonists used for the treatment of acute headache. The method was created using hybrid machine learning approach, namely Genetic algorithm (GA) coupled with artificial neutral networks (ANN)...
March 1, 2017: Talanta
https://www.readbyqxmd.com/read/28107680/a-randomized-clinical-trial-of-buprenorphine-for-prisoners-findings-at-12-months-post-release
#16
Michael S Gordon, Timothy W Kinlock, Robert P Schwartz, Kevin E O'Grady, Terrence T Fitzgerald, Frank J Vocci
BACKGROUND: This study examined whether starting buprenorphine treatment prior to prison and after release from prison would be associated with better drug treatment outcomes and whether males and females responded differently to the combination of in-prison treatment and post-release service setting. METHODS: Study design was a 2 (In-Prison Treatment: Condition: Buprenorphine Treatment: vs. Counseling Only)×2 [Post-Release Service Setting Condition: Opioid Treatment: Program (OTP) vs...
January 11, 2017: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/28107561/beta-blockers-for-hypertension
#17
REVIEW
Charles S Wiysonge, Hazel A Bradley, Jimmy Volmink, Bongani M Mayosi, Lionel H Opie
BACKGROUND: Beta-blockers refer to a mixed group of drugs with diverse pharmacodynamic and pharmacokinetic properties. They have shown long-term beneficial effects on mortality and cardiovascular disease (CVD) when used in people with heart failure or acute myocardial infarction. Beta-blockers were thought to have similar beneficial effects when used as first-line therapy for hypertension. However, the benefit of beta-blockers as first-line therapy for hypertension without compelling indications is controversial...
January 20, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28107320/chemotherapy-safe-handling-limiting-nursing-exposure-with-a-hazardous-drug-control-program
#18
Rachael Crickman
BACKGROUND: Nurses and other healthcare workers are at risk for adverse health consequences from occupational exposure to hazardous drugs. 
. OBJECTIVES: An evidence-based program for nurses was implemented to improve safe handling practices and reduce exposure to hazardous drugs. 
. METHODS: A quasiexperimental design was used, with pre- and post-tests of knowledge about chemotherapy exposure and pre- and post-test observations of compliance with donning and doffing personal protective equipment (PPE)...
February 1, 2017: Clinical Journal of Oncology Nursing
https://www.readbyqxmd.com/read/28106982/a-novel-iron-ii-preferring-dopamine-agonist-chelator-as-potential-symptomatic-and-neuroprotective-therapeutic-agent-for-parkinson-s-disease
#19
Banibrata Das, Ashoka Kandegedara, Liping Xu, Tamara Antonio, Timothy L Stemmler, Maarten E A Reith, Aloke K Dutta
Parkinson's disease (PD) is a progressive neurodegenerative disorder and development of disease-modifying treatment is still an unmet medical need. Considering the implication of free iron (II) in PD, we report here the design and characterization of a novel hybrid iron chelator, (-)-12 (D-607) as a multitarget-directed ligand against PD. Binding and functional assays at dopamine D2/D3 receptors indicate potent agonist activity of (-)-12. The molecule displayed an efficient preferential iron (II) chelation properties along with potent in vivo activity in a reserpinized PD animal model...
January 20, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28106947/3d-bioprinting-and-its-in-vivo-applications
#20
REVIEW
Nhayoung Hong, Gi-Hoon Yang, JaeHwan Lee, GeunHyung Kim
The purpose of 3D bioprinting technology is to design and create functional 3D tissues or organs in situ for in vivo applications. 3D cell-printing, or additive biomanufacturing, allows the selection of biomaterials and cells (bioink), and the fabrication of cell-laden structures in high resolution. 3D cell-printed structures have also been used for applications such as research models, drug delivery and discovery, and toxicology. Recently, numerous attempts have been made to fabricate tissues and organs by using various 3D printing techniques...
January 20, 2017: Journal of Biomedical Materials Research. Part B, Applied Biomaterials
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