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https://www.readbyqxmd.com/read/28938089/drug-discovery-and-chemical-biology-of-cancer-epigenetics
#1
REVIEW
Scott Ribich, Darren Harvey, Robert A Copeland
Comprehensive whole-exome sequencing, DNA copy-number determination, and transcriptomic analyses of diverse cancers have greatly expanded our understanding of the biology of many tumor types. In addition to mutations in the common cell-of-origin specific driver mutations, these studies have also revealed a large number of loss-of-function and gain-of-function mutations in chromatin-modifying proteins (CMPs). This has revealed that epigenetic dysregulation is a common feature of most pediatric and adult cancers...
September 21, 2017: Cell Chemical Biology
https://www.readbyqxmd.com/read/28935948/novel-scaffolds-for-inhibition-of-cruzipain-identified-from-high-throughput-screening-of-anti-kinetoplastid-chemical-boxes
#2
Emir Salas-Sarduy, Lionel Urán Landaburu, Joel X Karpiak, Kevin P Madauss, Juan José Cazzulo, Fernán Agüero, Vanina Eder Alvarez
American Trypanosomiasis or Chagas disease is a prevalent, neglected and serious debilitating illness caused by the kinetoplastid protozoan parasite Trypanosoma cruzi. The current chemotherapy is limited only to nifurtimox and benznidazole, two drugs that have poor efficacy in the chronic phase and are rather toxic. In this scenario, more efficacious and safer drugs, preferentially acting through a different mechanism of action and directed against novel targets, are particularly welcome. Cruzipain, the main papain-like cysteine peptidase of T...
September 21, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28935887/bitter-or-not-bitterpredict-a-tool-for-predicting-taste-from-chemical-structure
#3
Ayana Dagan-Wiener, Ido Nissim, Natalie Ben Abu, Gigliola Borgonovo, Angela Bassoli, Masha Y Niv
Bitter taste is an innately aversive taste modality that is considered to protect animals from consuming toxic compounds. Yet, bitterness is not always noxious and some bitter compounds have beneficial effects on health. Hundreds of bitter compounds were reported (and are accessible via the BitterDB http://bitterdb.agri.huji.ac.il/dbbitter.php ), but numerous additional bitter molecules are still unknown. The dramatic chemical diversity of bitterants makes bitterness prediction a difficult task. Here we present a machine learning classifier, BitterPredict, which predicts whether a compound is bitter or not, based on its chemical structure...
September 21, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28935266/diverse-amide-analogs-of-sulindac-for-cancer-treatment-and-prevention
#4
Bini Mathew, Judith V Hobrath, Michele C Connelly, R Kiplin Guy, Robert C Reynolds
Sulindac is a non-steroidal anti-inflammatory drug (NSAID) that has shown significant anticancer activity. Sulindac sulfide amide (1) possessing greatly reduced COX-related inhibition relative to sulindac displayed in vivo antitumor activity that was comparable to sulindac in a human colon tumor xenograft model. Inspired by these observations, a panel of diverse sulindac amide derivatives have been synthesized and their activity probed against three cancer cell lines (prostate, colon and breast). A neutral analog, compound 79 was identified with comparable potency relative to lead 1 and activity against a panel of lymphoblastic leukemia cell lines...
September 13, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28935100/a-critical-review-on-the-prospect-of-polyaniline-grafted-biodegradable-nanocomposite
#5
REVIEW
Mohammad Shahadat, Mohammad Zain Khan, Parveen Fatemeh Rupani, Asha Embrandiri, Saima Sultana, Shaikh Ziauddin Ahammad, S Wazed Ali, T R Sreekrishnan
Among the various electrically conducting polymers, polyaniline (PANI) has gained attentions due to its unique properties and doping chemistry. A number of electrically conducting biodegradable polymers has been synthesized by incorporating a biodegradable content of cellulose, chitin, chitosan, etc. in the matrix of PANI. The hybrid materials are also employed as photocatalysts, antibacterial agents, sensors, fuel cells and as materials in biomedical applications. Furthermore, these biodegradable and biocompatible conducting polymers are employed in tissue engineering, dental implants and targeted drug delivery...
September 6, 2017: Advances in Colloid and Interface Science
https://www.readbyqxmd.com/read/28934265/comparative-effectiveness-of-different-transarterial-embolization-therapies-alone-or-in-combination-with-local-ablative-or-adjuvant-systemic-treatments-for-unresectable-hepatocellular-carcinoma-a-network-meta-analysis-of-randomized-controlled-trials
#6
Konstantinos Katsanos, Panagiotis Kitrou, Stavros Spiliopoulos, Ioannis Maroulis, Theodore Petsas, Dimitris Karnabatidis
BACKGROUND: The optimal transcatheter embolization strategy for patients with unresectable hepatocellular carcinoma (HCC) remains elusive. We conducted a systematic review and network meta-analysis (NMA) of different embolization options for unresectable HCC. METHODS: Medical databases were searched for randomized controlled trials evaluating bland transarterial embolization (TAE), conventional TACE, drug-eluting bead chemoembolization (DEB-TACE), or transarterial radioembolization (TARE), either alone or combined with adjuvant chemotherapy, or local liver ablation, or external radiotherapy for unresectable HCC up to June 2017...
2017: PloS One
https://www.readbyqxmd.com/read/28933948/the-value-and-application-of-the-six-minute-walk-test-in-idiopathic-pulmonary-fibrosis
#7
A Whitney Brown, Steven D Nathan
The 6 minute walk test (6MWT) is a commonly employed assessment of performance ability in a variety of cardiopulmonary diseases. It provides important functional information that is not captured in standardized pulmonary function testing. The test may be influenced by factors other than the severity of lung disease, including frailty, deconditioning, and musculoskeletal issues. The primary output measure from the six minute walk test is the distance walked, which appears to confer prognostic information in many diverse disease states...
September 21, 2017: Annals of the American Thoracic Society
https://www.readbyqxmd.com/read/28933723/artificial-lipid-membranes-past-present-and-future
#8
REVIEW
Christina G Siontorou, Georgia-Paraskevi Nikoleli, Dimitrios P Nikolelis, Stefanos K Karapetis
The multifaceted role of biological membranes prompted early the development of artificial lipid-based models with a primary view of reconstituting the natural functions in vitro so as to study and exploit chemoreception for sensor engineering. Over the years, a fair amount of knowledge on the artificial lipid membranes, as both, suspended or supported lipid films and liposomes, has been disseminated and has helped to diversify and expand initial scopes. Artificial lipid membranes can be constructed by several methods, stabilized by various means, functionalized in a variety of ways, experimented upon intensively, and broadly utilized in sensor development, drug testing, drug discovery or as molecular tools and research probes for elucidating the mechanics and the mechanisms of biological membranes...
July 26, 2017: Membranes
https://www.readbyqxmd.com/read/28933550/boron-heteroatom-addition-reactions-via-borylative-heterocyclization-oxyboration-aminoboration-and-thioboration
#9
Adena Issaian, Kim N Tu, Suzanne A Blum
Organoboron compounds and heterocycles are powerful building blocks and precursors for organic synthesis, including for drug discovery and agrochemical and material synthesis. The common strategy for the synthesis of borylated heterocycles involves two separate synthetic steps: first, synthesis of the heterocyclic core, and second, borylation of the core through established methods such as transition-metal-catalyzed C-H or C-X activation/borylation or lithiation/borylation. In this Account, we describe our laboratory's development of borylative heterocyclization reactions that access the heterocyclic core and install boron in one synthetic step...
September 21, 2017: Accounts of Chemical Research
https://www.readbyqxmd.com/read/28933153/rapid-sequential-in-situ-multiplexing-with-dna-exchange-imaging-in-neuronal-cells-and-tissues
#10
Yu Wang, Johannes B Woehrstein, Noah Donoghue, Mingjie Dai, Maier S Avendano, Ron C J Schackmann, Jason Zoeller, Shan Shan H Wang, Paul W Tillberg, Demian Park, Sylvain W Lapan, Edward S Boyden, Joan S Brugge, Pascal S Kaeser, George Church, Sarit S Agasti, Ralf Jungmann, Peng Yin
To decipher the molecular mechanism of biological function, it is critical to map the molecular composition of individual cells or even more importantly tissue samples in the context of their biological environment in situ. Immunofluorescence (IF) provides specific labeling for molecular profiling. However, conventional IF methods have finite multiplexing capabilities due to spectral overlap of the fluorophores. Various sequential imaging methods have been developed to circumvent this spectral limit, but are not widely adopted due to the common limitation of requiring multi-rounds of slow (typically over 2 hours at room temperature to overnight at 4 °C in practice) immunostaining...
September 21, 2017: Nano Letters
https://www.readbyqxmd.com/read/28933075/-key-technologies-in-synthetic-biology-of-natural-products
#11
Xue-Jun Kuang, Li-Qiu Zou, Ying Li, Chao Sun, Shi-Lin Chen
Natural products with complex and diverse structures are the major sources of new drugs. The biosynthesis of natural products is considered to be one of the best ways to solve the problems of complex and scarce natural products. DNA assembly technology and genome editing technology are two key technologies in the emerging interdisciplinary field of synthetic biology. A number of novel DNA assembly methods developed in the last few years have paved the way for the engineering of high molecular weight DNA molecules, including whole genomes, hence, it can realize the reconstruction of the metabolic pathways and speed up optimization process...
November 2016: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/28933057/healthcare-finance-in-the-kingdom-of-saudi-arabia-a-qualitative-study-of-householders-attitudes
#12
Mohammed Khaled Al-Hanawi, Omar Alsharqi, Saja Almazrou, Kirit Vaidya
BACKGROUND: The public sector healthcare system in Saudi Arabia, essentially financed by oil revenues and 'free at the point of delivery', is coming under increasing strain due to escalating expenditure and an increasingly volatile oil market and is likely to be unsustainable in the medium to long term. OBJECTIVES: This study examines how satisfied the Saudi people are with their public sector healthcare services and assesses their willingness to contribute to financing the system through a national health insurance scheme...
September 20, 2017: Applied Health Economics and Health Policy
https://www.readbyqxmd.com/read/28932664/strong-electro-optic-effect-and-spontaneous-domain-formation-in-self-assembled-peptide-structures
#13
Barak Gilboa, Clément Lafargue, Amir Handelman, Linda J W Shimon, Gil Rosenman, Joseph Zyss, Tal Ellenbogen
Short peptides made from repeating units of phenylalanine self-assemble into a remarkable variety of micro- and nanostructures including tubes, tapes, spheres, and fibrils. These bio-organic structures are found to possess striking mechanical, electrical, and optical properties, which are rarely seen in organic materials, and are therefore shown useful for diverse applications including regenerative medicine, targeted drug delivery, and biocompatible fluorescent probes. Consequently, finding new optical properties in these materials can significantly advance their practical use, for example, by allowing new ways to visualize, manipulate, and utilize them in new, in vivo, sensing applications...
September 2017: Advanced Science (Weinheim, Baden-Wurttemberg, Germany)
https://www.readbyqxmd.com/read/28931899/energetics-and-mechanism-of-anion-permeation-across-formate-nitrite-transporters
#14
Kalina Atkovska, Jochen S Hub
Formate-nitrite transporters (FNTs) facilitate the translocation of monovalent polyatomic anions, such as formate and nitrite, across biological membranes. FNTs are widely distributed among pathogenic bacteria and eukaryotic parasites, but they lack human homologues, making them attractive drug targets. The mechanisms and energetics involved in anion permeation across the FNTs have remained largely unclear. Both, channel and transporter mode of function have been proposed, with strong indication of proton coupling to the permeation process...
September 20, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28931883/high-throughput-targeted-screening-in-triple-negative-breast-cancer-cells-identifies-wnt-inhibiting-activities-in-pacific-brittle-stars
#15
Artem Blagodatski, Vsevolod Cherepanov, Alexey Koval, Vladimir I Kharlamenko, Yuri S Khotimchenko, Vladimir L Katanaev
Pro-proliferative oncogenic signaling is one of the hallmarks of cancer. Specific targeting of such signaling pathways is one of the main approaches to modern anti-cancer drug discovery, as opposed to more traditional search for general cytotoxic agents. Natural products, especially from marine sources, represent a largely untapped source of chemical diversity, which so far have mostly been screened for cytotoxicity. Here we present a pioneering pipeline of high-throughput screening of marine-based activities targeted against the Wnt signaling pathway, which is one of the key factors in oncogenic transformation, growth and metastasis in different cancers, including the devastating triple-negative breast cancer (TNBC) currently lacking any targeted therapies...
September 20, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28931879/longitudinal-analysis-of-colon-crypt-stem-cell-dynamics-in-sulindac-treated-familial-adenomatous-polyposis-patients
#16
Huiying Ma, Lodewijk A A Brosens, Sjoerd G Elias, Folkert H M Morsink, Isaac J Nijman, Linda M Hylind, Elizabeth A Montgomery, G Johan A Offerhaus, Francis M Giardiello, Wendy W J de Leng
The non-steroidal anti-inflammatory drug sulindac decreases size and number of adenomas after 4-6 months of treatment for familial adenomatous polyposis (FAP) patients. However, the underlying mechanism remains unknown. As stem cells are thought to be the tumor precursor cells, visualizing their behavior is crucial for monitoring tumor progression. Increased tag diversity in inactive genes is indicative of a protracted clonal evolution and consequently, increased risk for tumor formation. Therefore, the effect of sulindac on stem cell dynamics was studied...
September 20, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28931623/small-molecule-screens-a-gateway-to-cancer-therapeutic-agents-with-case-studies-of-food-and-drug-administration-approved-drugs
#17
REVIEW
Nathan P Coussens, John C Braisted, Tyler Peryea, G Sitta Sittampalam, Anton Simeonov, Matthew D Hall
High-throughput screening (HTS) of small-molecule libraries accelerates the discovery of chemical leads to serve as starting points for probe or therapeutic development. With this approach, thousands of unique small molecules, representing a diverse chemical space, can be rapidly evaluated by biologically and physiologically relevant assays. The origins of numerous United States Food and Drug Administration-approved cancer drugs are linked to HTS, which emphasizes the value in this methodology. The National Institutes of Health Molecular Libraries Program made HTS accessible to the public sector, enabling the development of chemical probes and drug-repurposing initiatives...
October 2017: Pharmacological Reviews
https://www.readbyqxmd.com/read/28931578/lipid-topology-and-electrostatic-interactions-underpin-lytic-activity-of-linear-cationic-antimicrobial-peptides-in-membranes
#18
David J Paterson, Manlio Tassieri, Julien Reboud, Rab Wilson, Jonathan M Cooper
Linear cationic antimicrobial peptides are a diverse class of molecules that interact with a wide range of cell membranes. Many of these peptides disrupt cell integrity by forming membrane-spanning pores that ultimately lead to their death. Despite these peptides high potency and ability to evade acquired bacterial drug resistance, there is a lack of knowledge on their selectivity and activity mechanisms. Such an understanding would provide an informative framework for rational design and could lead to potential antimicrobial therapeutic targets...
September 20, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28931490/gpcrs-emerging-anti-cancer-drug-targets
#19
REVIEW
Ainhoa Nieto Gutierrez, Patricia H McDonald
G protein-coupled receptors (GPCRs) constitute the largest and most diverse protein family in the human genome with over 800 members identified to date. They play critical roles in numerous cellular and physiological processes, including cell proliferation, differentiation, neurotransmission, development and apoptosis. Consequently, aberrant receptor activity has been demonstrated in numerous disorders/diseases, and as a result GPCRs have become the most successful drug target class in pharmaceuticals treating a wide variety of indications such as pain, inflammation, neurobiological and metabolic disorders...
September 17, 2017: Cellular Signalling
https://www.readbyqxmd.com/read/28931441/tracking-progressive-pathological-and-functional-decline-in-the-rtg4510-mouse-model-of-tauopathy
#20
Thomas Blackmore, Soraya Meftah, Tracey Karen Murray, Peter James Craig, Anthony Blockeel, Keith Phillips, Brian Eastwood, Michael J O'Neill, Hugh Marston, Zeshan Ahmed, Gary Gilmour, Francois Gastambide
BACKGROUND: The choice and appropriate use of animal models in drug discovery for Alzheimer's disease (AD) is pivotal to successful clinical translation of novel therapeutics, yet true alignment of research is challenging. Current models do not fully recapitulate the human disease, and even exhibit various degrees of regional pathological burden and diverse functional alterations. Given this, relevant pathological and functional endpoints must be determined on a model-by-model basis. The present work explores the rTg4510 mouse model of tauopathy as a case study to define best practices for the selection and validation of cognitive and functional endpoints for the purposes of pre-clinical AD drug discovery...
September 20, 2017: Alzheimer's Research & Therapy
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