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https://www.readbyqxmd.com/read/28651376/comparison-of-sampling-strategies-for-tobacco-retailer-inspections-to-maximize-coverage-in-vulnerable-areas-and-minimize-cost
#1
Joseph G L Lee, Bonnie E Shook-Sa, J Michael Bowling, Kurt M Ribisl
Introduction: In the United States, tens of thousands of inspections of tobacco retailers are conducted each year. Various sampling choices can reduce travel costs, emphasize enforcement in areas with greater non-compliance, and allow for comparability between states and over time. We sought to develop a model sampling strategy for state tobacco retailer inspections. Methods: Using a 2014 list of 10,161 North Carolina tobacco retailers, we compared results from simple random sampling; stratified, clustered at the ZIP code sampling; and, stratified, clustered at the census tract sampling...
June 23, 2017: Nicotine & Tobacco Research: Official Journal of the Society for Research on Nicotine and Tobacco
https://www.readbyqxmd.com/read/28651155/covalent-inhibitors-design-and-discovery
#2
REVIEW
Stephane De Cesco, Jerry Kurian, Caroline Dufresne, Anthony K Mittermaier, Nicolas Moitessier
In the history of therapeutics, covalent drugs occupy a very distinct category. While representing a significant fraction of the drugs on the market, very few have been deliberately designed to interact covalently with their biological target. In this review, the prevalence of covalent drugs will first be briefly covered, followed by an introduction to their mechanisms of action and more detailed discussions of their discovery and the development of safe and efficient covalent enzyme inhibitors. All stages of a drug discovery program will be covered, from target considerations to lead optimization, strategies to tune reactivity and computational methods...
June 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28651153/the-role-of-marijuana-use-disorder-in-predicting-emergency-department-and-inpatient-encounters-a-retrospective-cohort-study
#3
Cynthia I Campbell, Amber L Bahorik, Andrea H Kline-Simon, Derek D Satre
BACKGROUND: Marijuana use disorder (MUD) is the most common illegal drug use disorder and its prevalence is increasing. It is associated with psychiatric and medical problems, but little is known about its impact on emergency department (ED) and inpatient utilization rates. DESIGN: In a retrospective cohort design, we used electronic health record (EHR) data to identify patients with MUD (n=2752) and demographically matched patients without MUD (n=2752) in 2010...
June 10, 2017: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/28650901/application-of-quality-by-design-approach-to-bioanalysis-development-of-a-method-for-elvitegravir-quantification-in-human-plasma
#4
Sara Baldelli, Giorgio Marrubini, Dario Cattaneo, Emilio Clementi, Matteo Cerea
BACKGROUND: The application of Quality by Design (QbD) principles in clinical laboratories can help to develop an analytical method through a systematic approach, providing a significant advance over the traditional heuristic and empirical methodology. In the present work, we applied for the first time the QbD concept in the development of a method for drug quantification in human plasma using elvitegravir as the test molecule. METHODS: The goal of the study was to develop a fast and inexpensive quantification method, with precision and accuracy as requested by the EMA guidelines on bioanalytical method validation...
June 22, 2017: Therapeutic Drug Monitoring
https://www.readbyqxmd.com/read/28650820/terahertz-channel-model-and-link-budget-analysis-for-intrabody-nanoscale-communication
#5
Hadeel Elayan, Raed M Shubair, Josep M Jornet, Pedram Johari
Nanosized devices operating inside the human body open up new prospects in the healthcare domain. In vivo wireless nanosensor networks (iWNSNs) will result in a plethora of applications ranging from intrabody health-monitoring to drug- delivery systems. With the development of miniature plasmonic signal sources, antennas and detectors, wireless communications among intrabody nanodevices will expectedly be enabled at both the Terahertz Band (0.1-10 THz) as well as optical frequencies (400-750 THz). This result motivates the analysis of the phenomena affecting the propagation of electromagnetic signals inside the human body...
June 22, 2017: IEEE Transactions on Nanobioscience
https://www.readbyqxmd.com/read/28650661/triaryl-benzimidazoles-as-a-new-class-of-antibacterial-agents-against-resistant-pathogenic-microorganisms
#6
Pietro Picconi, Charlotte Hind, Shirin Jamshidi, Kazi Nahar, Melanie Clifford, Matthew E Wand, J Mark Sutton, K Miraz Rahman
A new class of non-toxic triaryl benzimidazole compounds, derived from existing classes of DNA minor groove binders, were designed, synthesized and evaluated for their antibacterial activity against multi-drug resistant (MDR) Gram-positive and Gram-negative species. Molecular modelling experiments suggest that the newly synthesized class cannot be accommodated within the minor groove of DNA, due to a change in the shape of the molecules. Compounds 8, 13 and 14 were found to be the most active of the series, with MICs in the range of 0...
June 26, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28650492/exploiting-the-biosynthetic-machinery-of-streptomyces-pilosus-to-engineer-a-water-soluble-zirconium-iv-chelator
#7
Tomas Richardson-Sanchez, William Tieu, Michael P Gotsbacher, Thomas J Telfer, Rachel Codd
The water solubility of a natural product-inspired octadentate hydroxamic acid chelator designed to coordinate Zr(iv)-89 has been improved by using a combined microbiological-chemical approach to engineer four ether oxygen atoms into the main-chain region of a methylene-containing analogue. First, an analogue of the trimeric hydroxamic acid desferrioxamine B (DFOB) that contained three main-chain ether oxygen atoms (DFOB-O3) was generated from cultures of the native DFOB-producer Streptomyces pilosus supplemented with oxybis(ethanamine) (OBEA), which competed against the native 1,5-diaminopentane (DP) substrate during DFOB assembly...
June 26, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28650490/hypoxia-induced-tumor-cell-resistance-is-overcome-by-synergistic-gapdh-sirna-and-chemotherapy-co-delivered-by-long-circulating-and-cationic-interior-liposomes
#8
Jibin Guan, Jin Sun, Feilong Sun, Bo Lou, Dong Zhang, Vida Mashayekhi, Negar Sadeghi, Gert Storm, Enrico Mastrobattista, Zhonggui He
Chemotherapeutic drug resistance of tumor cells under hypoxic conditions is caused by the inhibition of apoptosis by autophagy and drug efflux via adenosine triphosphate (ATP)-dependent transporter activation, among other factors. Here, we demonstrate that disrupting glyceraldehyde-3-phosphate dehydrogenase (GAPDH) expression can reduce the autophagy and ATP levels in tumor cells. To test whether GAPDH knockdown is sufficient to overcome drug resistance, a nanocarrier (asymmetry-membrane liposome) was designed to encapsulate GAPDH-siRNA with a low dose of paclitaxel (PTX)...
June 26, 2017: Nanoscale
https://www.readbyqxmd.com/read/28650328/studies-on-self-nanoemulsifying-drug-delivery-system-of-flurbiprofen-employing-long-medium-and-short-chain-triglycerides
#9
Junaid Daar, Ahmad Khan, Jallat Khan, Amjad Khan, Gul Majid Khan
The aim of the study was to successfully design, formulate and evaluate self-nanoemulsifying drug delivery system (SNEDDS) of poorly aqueous soluble drug viz. flurbiprofen using long (LCT), medium (MCT) and short chain triglycerides (SCT). The SNEDDS are thermodynamically stable lipid based drug delivery systems which consist of mixture of oil, surfactant and co-surfactant. Upon aqueous dilution, this mixture produces nano-emulsion spontaneously on slight agitation. The excipients intended to be used were screened for their potential to dissolve the drug and to form clear dispersion upon aqueous dilution...
March 2017: Pakistan Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28650253/diagnosis-and-treatment-of-osteoporosis-before-and-after-fracture-a-side-by-side-analysis-of-commercially-insured-and-medicare-advantage-osteoporosis-patients
#10
Jessica Weaver, Shiva Sajjan, E Michael Lewiecki, Steven T Harris
BACKGROUND: Although treatment for osteoporosis is recommended by U.S. clinical guidelines, a lack of diagnosis and treatment is common among patients with osteoporotic fractures. OBJECTIVE: To determine the rates of osteoporosis diagnosis and treatment before and after various types of fractures. METHODS: This was a retrospective claims analysis using data from the Humana Medicare Advantage claims (Medicare group) and Optum Insight Clinformatics Data Mart commercial claims (Commercial group)...
July 2017: Journal of Managed Care & Specialty Pharmacy
https://www.readbyqxmd.com/read/28650247/burden-of-alcohol-abuse-or-dependence-among-long-term-opioid-users-with-chronic-noncancer-pain
#11
Pamela B Landsman-Blumberg, Nathaniel Katz, Kavita Gajria, Anna D Coutinho, Paul P Yeung, Richard White
BACKGROUND: Substance abuse disorders among chronic noncancer pain (CNCP) patients add to the clinical challenges and economic burden of caring for such patients. Despite potential risks, some CNCP patients with a history of alcohol abuse or dependence (AAD) and pain that is refractory to nonopioid treatment options may still need opioids for pain management. However, there is a lack of data on adverse outcomes in long-term opioid users with CNCP and a history of substance abuse or AAD disorders...
July 2017: Journal of Managed Care & Specialty Pharmacy
https://www.readbyqxmd.com/read/28650184/effects-of-nicotine-versus-placebo-e-cigarette-use-on-symptom-relief-during-initial-tobacco-abstinence
#12
Kenneth A Perkins, Joshua L Karelitz, Valerie C Michael
Because electronic cigarettes (e-cigs) containing nicotine may relieve smoking abstinence symptoms similar to nicotine replacement therapy medication, we used within-subjects designs to test these effects with a first-generation e-cig in nonquitting and quitting smokers. In Study 1, 28 nontreatment-seeking smokers abstained overnight prior to each of 3 sessions. Minnesota Nicotine Withdrawal Scale (MNWS) withdrawal (and craving item) relief was assessed following 4 exposures (each 10 puffs) over 2 hr to e-cigs that either did (36 mg/ml) or did not (i...
June 26, 2017: Experimental and Clinical Psychopharmacology
https://www.readbyqxmd.com/read/28650175/bioactive-peptide-natural-products-as-lead-structures-for-medicinal-use
#13
Tam Dang, Roderich D Süssmuth
The need for new drugs for the treatment of various diseases is enormous. From the previous century until the present, numerous peptide and peptide-derived natural products have been isolated from bacteria and fungi. Hence, microorganisms play a pivotal role as sources for novel drugs with an emphasis on anti-infective agents. Various disciplines from biology, chemistry, and medicine are involved in early stages of the search for peptide natural products including taxonomy, microbiology, bioanalytics, bioinformatics, and medicinal chemistry...
June 26, 2017: Accounts of Chemical Research
https://www.readbyqxmd.com/read/28650160/discovery-of-novel-nucleotide-prodrugs-with-improved-potency-against-hcv-variants-carrying-ns5b-s282t-mutation
#14
Le Zhen, Liang Dai, Xiaoan Wen, Lan Yao, Xiaoliang Jin, Xiaowen Yang, Wenfeng Zhao, Sheng-Qi Yu, Haoliang Yuan, Guangji Wang, Hongbin Sun
Resistant HCV variants carrying NS5B S282T mutation confer reduced sensitivity to sofosbuvir, the sole marketed NS5B polymerase inhibitor. Based on the finding that 2'-α-F-2'-β-C-methylcytidine 5'-triphosphate (8) was more potent than sofosbuvir's active metabolite on inhibition of both wild-type and S282T mutant polymerase, a dual-prodrug approach has been established. Twenty-nine phosphoramidates with N4-modified cytosine were designed, synthesized, and evaluated for anti-HCV activity. The results showed that compounds 4c-4e, 4m (EC50 0...
June 26, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28650116/polymeric-drug-delivery-systems-for-intraoral-site-specific-chemoprevention-of-oral-cancer
#15
REVIEW
Kashappa Goud H Desai
Oral cancer is among the most prevalent cancers in the world. Moreover, it is one of the major health problems and causes of death in many regions of the world. The traditional treatment modalities include surgical removal, radiation therapy, systemic chemotherapy, or a combination of these methods. In recent decades, there has been significant interest in intraoral site-specific chemoprevention via local drug delivery using polymeric systems. Because of its easy accessibility and clear visibility, the oral mucosa is amenable for local drug delivery...
June 26, 2017: Journal of Biomedical Materials Research. Part B, Applied Biomaterials
https://www.readbyqxmd.com/read/28650048/cooperative-wrapping-of-nanoparticles-of-various-sizes-and-shapes-by-lipid-membranes
#16
Kai Xiong, Jiayin Zhao, Daowen Yang, Qingwen Cheng, Jiuling Wang, Hongbing Ji
Understanding the interaction between nanoparticles (NPs) and cell membranes is crucial for the design of NP-based drug delivery systems and for the assessment of the risks exerted by the NPs. Recent experimental and theoretical studies have shown that cell membranes can mediate attraction between NPs and form tubular structures to wrap multiple NPs. However, the cooperative wrapping process is still not well understood, and the shape effect of NPs is not considered. In this article, we use large-scale coarse-grained molecular dynamics (CGMD) simulations to study the cooperative wrapping of NPs when a varying number of NPs adhered to the membrane...
June 26, 2017: Soft Matter
https://www.readbyqxmd.com/read/28650043/heme-containing-enzymes-and-inhibitors-for-tryptophan-metabolism
#17
REVIEW
Daojing Yan, Ying-Wu Lin, Xiangshi Tan
Iron-containing enzymes such as heme enzymes play crucial roles in biological systems. Three distinct heme-containing dioxygenase enzymes, tryptophan 2,3-dioxygenase (TDO), indoleamine 2,3-dioxygenase 1 (IDO1) and indoleamine 2,3-dioxygenase 2 (IDO2) catalyze the initial and rate-limiting step of l-tryptophan catabolism through the kynurenine pathway in mammals. Overexpression of these enzymes causes depletion of tryptophan and the accumulation of metabolic products, which contributes to tumor immune tolerance and immune dysregulation in a variety of disease pathologies...
June 26, 2017: Metallomics: Integrated Biometal Science
https://www.readbyqxmd.com/read/28650030/carbon-nanoscroll-silk-crystallite-hybrid-structures-with-controllable-hydration-and-mechanical-properties
#18
Yuan Cheng, Leng-Duei Koh, Fan Wang, Dechang Li, Baohua Ji, Jingjie Yeo, Guijian Guan, Ming-Yong Han, Yong-Wei Zhang
Hybrid structures of nanomaterials (e.g. tubes, scrolls, threads, cages) and biomaterials (e.g. proteins) hold tremendous potential for applications as drug carriers, biosensors, tissue scaffolds, cancer therapeutic agents, etc. However, in many cases, the interacting forces at the nano-bio interfaces and their roles in controlling the structures and dynamics of nano-bio-hybrid systems are very complicated but poorly understood. In this study, we investigate the structure and mechanical behavior of a protein-based hybrid structure, i...
June 26, 2017: Nanoscale
https://www.readbyqxmd.com/read/28650023/ligand-induced-conformational-preorganization-of-loops-of-c-myc-g-quadruplex-dna-and-its-implications-in-structure-specific-drug-design
#19
S Harikrishna, Saikiran Kotaru, P I Pradeepkumar
Stabilization of a G-quadruplex (G4) DNA structure in the proto-oncogene c-MYC using small molecule ligands has emerged as an attractive strategy for the development of anticancer therapeutics. To understand the subtle structural changes in the G4 structure upon ligand binding, molecular dynamics (MD) simulations of c-MYC G4 DNA were carried out in a complex with six different potent ligands: 3AQN, 6AQN, 3APN, 360A, Nap-Et, and Nap-Pr. The results show that the ligands 3AQN, 6AQN, 3APN, and 360A stabilize the G4 structure by making stacking interactions with the top quartet...
June 26, 2017: Molecular BioSystems
https://www.readbyqxmd.com/read/28650000/andexanet-alfa-a-recombinant-mimetic-of-human-factor-xa-for-the-reversal-of-anticoagulant-therapies
#20
G Escolar, M Diaz-Ricart, E Arellano-Rodrigo
Activated coagulation factor X (FXa) is a common target for classic and newer anticoagulants. Parenteral anticoagulants with an indirect inhibitory action on FXa (low-molecular-weight heparins) have a well-established clinical efficacy in the prophylaxis and therapy of thromboembolic conditions. More recently developed direct oral anticoagulants (DOACs) have emerged as a new class of antithrombotic drugs. Rivaroxaban, apixaban and edoxaban are direct inhibitors of FXa approved for the management of venous thromboembolism and stroke prevention in atrial fibrillation...
May 2017: Drugs of Today
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