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https://www.readbyqxmd.com/read/29774351/diversity-of-biologically-active-secondary-metabolites-from-endophytic-and-saprotrophic-fungi-of-the-ascomycete-order-xylariales
#1
REVIEW
Soleiman E Helaly, Benjarong Thongbai, Marc Stadler
Covering: up to December 2017The diversity of secondary metabolites in the fungal order Xylariales is reviewed with special emphasis on correlations between chemical diversity and biodiversity as inferred from recent taxonomic and phylogenetic studies. The Xylariales are arguably among the predominant fungal endophytes, which are the producer organisms of pharmaceutical lead compounds including the antimycotic sordarins and the antiparasitic nodulisporic acids, as well as the marketed drug, emodepside. Many Xylariales are "macromycetes", which form conspicuous fruiting bodies (stromata), and the metabolite profiles that are predominant in the stromata are often complementary to those encountered in corresponding mycelial cultures of a given species...
May 18, 2018: Natural Product Reports
https://www.readbyqxmd.com/read/29774137/saudi-anti-human-cancer-plants-database-sacpd-a-collection-of-plants-with-anti-human-cancer-activities
#2
Ateeq Ahmed Al-Zahrani
Several anticancer drugs have been developed from natural products such as plants. Successful experiments in inhibiting the growth of human cancer cell lines using Saudi plants were published over the last three decades. Up to date, there is no Saudi anticancer plants database as a comprehensive source for the interesting data generated from these experiments. Therefore, there was a need for creating a database to collect, organize, search and retrieve such data. As a result, the current paper describes the generation of the Saudi anti-human cancer plants database (SACPD)...
January 30, 2018: Oncology Reviews
https://www.readbyqxmd.com/read/29773916/the-haemophilia-drug-market
#3
Kerri Brown, Graeme Green
No abstract text is available yet for this article.
May 18, 2018: Nature Reviews. Drug Discovery
https://www.readbyqxmd.com/read/29773358/-antidepressive-agents-and-hyponatremia-a-literature-review-and-a-case-non-case-study-in-the-french-pharmacovigilance-database
#4
Michaël Rochoy, Christina Zakhem-Stachera, Johana Béné, Christophe Berkhout, Sophie Gautier
OBJECTIVE: Most antidepressants have been associated with a risk of hyponatremia in the literature. This effect is not always reported in monographs. The aim of our study was to clarify the difference of increased risk of hyponatremia among various antidepressants. METHODS: Retrospective study of such cases/non-cases from observations recorded in the French national pharmacovigilance between 01/01/2004 and 31/12/2013. We studied all antidepressants marketed in 2014 in France, with a positive control (haloperidol) and a negative one (amoxicillin)...
March 1, 2018: Thérapie
https://www.readbyqxmd.com/read/29773056/nanocrystals-technology-for-pharmaceutical-science
#5
Zhongyao Cheng, Yumei Lian, Zul Kamal, Xin Ma, Jianjun Chen, Xinbo Zhou, Jing Su, Mingfeng Qiu
BACKGROUND: Nanocrystals technology is a promising method for improving the dissolution rate and enhancing the bioavailability of poorly soluble drugs. In recent years, it has been developing rapidly and applied to drug research and engineering. Nanocrystal drugs can be formulated into various dosage forms. OBJECTIVE: This review mainly focused on the nanocrystals technology and its application in pharmaceutical science. Firstly, different preparation methods of nanocrystal technology and the characterization of nanocrystal drugs are briefly described...
May 17, 2018: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/29772901/the-catch-22-of-predicting-herg-blockade-using-publicly-accessible-bioactivity-data
#6
Vishal Babu Siramshetty, Qiaofeng Chen, Prashanth Devarakonda, Robert Preissner
Drug-induced inhibition of the human Ether-à-go-go-Related Gene (hERG) encoded potassium ion (K+) channels can lead to fatal cardiotoxicity. Several marketed drugs and promising drug candidates were recalled due to this concern. Diverse modeling methods ranging from molecular similarity assessment to quantitative structure activity relationship analysis employing machine learning techniques have been applied to datasets of varying size and composition (number of blockers and non-blockers). In this study, we highlight the challenges involved in development of a robust classifier for predicting the hERG endpoint using bioactivity data extracted from the public domain...
May 17, 2018: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/29772697/structure-activity-relationships-based-on-3d-qsar-comfa-comsia-and-design-of-aryloxypropanol-amine-agonists-with-selectivity-for-the-human-%C3%AE-3-adrenergic-receptor-and-anti-obesity-and-anti-diabetic-profiles
#7
Marcos Lorca, Cesar Morales-Verdejo, David Vásquez-Velásquez, Juan Andrades-Lagos, Javier Campanini-Salinas, Jorge Soto-Delgado, Gonzalo Recabarren-Gajardo, Jaime Mella
The wide tissue distribution of the adrenergic β3 receptor makes it a potential target for the treatment of multiple pathologies such as diabetes, obesity, depression, overactive bladder (OAB), and cancer. Currently, there is only one drug on the market, mirabegron, approved for the treatment of OAB. In the present study, we have carried out an extensive structure-activity relationship analysis of a series of 41 aryloxypropanolamine compounds based on three-dimensional quantitative structure-activity relationship (3D-QSAR) techniques...
May 16, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29772300/effect-of-nagilactone-e-on-cell-morphology-and-glucan-biosynthesis-in-budding-yeast-saccharomyces-cerevisiae
#8
Kengo Hayashi, Yoshihiro Yamaguchi, Akira Ogita, Toshio Tanaka, Isao Kubo, Ken-Ichi Fujita
Nagilactones are norditerpene dilactones isolated from the root bark of Podocarpus nagi. Although nagilactone E has been reported to show antifungal activities, its activity is weaker than that of antifungals on the market. Nagilactone E enhances the antifungal activity of phenylpropanoids such as anethole and isosafrole against nonpathogenic Saccharomyces cerevisiae and pathogenic Candida albicans. However, the detailed mechanisms underlying the antifungal activity of nagilactone E itself have not yet been elucidated...
May 14, 2018: Fitoterapia
https://www.readbyqxmd.com/read/29772289/nose-to-brain-drug-delivery-an-update-on-clinical-challenges-and-progress-towards-approval-of-anti-alzheimer-drugs
#9
REVIEW
Mukta Agrawal, Swarnlata Saraf, Shailendra Saraf, Sophia G Antimisiaris, Mahavir Chougule, Sunday A Shoyele, Amit Alexander
According to the Alzheimer Association Report (2017), Alzheimer's disease (AD) is the 6th primary cause of death in the USA, which affects nearly 5.5 million people. In the year 2017 itself, the cost of AD treatment in the USA has been reported to rise to $259 billion. This statistic shows the severity of the disease in the USA which is very much similar across the globe. On the other hand, the treatment remains limited to a few conventional oral medications (approved by FDA). These are mainly acting superficially from mild to the moderate AD...
May 14, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/29771942/antisense-pmo-cocktails-effectively-skip-dystrophin-exons-45-55-in-myotubes-transdifferentiated-from-dmd-patient-fibroblasts
#10
Joshua Lee, Yusuke Echigoya, William Duddy, Takashi Saito, Yoshitsugu Aoki, Shin'ichi Takeda, Toshifumi Yokota
Antisense-mediated exon skipping has made significant progress as a therapeutic platform in recent years, especially in the case of Duchenne muscular dystrophy (DMD). Despite FDA approval of eteplirsen-the first-ever antisense drug clinically marketed for DMD-exon skipping therapy still faces the significant hurdles of limited applicability and unknown truncated protein function. In-frame exon skipping of dystrophin exons 45-55 represents a significant approach to treating DMD, as a large proportion of patients harbor mutations within this "hotspot" region...
2018: PloS One
https://www.readbyqxmd.com/read/29771317/exon-skipping-advances-for-duchenne-muscular-dystrophy
#11
Lucía Echevarría, Philippine Aupy, Aurélie Goyenvalle
Duchenne muscular dystrophy (DMD) is a fatal genetic disorder characterized by progressive muscle wasting that has currently no cure. Exon-skipping strategy represents one of the most promising therapeutic approaches that aims to restore expression of a shorter but functional dystrophin protein. The antisense field has remarkably progress over the last years with recent accelerated approval of the first ASO-based therapy for DMD, Exondys 51, though the therapeutic benefit remains to be proven in patients. Despite clinical advances, the poor effective delivery to target all muscle remains the main hurdle for antisense drug therapy...
May 16, 2018: Human Molecular Genetics
https://www.readbyqxmd.com/read/29770277/a-strategy-to-find-novel-candidate-anti-alzheimer-s-disease-drugs-by-constructing-interaction-networks-between-drug-targets-and-natural-compounds-in-medical-plants
#12
Bi-Wen Chen, Wen-Xing Li, Guang-Hui Wang, Gong-Hua Li, Jia-Qian Liu, Jun-Juan Zheng, Qian Wang, Hui-Juan Li, Shao-Xing Dai, Jing-Fei Huang
Background: Alzheimer' disease (AD) is an ultimately fatal degenerative brain disorder that has an increasingly large burden on health and social care systems. There are only five drugs for AD on the market, and no new effective medicines have been discovered for many years. Chinese medicinal plants have been used to treat diseases for thousands of years, and screening herbal remedies is a way to develop new drugs. Methods: We used molecular docking to screen 30,438 compounds from Traditional Chinese Medicine (TCM) against a comprehensive list of AD target proteins...
2018: PeerJ
https://www.readbyqxmd.com/read/29768712/innovation-at-the-intersection-of-clinical-trials-and-real-world-data-science-to-advance-patient-care
#13
REVIEW
Brandon Swift, Lokesh Jain, Craig White, Vasu Chandrasekaran, Aman Bhandari, Dyfrig A Hughes, Pravin R Jadhav
While efficacy and safety data collected from randomized clinical trials are the evidentiary standard for determining market authorization, this alone may no longer be sufficient to address the needs of key stakeholders (regulators, providers, and payers) and guarantee long-term success of pharmaceutical products. There is a heightened interest from stakeholders on understanding the use of real-world evidence (RWE) to substantiate benefit-risk assessment and support the value of a new drug. This review provides an overview of real-world data (RWD) and related advances in the regulatory framework, and discusses their impact on clinical research and development...
May 16, 2018: Clinical and Translational Science
https://www.readbyqxmd.com/read/29768576/recent-advances-and-perspectives-in-cancer-drug-design
#14
Luma G Magalhaes, Leonardo L G Ferreira, Adriano D Andricopulo
Cancer is one of the leading causes of death worldwide. With the increase in life expectancy, the number of cancer cases has reached unprecedented levels. In this scenario, the pharmaceutical industry has made significant investments in this therapeutic area. Despite these efforts, cancer drug research remains a remarkably challenging field, and therapeutic innovations have not yet achieved expected clinical results. However, the physiopathology of the disease is now better understood, and the discovery of novel molecular targets has refreshed the expectations of developing improved treatments...
May 14, 2018: Anais da Academia Brasileira de Ciências
https://www.readbyqxmd.com/read/29768546/first-wave-protease-inhibitors-for-hepatitis-c-genotype-1-treatment-a-real-life-experience-in-brazilian-patients
#15
Silvana Gama Florencio Chachá, João Paulo Vilela Rodrigues, Roberta Chaves Araújo, Leonardo Régis Leira Pereira, Márcia Guimarães Villanova, Fernanda Fernandes Souza, Rodrigo de Carvalho Santana, Ana de Lourdes Candolo Martinelli
INTRODUCTION: Licensed for chronic hepatitis C treatment in 2011, the protease inhibitors (PIs) telaprevir (TVR) and boceprevir (BOC), which have high sustained viral responses (SVR), ushered a new era characterized by the development of direct-action drugs against the hepatitis C virus (HCV). The aim of this study was to analyze the effectiveness and safety of BOC and TVR administered with pegylated interferon and ribavirin and to share the experience of a Brazilian reference center...
March 2018: Revista da Sociedade Brasileira de Medicina Tropical
https://www.readbyqxmd.com/read/29768140/addressing-generic-drug-market-failures-the-case-for-establishing-a-nonprofit-manufacturer
#16
Dan Liljenquist, Ge Bai, Gerard F Anderson
Robust competition usually keeps the price of generic drugs well below that of brand-name drugs. When there is little or no competition, however, generic-drug manufacturers can substantially increase prices, and drug shortages may occur. Such market failures can compromise care and negatively..
May 17, 2018: New England Journal of Medicine
https://www.readbyqxmd.com/read/29768112/-marvin-the-paranoid-android-the-case-of-an-alpha-pvp-user-in-the-expanding-galaxy-of-nps
#17
Simonato Pierluigi, Bulsis Laura, Negri Attilio, Bansal Gurjeet K, Pessa Gloria, Mioni Davide, Giuseppe Borgherini, Martinotti Giovanni, Schifano Fabrizio, Giulia Perini, Corazza Ornella
Alpha-PVP can be defined as a novel psychoactive substance (NPS)-more specifically, a novel synthetic cathinone with unpredictable stimulant effects in humans. "Marvin" arrived at a Dual Diagnosis Unit at Parco dei Tigli, Italy. He underwent a 30-day rehabilitation program to overcome his problematic Alpha-PVP use as a psychonaut. We conducted an online search to understand the properties of Alpha-PVP and its presence in scientific literature, reviewing official reports and the online drug market (e...
May 16, 2018: Journal of Psychoactive Drugs
https://www.readbyqxmd.com/read/29767543/efficacy-of-single-tablet-darunavir-cobicistat-emtricitabine-and-tenofovir-alafenamide-in-the-treatment-of-hiv-1
#18
Eugènia Negredo, Bonaventura Clotet
HIV eradication is not feasible and lifelong treatment is warranted to manage HIV infection. In this scenario, the advent of single-tablet, once-daily, fixed-dose co-formulations is important for reducing pill burden and maximize long-term drug adherence. Cobicistat-boosted darunavir along with emtricitabine and tenofovir alafenamide co-formulation (DRV/c/FTC/TAF or the trade name Symtuza®) is the first marketed protease inhibitor-based fixed-dose combination regimen for the treatment of HIV infection. It was approved in late 2017 by the European Medical Agency both for naïve patients and treatment-experienced patients with viral suppression...
May 16, 2018: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/29766592/scoring-the-best-deal-quantity-discounts-and-street-price-variation-of-diverted-oxycodone-and-oxymorphone
#19
Jacob A Lebin, David L Murphy, Stevan Geoffrey Severtson, Gabrielle E Bau, Nabarun Dasgupta, Richard C Dart
BACKGROUND: Diverted prescription opioids are significant contributors to drug overdose mortality. Street price has been suggested as an economic metric of the diverted prescription opioid black market. This study examined variables that may influence the street price of diverted oxycodone and oxymorphone. METHODS: A cross-sectional study was conducted utilizing data from the previously validated, crowdsourcing website StreetRx. Street price reports of selected oxycodone and oxymorphone products, between August 22, 2014 and June 30, 2016, were considered for analysis...
May 15, 2018: Pharmacoepidemiology and Drug Safety
https://www.readbyqxmd.com/read/29766296/characterization-of-in-vivo-metabolites-in-rat-urine-following-an-oral-dose-of-masitinib-by-liquid-chromatography-tandem-mass-spectrometry
#20
Adnan A Kadi, Sawsan M Amer, Hany W Darwish, Mohamed W Attwa
Masitinib (MST) is an orally administered drug that targets mast cells and macrophages, important cells for immunity, by inhibiting a limited number of tyrosine kinases. It is currently registered in Europe and USA for the treatment of mast cell tumors in dogs. AB Science announced that the European Medicines Agency has accepted a conditional marketing authorization application for MST to treat amyotrophic lateral sclerosis. In our work, we focused on studying in vivo metabolism of MST in Sprague-Dawley rats...
May 15, 2018: Chemistry Central Journal
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