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https://www.readbyqxmd.com/read/28230985/discovery-of-competitive-and-non-competitive-ligands-of-the-organic-cation-transporter-1-oct1-slc22a1
#1
Eugene C Chen, Natalia Khuri, Xiaomin Liang, Adrian Stecula, Huan-Chieh Chien, Sook Wah Yee, Yong Huang, Andrej Sali, Kathleen M Giacomini
Organic cation transporter 1 (OCT1) plays a critical role in the hepatocellular uptake of structurally diverse endogenous compounds and xenobiotics. Here, we identified competitive and noncompetitive OCT1 interacting ligands in a library of 1,780 prescription drugs by combining in silico and in vitro methods. Ligands were predicted by docking against a comparative model based a eukaryotic homolog. In parallel, high-throughput screening (HTS) was conducted using the fluorescent probe substrate ASP+ in cells overexpressing human OCT1...
February 23, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28230870/colloidal-capsules-nano-and-microcapsules-with-colloidal-particle-shells
#2
REVIEW
Tobias Bollhorst, Kurosch Rezwan, Michael Maas
Utilizing colloidal particles for the assembly of the shell of nano- and microcapsules holds great promise for the tailor-made design of new functional materials. Increasing research efforts are devoted to the synthesis of such colloidal capsules, by which the integration of modular building blocks with distinct physical, chemical, or morphological characteristics in a capsule's shell can result in novel properties, not present in previous encapsulation structures. This review will provide a comprehensive overview of the synthesis strategies and the progress made so far of bringing nano- and microcapsules with shells of densely packed colloidal particles closer to application in fields such as chemical engineering, materials science, or pharmaceutical and life science...
February 23, 2017: Chemical Society Reviews
https://www.readbyqxmd.com/read/28230095/genetic-diversity-transmission-dynamics-and-drug-resistance-of-mycobacterium-tuberculosis-in-angola
#3
João Perdigão, Sofia Clemente, Jorge Ramos, Pedro Masakidi, Diana Machado, Carla Silva, Isabel Couto, Miguel Viveiros, Nuno Taveira, Isabel Portugal
Tuberculosis (TB) poses a serious public health problem in Angola. No surveillance data on drug resistance is available and nothing is known regarding the genetic diversity and population structure of circulating Mycobacterium tuberculosis strains. Here, we have genotyped and evaluated drug susceptibility of 89 Mycobacterium tuberculosis clinical isolates from Luanda. Thirty-three different spoligotype profiles corresponding to 24 different Shared International Types (SIT) and 9 orphan profiles were detected...
February 23, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28228160/assessment-of-lymphatic-filariasis-prior-to-re-starting-mass-drug-administration-campaigns-in-coastal-kenya
#4
Sammy M Njenga, Henry M Kanyi, Faith M Mutungi, Collins Okoyo, Hadley S Matendechero, Rachel L Pullan, Katherine E Halliday, Simon J Brooker, C Njeri Wamae, Joyce K Onsongo, Kimberly Y Won
BACKGROUND: Lymphatic filariasis (LF) is a debilitating disease associated with extensive disfigurement and is one of a diverse group of diseases referred to as neglected tropical diseases (NTDs) which mainly occur among the poorest populations. In line with global recommendations to eliminate LF, Kenya launched its LF elimination programme in 2002 with the aim to implement annual mass drug administration (MDA) in order to interrupt LF transmission. However, the programme faced financial and administrative challenges over the years such that sustained annual MDA was not possible...
February 22, 2017: Parasites & Vectors
https://www.readbyqxmd.com/read/28228080/marine-drugs-a-hidden-wealth-and-a-new-epoch-for-cancer-management
#5
Eram Shakeel, Deepika Arora, Qazi Mohammad Sajid Jamal, Salman Akhtar, Mohd Kalim Ahmad Khan, Mohammad A Kamal, Mohd Haris Siddiqui, Mohtashim Lohani, Jamal M Arif
Malignant tumors are the leading cause of death in humans. Due to tedious efforts and investigation made in the field of marine drug discovery, there is now a scientific bridge between marine and pharmaceutical sciences. However, at present only few marine drugs have been paved towards anticancer management, yet many more to be established. Marine organisms are profuse manufacturer of structurally inimitable bioactive metabolites that have unusual mechanisms of action and diverse biosynthetic pathways. Some of the compounds derived from marine organisms have antioxidant property and anticancer activities, but they are largely unexplored...
February 20, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/28227226/learning-approaches-to-improve-prediction-of-drug-sensitivity-in-breast-cancer-patients
#6
Turki Turki, Zhi Wei, Turki Turki, Zhi Wei, Turki Turki, Zhi Wei
Predicting drug response to cancer disease is an important problem in modern clinical oncology that attracted increasing recent attention from various domains such as computational biology, machine learning, and data mining. Cancer patients respond differently to each cancer therapy owing to disease diversity, genetic factors, and environmental causes. Thus, oncologists aim to identify the effective therapies for cancer patients and avoid adverse drug reactions in patients. By predicting the drug response to cancer, oncologists gain full understanding of the effective treatments on each patient, which leads to better personalized treatment...
August 2016: Conference Proceedings: Annual International Conference of the IEEE Engineering in Medicine and Biology Society
https://www.readbyqxmd.com/read/28226334/prescription-opioid-abuse-in-chronic-pain-an-updated-review-of-opioid-abuse-predictors-and-strategies-to-curb-opioid-abuse-part-2
#7
Alan D Kaye, Mark R Jones, Adam M Kaye, Juan G Ripoll, Donald E Jones, Vincent Galan, Burton D Beakley, Frank Calixto, Jamie L Bolden, Richard D Urman, Laxmaiah Manchikanti
Chronic pain and prescription opioid abuse are extremely prevalent in the United States and worldwide. The consequences of opioid misuse can be life-threatening with significant morbidity and mortality, exacting a heavy toll on patients, physicians, and society. The risk for misuse of prescribed opioids is much higher in patients with chronic pain, especially those with concurrent substance use and /or mental health disorders. Several reasons can account for the occurrence of opioid abuse and misuse, including self-medication, use for reward, compulsive use related to addiction, and diversion for profit...
February 2017: Pain Physician
https://www.readbyqxmd.com/read/28226333/prescription-opioid-abuse-in-chronic-pain-an-updated-review-of-opioid-abuse-predictors-and-strategies-to-curb-opioid-abuse-part-1
#8
Alan D Kaye, Mark R Jones, Adam M Kaye, Juan G Ripoll, Vincent Galan, Burton D Beakley, Frank Calixto, Jamie L Bolden, Richard D Urman, Laxmaiah Manchikanti
Chronic pain and prescription opioid abuse are extremely prevalent both in this country and worldwide. Consequences of opioid misuse can be life-threatening with significant morbidity and mortality, exacting a heavy toll on patients, physicians, and society. Individuals with chronic pain and co-occurring substance use disorders and/or mental health disorders, are at a higher risk for misuse of prescribed opioids. Opioid abuse and misuse occurs for a variety of reasons, including self-medication, use for reward, compulsive use because of addiction, and diversion for profit...
February 2017: Pain Physician
https://www.readbyqxmd.com/read/28226332/responsible-safe-and-effective-prescription-of-opioids-for-chronic-non-cancer-pain-american-society-of-interventional-pain-physicians-asipp-guidelines
#9
Laxmaiah Manchikanti, Adam M Kaye, Nebojsa Nick Knezevic, Heath McAnally, Konstantin Slavin, Andrea M Trescot, Susan Blank, Vidyasagar Pampati, Salahadin Abdi, Jay S Grider, Alan D Kaye, Kavita N Manchikanti, Harold Cordner, Christopher G Gharibo, Michael E Harned, Sheri L Albers, Sairam Atluri, Steve M Aydin, Sanjay Bakshi, Robert L Barkin, Ramsin M Benyamin, Mark V Boswell, Ricardo M Buenaventura, Aaron K Calodney, David L Cedeno, Sukdeb Datta, Timothy R Deer, Bert Fellows, Vincent Galan, Vahid Grami, Hans Hansen, Standiford Helm Ii, Rafael Justiz, Dhanalakshmi Koyyalagunta, Yogesh Malla, Annu Navani, Kent H Nouri, Ramarao Pasupuleti, Nalini Sehgal, Sanford M Silverman, Thomas T Simopoulos, Vijay Singh, Daneshvari R Solanki, Peter S Staats, Ricardo Vallejo, Bradley W Wargo, Arthur Watanabe, Joshua A Hirsch
BACKGROUND: Opioid use, abuse, and adverse consequences, including death, have escalated at an alarming rate since the 1990s. In an attempt to control opioid abuse, numerous regulations and guidelines for responsible opioid prescribing have been developed by various organizations. However, the US opioid epidemic is continuing and drug dose deaths tripled during 1999 to 2015. Recent data show a continuing increase in deaths due to natural and semisynthetic opioids, a decline in methadone deaths, and an explosive increase in the rates of deaths involving other opioids, specifically heroin and illicit synthetic fentanyl...
February 2017: Pain Physician
https://www.readbyqxmd.com/read/28225193/human-neural-progenitor-transplantation-rescues-behavior-and-reduces-%C3%AE-synuclein-in-a-transgenic-model-of-dementia-with-lewy-bodies
#10
Natalie R S Goldberg, Samuel E Marsh, Joseph Ochaba, Brandon C Shelley, Hayk Davtyan, Leslie M Thompson, Joan S Steffan, Clive N Svendsen, Mathew Blurton-Jones
Synucleinopathies are a group of neurodegenerative disorders sharing the common feature of misfolding and accumulation of the presynaptic protein α-synuclein (α-syn) into insoluble aggregates. Within this diverse group, Dementia with Lewy Bodies (DLB) is characterized by the aberrant accumulation of α-syn in cortical, hippocampal, and brainstem neurons, resulting in multiple cellular stressors that particularly impair dopamine and glutamate neurotransmission and related motor and cognitive function. Recent studies show that murine neural stem cell (NSC) transplantation can improve cognitive or motor function in transgenic models of Alzheimer's and Huntington's disease, and DLB...
February 22, 2017: Stem Cells Translational Medicine
https://www.readbyqxmd.com/read/28224884/water-soluble-co-polyelectrolytes-by-selective-modification-of-cellulose-esters
#11
Shu Liu, Kevin J Edgar
Cellulose-based materials are well-suited for biomedical uses, because of their abundance, renewable nature, biodegradability, and relatively low cost. However, the set of commercially available cellulose esters and ethers is limited in number and diversity, and contains no cationically charged cellulose esters. Herein we report a simple, efficient strategy for synthesizing cationic, water-soluble co-polyelectrolytes from commercial, hydrophobic, renewable-based cellulose esters. Cellulose acetate (degree of substitution (DS) 1...
April 15, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28224677/dynamic-nanoparticle-assemblies-for-biomedical-applications
#12
REVIEW
Fangyuan Li, Jingxiong Lu, Xueqian Kong, Taeghwan Hyeon, Daishun Ling
Designed synthesis and assembly of nanoparticles assisted by their surface ligands can create "smart" materials with programmed responses to external stimuli for biomedical applications. These assemblies can be designed to respond either exogenously (for example, to magnetic field, temperature, ultrasound, light, or electric pulses) or endogenously (to pH, enzymatic activity, or redox gradients) and play an increasingly important role in a diverse range of biomedical applications, such as biosensors, drug delivery, molecular imaging, and novel theranostic systems...
February 22, 2017: Advanced Materials
https://www.readbyqxmd.com/read/28224148/hypercrosslinked-porous-polymer-materials-design-synthesis-and-applications
#13
REVIEW
Liangxiao Tan, Bien Tan
Hypercrosslinked polymers (HCPs) are a series of permanent microporous polymer materials initially reported by Davankov, and have received an increasing level of research interest. In recent years, HCPs have experienced rapid growth due to their remarkable advantages such as diverse synthetic methods, easy functionalization, high surface area, low cost reagents and mild operating conditions. Judicious selection of monomers, appropriate length crosslinkers and optimized reaction conditions yielded a well-developed polymer framework with an adjusted porous topology...
February 22, 2017: Chemical Society Reviews
https://www.readbyqxmd.com/read/28223733/impact-of-humic-acids-on-the-colonic-microbiome-in-healthy-volunteers
#14
Alexander Swidsinski, Yvonne Dörffel, Vera Loening-Baucke, Christoph Gille, Anne Reißhauer, Onder Göktas, Monika Krüger, Jürgen Neuhaus, Wieland Schrödl
AIM: To test the effects of humic acids on innate microbial communities of the colon. METHODS: We followed the effects of oral supplementation with humic acids (Activomin(®)) on concentrations and composition of colonic microbiome in 14 healthy volunteers for 45 d. 3 × 800 mg Activomin(®) were taken orally for 10 d followed by 3 × 400 mg for 35 d. Colonic microbiota were investigated using multicolor fluorescence in situ hybridization (FISH) of Carnoy fixated and paraffin embedded stool cylinders...
February 7, 2017: World Journal of Gastroenterology: WJG
https://www.readbyqxmd.com/read/28223459/evolution-and-epidemiology-of-multidrug-resistant-klebsiella-pneumoniae-in-the-united-kingdom-and-ireland
#15
Danesh Moradigaravand, Veronique Martin, Sharon J Peacock, Julian Parkhill
Klebsiella pneumoniae is a human commensal and opportunistic pathogen that has become a leading causative agent of hospital-based infections over the past few decades. The emergence and global expansion of hypervirulent and multidrug-resistant (MDR) clones of K. pneumoniae have been increasingly reported in community-acquired and nosocomial infections. Despite this, the population genomics and epidemiology of MDR K. pneumoniae at the national level are still poorly understood. To obtain insights into these, we analyzed a systematic large-scale collection of invasive MDR K...
February 21, 2017: MBio
https://www.readbyqxmd.com/read/28223047/diversity-in-sequences-post-translational-modifications-and-expected-pharmacological-activities-of-toxins-from-four-conus-species-revealed-by-the-combination-of-cutting-edge-proteomics-transcriptomics-and-bioinformatics
#16
Michel Degueldre, Marion Verdenaud, Garikoitz Legarda, Rebeca Minambres, Sheila Zuniga, Mathieu Leblanc, Nicolas Gilles, Frederic Ducancel, Edwin De Pauw, Loic Quinton
Venomous animals have developed a huge arsenal of reticulated peptides for defense and predation. Based on various scaffolds, they represent a colossal pharmacological diversity, making them top candidates for the development of innovative drugs. Instead of relying on the classical, low-throughput bioassay-guided approach to identify innovative bioactive peptides, this work exploits a recent paradigm to access to venom diversity. This strategy bypasses the classical approach by combining high-throughput transcriptomics, proteomics and bioinformatics cutting-edge technologies to generate reliable peptide sequences...
February 18, 2017: Toxicon: Official Journal of the International Society on Toxinology
https://www.readbyqxmd.com/read/28222793/corporate-social-responsibility-to-improve-access-to-medicines-the-case-of-brazil
#17
Halla Thorsteinsdóttir, Natasha Ovtcharenko, Jillian Clare Kohler
BACKGROUND: Access to medicines and the development of a strong national pharmaceutical industry are two longstanding pillars of health policy in Brazil. This is reflected in a clear emphasis by Brazil's Federal Government on improving access to medicine in national health plans and industrial policies aimed at promoting domestic pharmaceutical development. This research proposes that such policies may act as incentives for companies to pursue a strategic Corporate Social Responsibility (CSR) agenda...
February 21, 2017: Globalization and Health
https://www.readbyqxmd.com/read/28222612/in-vitro-ex-vivo-correlations-between-a-cell-laden-hydrogel-and-mucosal-tissue-for-screening-composite-delivery-systems
#18
Anna K Blakney, Adam B Little, Yonghou Jiang, Kim A Woodrow
Composite delivery systems where drugs are electrospun in different layers and vary the drug stacking-order are posited to affect bioavailability. We evaluated how the formulation characteristics of both burst- and sustained-release electrospun fibers containing three physicochemically diverse drugs: dapivirine (DPV), maraviroc (MVC) and tenofovir (TFV) affect in vitro and ex vivo release. We developed a poly(hydroxyethyl methacrylate) (pHEMA) hydrogel release platform for the rapid, inexpensive in vitro evaluation of burst- and sustained-release topical or dermal drug delivery systems with varying microarchitecture...
November 2016: Drug Delivery
https://www.readbyqxmd.com/read/28220474/buprenorphine-for-managing-opioid-withdrawal
#19
REVIEW
Linda Gowing, Robert Ali, Jason M White, Dalitso Mbewe
BACKGROUND: Managed withdrawal is a necessary step prior to drug-free treatment or as the endpoint of substitution treatment. OBJECTIVES: To assess the effects of buprenorphine versus tapered doses of methadone, alpha2-adrenergic agonists, symptomatic medications or placebo, or different buprenorphine regimens for managing opioid withdrawal, in terms of the intensity of the withdrawal syndrome experienced, duration and completion of treatment, and adverse effects...
February 21, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28220073/enhanced-late-na-and-ca-currents-as-effective-antiarrhythmic-drug-targets
#20
REVIEW
Hrayr S Karagueuzian, Arash Pezhouman, Marina Angelini, Riccardo Olcese
While recent advances clarified the molecular and cellular modes of action of antiarrhythmic drugs (AADs), their link to suppression of dynamical arrhythmia mechanisms remains only partially understood. The current classifications of AADs (Classes I, III, and IV) rely on blocking peak Na, K and L-type calcium currents (ICa,L), with Class II with dominant beta receptor blocking activity and Class V including drugs with diverse classes of actions. The discovery that the calcium and redox sensor, cardiac Ca/calmodulin-dependent protein kinase II (CaMKII) enhances both the late Na (INa-L) and the late ICa,L in patients at high risk of VT/VF provided a new and a rational AAD target...
2017: Frontiers in Pharmacology
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