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https://www.readbyqxmd.com/read/28644502/au3-%C3%AE-3-s-0e-elementary-block-new-insights-into-ligated-gold-clusters-with-%C3%AE-3-sulfido-motifs
#1
Wen Wu Xu, Xiao Cheng Zeng, Yi Gao
An understanding of the structural stability and formation mechanism of ligated gold nanoclusters with triply coordinated μ3-sulfido (μ3-S) motifs is important not only for gold chemistry but also for the design of more effective catalysts or drug carriers for various applications. In this article, a new elementary block Au3(μ3-S) with zero valence electrons [referred to as Au3(μ3-S)(0e)] has been identified, which describes all crystallized ligated gold clusters with μ3-S motifs, in conjunction with the previously reported Au3(2e) and Au4(2e) elementary blocks, in a grand unified model (GUM)...
June 23, 2017: Nanoscale
https://www.readbyqxmd.com/read/28644406/an-updated-review-on-marine-anticancer-compounds-the-use-of-virtual-screening-for-the-discovery-of-small-molecule-cancer-drugs
#2
REVIEW
Verónica Ruiz-Torres, Jose Antonio Encinar, María Herranz-López, Almudena Pérez-Sánchez, Vicente Galiano, Enrique Barrajón-Catalán, Vicente Micol
Marine secondary metabolites are a promising source of unexploited drugs that have a wide structural diversity and have shown a variety of biological activities. These compounds are produced in response to the harsh and competitive conditions that occur in the marine environment. Invertebrates are considered to be among the groups with the richest biodiversity. To date, a significant number of marine natural products (MNPs) have been established as antineoplastic drugs. This review gives an overview of MNPs, both in research or clinical stages, from diverse organisms that were reported as being active or potentially active in cancer treatment in the past seventeen years (from January 2000 until April 2017) and describes their putative mechanisms of action...
June 23, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28644007/cyclotides-as-tools-in-chemical-biology
#3
Simon J de Veer, Joachim Weidmann, David J Craik
Among the various molecules that plants produce for defense against pests and pathogens, cyclotides stand out as exceptionally stable and structurally unique. These ribosomally synthesized peptides are around 30 amino acids in size, and are stabilized by a head-to-tail cyclic peptide backbone and three disulfide bonds that form a cystine knot. They occur in certain plants of the Rubiaceae, Violaceae, Cucurbitaceae, Fabaceae, and Solanaceae families, with an individual plant producing up to hundreds of different cyclotides...
June 23, 2017: Accounts of Chemical Research
https://www.readbyqxmd.com/read/28643796/benchmarking-cataract-surgery-outcomes-in-an-ethnically-diverse-and-diabetic-population-final-post-operative-visual-acuity-and-rates-of-post-operative-cystoid-macular-oedema
#4
K Oyewole, F Tsogkas, M Westcott, S Patra
PurposeTo determine visual acuity and rates of post-operative cystoid macular oedema (CMO) in an ethnically diverse and predominantly diabetic population.MethodsThe study was undertaken over a one year period. Snellen visual acuity (VA) was measured pre and 4-8 weeks post-operatively and optical coherence topography (OCT) was performed at baseline and post-operatively. No eyes received prophylactic non-steroidal anti-inflammatory drugs (NSAIDs) prior to or after surgery.ResultsOut of 262 eyes, 59% were in the Black, Asian and minority ethnic group (BAME), 57% had a history of diabetes mellitus and 34% had pre-existing diabetic retinopathy...
June 23, 2017: Eye
https://www.readbyqxmd.com/read/28643580/cyclophilins-less-studied-proteins-with-critical-roles-in-pathogenesis
#5
Khushwant Singh, Mark Winter, Miloslav Zouhar, Pavel Rysanek
Cyclophilins (EC 5.2.1.8) (CYPs) belong to a subgroup of proteins known as immunophilins, which also include FK-506 binding proteins (FKBPs) and parvulins. Members of the immunophilins have two main characteristic properties: I) peptidyl-prolyl cis-trans isomerase activity (PPIases) and II) the ability to bind immunosuppressant molecules of fungal origin. Cyclophilins are some of the most conserved proteins present in eukaryotes and prokaryotes, and they have been implicated in diverse cellular processes and responses to multiple biotic and abiotic stresses...
June 23, 2017: Phytopathology
https://www.readbyqxmd.com/read/28642701/the-market-of-biopharmaceutical-medicines-a-snapshot-of-a-diverse-industrial-landscape
#6
Evelien Moorkens, Nicolas Meuwissen, Isabelle Huys, Paul Declerck, Arnold G Vulto, Steven Simoens
Background: Biopharmaceutical medicines represent a growing share of the global pharmaceutical market, and with many of these biopharmaceutical products facing loss of exclusivity rights, also biosimilars may now enter the biopharmaceutical market. Objectives: This study aims to identify and document which investment and development strategies are adopted by industrial players in the global biopharmaceutical market. Methods: A descriptive analysis was undertaken of the investment and development strategies of the top 25 pharmaceutical companies according to 2015 worldwide prescription drug sales...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28642642/access-to-and-payment-for-office-based-buprenorphine-treatment-in-ohio
#7
Theodore V Parran, Joseph Z Muller, Elina Chernyak, Chris Adelman, Christina M Delos Reyes, Douglas Rowland, Mykola Kolganov
IMPORTANCE: Office-based opiate agonist therapy has dramatically expanded access to medication-assisted treatment over the past decade but has also led to increased buprenorphine diversion. OBJECTIVE: Our study sought to characterize physicians who participate in office-based therapy (OBT) to assess patient access to OBT in Ohio 10 years after its introduction. DESIGN/SETTING/PARTICIPANTS: Cross-sectional telephone survey of Drug Addiction Treatment Act-waivered physicians in Ohio listed by the Center for Substance Abuse Treatment (CSAT)...
2017: Substance Abuse: Research and Treatment
https://www.readbyqxmd.com/read/28642603/imaging-of-anticancer-drug-action-in-single-cells
#8
REVIEW
Miles A Miller, Ralph Weissleder
Imaging is widely used in anticancer drug development, typically for whole-body tracking of labelled drugs to different organs or to assess drug efficacy through volumetric measurements. However, increasing attention has been drawn to pharmacology at the single-cell level. Diverse cell types, including cancer-associated immune cells, physicochemical features of the tumour microenvironment and heterogeneous cell behaviour all affect drug delivery, response and resistance. This Review summarizes developments in the imaging of in vivo anticancer drug action, with a focus on microscopy approaches at the single-cell level and translational lessons for the clinic...
June 23, 2017: Nature Reviews. Cancer
https://www.readbyqxmd.com/read/28641547/recent-advances-on-the-role-of-micrornas-in-both-insulin-resistance-and-cancer
#9
Adele Vivacqua, Paola De Marco, Antonino Belfiore, Marcello Maggiolini
BACKGROUND: Insulin resistance is a pathological condition characterized by the failure of target cells to uptake and metabolizes glucose in response to insulin. In particular, the elevated concentrations of glucose, insulin and free insulin growth factor-1, which result from insulin resistance, may generate a pro-inflammatory and pro-tumorigenic state. These alterations may underlie the increased risk to develop various types of cancer as well as the worse cancer prognosis observed in obese and diabetic patients...
June 22, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28641130/sexual-orientation-minority-stress-social-norms-and-substance-use-among-racially-diverse-adolescents
#10
Ethan H Mereish, Jeremy T Goldbach, Claire Burgess, Angelo M DiBello
BACKGROUND: Sexual minority adolescents are more likely than their heterosexual peers to use substances. This study tested factors that contribute to sexual orientation disparities in substance use among racially and ethnically diverse adolescents. Specifically, we examined how both minority stress (i.e., homophobic bullying) and social norms (i.e., descriptive and injunctive norms) may account for sexual orientation disparities in recent and lifetime use of four substances: tobacco, alcohol, marijuana, and prescription drugs...
June 8, 2017: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/28641010/alpha-mangostin-reverses-multidrug-resistance-by-attenuating-the-function-of-the-multidrug-resistance-linked-abcg2-transporter
#11
Chung-Pu Wu, Sung-Han Hsiao, Megumi Murakami, Yu-Jen Lu, Yan-Qing Li, Yang-Hui Huang, Tai-Ho Hung, Suresh V Ambudkar, Yu-Shan Wu
The ATP-binding cassette (ABC) drug transporter ABCG2 can actively efflux a wide variety of chemotherapeutic agents out of cancer cells and subsequently reduce the intracellular accumulation of these drugs. Therefore, the overexpression of ABCG2 often contributes to the development of multidrug resistance (MDR) in cancer cells, which is one of the major obstacles to successful cancer chemotherapy. Moreover, ABCG2 is highly expressed in various tissues including the intestine and blood-brain barrier (BBB), limiting the absorption and bioavailability of many therapeutic agents...
June 22, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28640968/the-impact-of-andean-patagonian-mycoflora-in-the-search-for-new-lead-molecules
#12
REVIEW
Pedro M Aqueveque, Carlos L Cespedes, Isao Kubo, David S Seigler, Olov Sterner
Secondary metabolites from fungi have become a major source of chemical innovation in programs searching for lead molecules with bioactivities, especially over the last 50 years. In this review, we discuss the fundamental considerations in the discovery of molecules for agricultural and medicinal uses. This group of organisms possesses a strong potential for scientific and industrial communities. Recently, the incorporation of new technologies for the artificial cultivation of fungi and the use of better equipment to isolate and identify active metabolites has allowed the discovery of leading molecules for the design of new and safer drugs and pesticides...
June 22, 2017: Annals of the New York Academy of Sciences
https://www.readbyqxmd.com/read/28640849/motility-in-blastogregarines-apicomplexa-native-and-drug-induced-organisation-of-siedleckia-nematoides-cytoskeletal-elements
#13
Andrea Valigurová, Naděžda Vaškovicová, Andrei Diakin, Gita G Paskerova, Timur G Simdyanov, Magdaléna Kováčiková
Recent studies on motility of Apicomplexa concur with the so-called glideosome concept applied for apicomplexan zoites, describing a unique mechanism of substrate-dependent gliding motility facilitated by a conserved form of actomyosin motor and subpellicular microtubules. In contrast, the gregarines and blastogregarines exhibit different modes and mechanisms of motility, correlating with diverse modifications of their cortex. This study focuses on the motility and cytoskeleton of the blastogregarine Siedleckia nematoides Caullery et Mesnil, 1898 parasitising the polychaete Scoloplos cf...
2017: PloS One
https://www.readbyqxmd.com/read/28639654/fast-easy-preparation-of-3d-scaffolds-from-methyl-benzoate-by-a-diversity-oriented-synthesis-strategy-based-on-diels-alder-and-ene-reactions
#14
Dominique Brossard, Pascal Retailleau, Vincent Dumontet, Philippe Breton, Sandy Desrat, Fanny Roussi
Thermic dimerization of methyl 1,3-cyclohexadiene 2-carboxylate gave original 3D-shape compounds by Diels-Alder cycloaddition and original [6 + 4]-ene reaction. Further selective modifications on an endo [4 + 2] cycloadduct via a diversity oriented synthesis (DOS) strategy quickly led to the preparation of a small library of original 3D scaffolds, providing access to a larger and unexplored chemical space for drug discovery processes.
June 22, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28639115/chemical-composition-of-selected-commercial-herbal-remedies-in-relation-to-geographical-origin-and-inter-species-diversity
#15
Pawel Konieczynski, Agnieszka Viapiana, Roman Lysiuk, Marek Wesolowski
Infusions prepared from medicinal herbs that are rich in flavonoids are very popular herbal remedies in societies of Eastern Europe. Therefore, the content of essential elements together with total flavonoids was analyzed in 65 commercially available samples of herbal drugs originating from Ukraine, Romania, and Belarus. The results showed that metallic elements (in mg kg(-1) d.w.) have occurred in the following order: Fe > Mn > Zn > Cu, both for total and water-extractable species. Total flavonoids were determined in the range from 10...
June 21, 2017: Biological Trace Element Research
https://www.readbyqxmd.com/read/28638868/in-vivo-effect-of-ruta-chalepensis-extract-on-hepatic-cytochrome-3a1-in-rats
#16
Edith Fabiola Martínez-Pérez, Fernando Hernández-Terán, Luis Benjamín Serrano-Gallardo
BACKGROUND: Since the time when drugs began to be used, it became evident that they could produce a therapeutic effect, but also a clinical condition of toxicity or no effect at all on humans, despite using the same doses in different patients. Such untoward effects were termed "drug idiosyncrasy" and also "idiosyncratic drug effects", but the factors producing such diverse responses were never taken into account. MATERIALS AND METHODS: Ruta chalepensis L. (fringed rue) is an herbaceous plant of the Rutaceae family used in traditional medicine due to its properties, such as its analgesic and antipyretic effects...
2017: African Journal of Traditional, Complementary, and Alternative Medicines: AJTCAM
https://www.readbyqxmd.com/read/28638861/randomized-anticancer-and-cytotoxicity-activities-of-guibourtia-coleosperma-and-diospyros-chamaethamnus
#17
Florence Dushimemaria, C Iwanette Du Preez, Davis R Mumbengegwi
BACKGROUND: Plants have consistently proven to be a reliable and yet not fully explored source of medicines. In light of this, there is a constant demand for new treatment regimens for cancer. Namibia has a rich diversity of plant species of over 4300 with 17 % of them being endemic to Namibia. Plants growing in Namibia's diverse climatic zones produce many secondary metabolites as part of adaptation to their environment. This article focused on the screening of such phytochemicals and their cytotoxic and anticancer properties in vitro...
2017: African Journal of Traditional, Complementary, and Alternative Medicines: AJTCAM
https://www.readbyqxmd.com/read/28638377/a-novel-bromodomain-inhibitor-reverses-hiv-1-latency-through-specific-binding-with-brd4-to-promote-tat-and-p-tefb-association
#18
Huachao Huang, Shuai Liu, Maxime Jean, Sydney Simpson, He Huang, Mark Merkley, Tsuyoshi Hayashi, Weili Kong, Irene Rodríguez-Sánchez, Xiaofeng Zhang, Hailemichael O Yosief, Hongyu Miao, Jianwen Que, James J Kobie, James Bradner, Netty G Santoso, Wei Zhang, Jian Zhu
While combinatory antiretroviral therapy (cART) can effectively reduce HIV-1 viremia, it cannot eliminate HIV-1 infection. In the presence of cART, viral reservoirs remain latent, impeding the cure of HIV-1/AIDS. Recently, latency-reversing agents (LRAs) have been developed with the intent of purging latent HIV-1, providing an intriguing strategy for the eradication of the residual viral reservoirs. Our earlier studies show that the first-generation, methyl-triazolo bromodomain, and extra-terminal domain inhibitor (BETi), JQ1, facilitates the reversal of HIV-1 latency...
2017: Frontiers in Microbiology
https://www.readbyqxmd.com/read/28638082/tandem-malonate-based-glucosides-tmgs-for-membrane-protein-structural-studies
#19
Hazrat Hussain, Jonas S Mortensen, Yang Du, Claudia Santillan, Orquidea Ribeiro, Juyeon Go, Parameswaran Hariharan, Claus J Loland, Lan Guan, Brian K Kobilka, Bernadette Byrne, Pil Seok Chae
High-resolution membrane protein structures are essential for understanding the molecular basis of diverse biological events and important in drug development. Detergents are usually used to extract these bio-macromolecules from the membranes and maintain them in a soluble and stable state in aqueous solutions for downstream characterization. However, many eukaryotic membrane proteins solubilized in conventional detergents tend to undergo structural degradation, necessitating the development of new amphiphilic agents with enhanced properties...
June 21, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28637430/malaria-control-by-commodities-without-practical-malariology
#20
J Kevin Baird
Malaria remains a serious clinical and public health problem, the object of an ongoing technological and humanitarian struggle to abate the very substantial harm done. The manner by which humanity approached malaria control changed abruptly and profoundly after 1945 with the advent of the insecticide DDT. Malariologists in the first half of the twentieth century conceived precise modifications to natural or man-made environments aimed at making those less hospitable to specific anopheline mosquito vector species...
June 21, 2017: BMC Public Health
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