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https://www.readbyqxmd.com/read/29342135/structures-of-%C3%AE-klotho-reveal-a-zip-code-like-mechanism-for-endocrine-fgf-signalling
#1
Sangwon Lee, Jungyuen Choi, Jyotidarsini Mohanty, Leiliane P Sousa, Francisco Tome, Els Pardon, Jan Steyaert, Mark A Lemmon, Irit Lax, Joseph Schlessinger
Canonical fibroblast growth factors (FGFs) activate FGF receptors (FGFRs) through paracrine or autocrine mechanisms in a process that requires cooperation with heparan sulfate proteoglycans, which function as co-receptors for FGFR activation. By contrast, endocrine FGFs (FGF19, FGF21 and FGF23) are circulating hormones that regulate critical metabolic processes in a variety of tissues. FGF19 regulates bile acid synthesis and lipogenesis, whereas FGF21 stimulates insulin sensitivity, energy expenditure and weight loss...
January 17, 2018: Nature
https://www.readbyqxmd.com/read/29342104/synthesis-anti-proliferative-activity-evaluation-and-3d-qsar-study-of-naphthoquinone-derivatives-as-potential-anti-colorectal-cancer-agents
#2
Julio Acuña, Jhoan Piermattey, Daneiva Caro, Sven Bannwitz, Luis Barrios, Jairo López, Yanet Ocampo, Ricardo Vivas-Reyes, Fabio Aristizábal, Ricardo Gaitán, Klaus Müller, Luis Franco
Colorectal cancer (CRC) is a disease with high incidence and mortality, constituting the fourth most common cause of death from cancer worldwide. Naphthoquinones are attractive compounds due to their biological and structural properties. In this work, 36 naphthoquinone derivatives were synthesized and their activity evaluated against HT-29 cells. Overall, high to moderate anti-proliferative activity was observed in most members of the series, with 15 compounds classified as active (1.73 < IC50 < 18.11 μM)...
January 17, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29341418/hand-held-clinical-dual-mode-ultrasound-photoacoustic-imaging-of-rat-urinary-bladder-and-its-applications
#3
Kathyayini Sivasubramanian, Vijitha Periyasamy, Rhonnie Austria Dienzo, Manojit Pramanik
Urinary bladder imaging is critical to diagnose urinary tract disorders, and bladder cancer. There is a great need for safe, non-invasive, and sensitive imaging technique which enables bladder imaging. Photoacoustic imaging is a rapidly growing imaging technique for various biological applications. It can be combined with clinical ultrasound imaging system for hand-held, dual modal ultrasound-photoacoustic real-time imaging. Structural (bladder wall) and functional (accretion of nanoparticles) bladder imaging is shown here with combined ultrasound and photoacoustic imaging in rats...
January 17, 2018: Journal of Biophotonics
https://www.readbyqxmd.com/read/29341023/anesthesia-and-monitoring-of-animals-during-mri-studies
#4
Jordi L Tremoleda, Sven Macholl, Jane K Sosabowski
The use of imaging represents a major impact on the refinement and the reduction of in vivo studies in animal models, in particular for allowing longitudinal monitoring of the onset and the progression of disease within the same animal, and studying the biological effects of drug candidate and their therapeutic effectiveness. But the use of imaging procedures can affect animal physiology, and the need to anesthetize the animals for imaging entails potential health risks. During anesthesia, there is an inevitable autonomic nervous system depression which induces cardiovascular depression, respiratory depression, and hypothermia...
2018: Methods in Molecular Biology
https://www.readbyqxmd.com/read/29341020/mri-in-the-study-of-animal-models-of-stroke
#5
Pedro Ramos-Cabrer, Daniel Padro
Stroke consists of the loss of cerebral functions resulting from the interruption of blood supply to a region of the brain, and represents the second cause of death and the leading cause of major disability in adults in Europe. Stroke is a very active field of research at preclinical and clinical levels, and Magnetic Resonance Imaging (MRI) is one of the most powerful tools that scientist and clinicians have for the study of the onset, evolution and consequences of this devastating disease, as well as for the monitoring of the success of available treatments, or for the development of novel therapeutic strategies...
2018: Methods in Molecular Biology
https://www.readbyqxmd.com/read/29341016/oxygenation-imaging-by-nuclear-magnetic-resonance-methods
#6
Heling Zhou, Nuria Arias-Ramos, Pilar López-Larrubia, Ralph P Mason, Sebastián Cerdán, Jesús Pacheco-Torres
Oxygen monitoring is a topic of exhaustive research due to its central role in many biological processes, from energy metabolism to gene regulation. The ability to monitor in vivo the physiological distribution and the dynamics of oxygen from subcellular to macroscopic levels is a prerequisite to better understand the mechanisms associated with both normal and disease states (cancer, neurodegeneration, stroke, etc.). This chapter focuses on magnetic resonance imaging (MRI) based techniques to assess oxygenation in vivo...
2018: Methods in Molecular Biology
https://www.readbyqxmd.com/read/29340619/recurrent-serious-infections-in-patients-with-rheumatoid-arthritis-results-from-the-british-society-for-rheumatology-biologics-register
#7
Sujith Subesinghe, Andrew Ian Rutherford, Rachel Byng-Maddick, Kimme Leanne Hyrich, James Benjamin Galloway
Objectives: To establish the rate of recurrent infection in RA patients recruited to the British Society for Rheumatology Biologics Register - Rheumatoid Arthritis. Secondary objectives were to establish whether the organ class of index infection predicted future serious infection (SI). Methods: Using data from the British Society for Rheumatology Biologics Register - Rheumatoid Arthritis, a prospective observational cohort, we identified patients with at least one episode of SI...
January 10, 2018: Rheumatology
https://www.readbyqxmd.com/read/29339554/synthetic-biology-strategies-for-improving-microbial-synthesis-of-green-biopolymers
#8
Lisa A Anderson, M Ahsanul Islam, Kristala L J Prather
Polysaccharide-based biopolymers have many material properties relevant to industrial and medical uses, including as drug delivery agents, wound healing adhesives, and food additives and stabilizers. Traditionally, polysaccharides are obtained from natural sources. Microbial synthesis offers an attractive alternative for sustainable production of tailored biopolymers. Here, we review synthetic biology strategies for select "green" biopolymers: cellulose, alginate, chitin, chitosan, and hyaluronan. Microbial production pathways, opportunities for pathway yield improvements, and advances in microbial engineering of biopolymers in various hosts are discussed...
January 16, 2018: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29339255/design-synthesis-and-biological-evaluation-of-lx2343-derivatives-as-neuroprotective-agents-for-the-treatment-of-alzheimer-s-disease
#9
Guanglong Sun, Junwei Wang, Xiaodan Guo, Min Lei, Yinan Zhang, Xiachang Wang, Xu Shen, Lihong Hu
A series of LX2343 derivatives were designed, synthesized and evaluated as neuroprotective agents for Alzheimer's disease (AD) in vitro. Most of the compounds displayed potent neuroprotective activities. Especially for compound A6, exhibited a remarkable EC50 value of 0.22 μM. Further investigation demonstrated that compound A6 can significantly reduce Aβ production and increase Aβ clearance, and alleviate Tau hyperphosphorylation. Most importantly, compound A6 could ameliorate learning and memory impairments in APP/PS1 transgenic mice...
January 2, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29338771/regulation-of-aquaporins-in-plants-under-stress
#10
REVIEW
Ranganathan Kapilan, Maryam Vaziri, Janusz J Zwiazek
Aquaporins (AQP) are channel proteins belonging to the Major Intrinsic Protein (MIP) superfamily that play an important role in plant water relations. The main role of aquaporins in plants is transport of water and other small neutral molecules across cellular biological membranes. AQPs have remarkable features to provide an efficient and often, specific water flow and enable them to transport water into and out of the cells along the water potential gradient. Plant AQPs are classified into five main subfamilies including the plasma membrane intrinsic proteins (PIPs), tonoplast intrinsic proteins (TIPs), nodulin 26 like intrinsic proteins (NIPs), small basic intrinsic proteins (SIPs) and X intrinsic proteins (XIPs)...
January 16, 2018: Biological Research
https://www.readbyqxmd.com/read/29338721/infectious-keratoconjunctivitis-in-semi-domesticated-eurasian-tundra-reindeer-rangifer-tarandus-tarandus-microbiological-study-of-clinically-affected-and-unaffected-animals-with-special-reference-to-cervid-herpesvirus-2
#11
Javier Sánchez Romano, Torill Mørk, Sauli Laaksonen, Erik Ågren, Ingebjørg H Nymo, Marianne Sunde, Morten Tryland
BACKGROUND: Infectious keratoconjunctivitis (IKC) is one of the most common ocular diseases in ruminants worldwide. In addition to keratitis and conjunctivitis, animals with IKC can develop uveitis, corneal ulcer, and in severe cases, blindness. The bacteria Moraxella spp. has been described as the primary causative agent of infectious bovine keratoconjunctivitis (IBK) in cattle (Bos taurus), while Chlamydia spp. and Mycoplasma conjunctivae are considered the main causative agents of IKC in sheep (Ovis aries)...
January 16, 2018: BMC Veterinary Research
https://www.readbyqxmd.com/read/29338536/p2y12-receptor-inhibitors-an-evolution-in-drug-design-to-prevent-arterial-thrombosis
#12
Danny Kupka, Dirk Sibbing
P2Y12 inhibitors are a critical component of dual antiplatelet therapy (DAPT) - a combination of a P2Y12 receptor inhibitor and aspirin - which is the superior strategy to prevent arterial thrombosis in patients with acute coronary syndromes (ACS) and undergoing stent implantation. Areas covered: Basic science articles, clinical studies, and reviews from 1992-2017 were searched using Pubmed library to collet impactful literature. After an introduction to the purinergic receptor biology, this review summarizes current knowledge on P2Y12 receptor inhibitors including their specific pharmacodynamic as well as pharmacokinetic and drug interaction features...
January 17, 2018: Expert Opinion on Drug Metabolism & Toxicology
https://www.readbyqxmd.com/read/29337925/plant-secondary-metabolites-as-anticancer-agents-successes-in-clinical-trials-and-therapeutic-application
#13
REVIEW
Ana M L Seca, Diana C G A Pinto
Cancer is a multistage process resulting in an uncontrolled and abrupt division of cells and is one of the leading causes of mortality. The cases reported and the predictions for the near future are unthinkable. Food and Drug Administration data showed that 40% of the approved molecules are natural compounds or inspired by them, from which, 74% are used in anticancer therapy. In fact, natural products are viewed as more biologically friendly, that is less toxic to normal cells. In this review, the most recent and successful cases of secondary metabolites, including alkaloid, diterpene, triterpene and polyphenolic type compounds, with great anticancer potential are discussed...
January 16, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29337878/tetrasubstituted-imidazolium-salts-as-potent-antiparasitic-agents-against-african-and-american-trypanosomiases
#14
Ouldouz Ghashghaei, Nicola Kielland, Marc Revés, Martin C Taylor, John M Kelly, Ornella Di Pietro, Diego Muñoz-Torrero, Belén Pérez, Rodolfo Lavilla
Imidazolium salts are privileged compounds in organic chemistry, and have valuable biological properties. Recent studies show that symmetric imidazolium salts with bulky moieties can display antiparasitic activity against T. cruzi. After developing a facile methodology for the synthesis of tetrasubstituted imidazolium salts from propargylamines and isocyanides, we screened a small library of these adducts against the causative agents of African and American trypanosomiases. These compounds display nanomolar activity against T...
January 16, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29337486/improving-risk-stratification-among-veterans-diagnosed-with-prostate-cancer-impact-of-the-17-gene-prostate-score-assay
#15
Julie A Lynch, Megan P Rothney, Raoul R Salup, Cesar E Ercole, Sharad C Mathur, David A Duchene, Joseph W Basler, Javier Hernandez, Michael A Liss, Michael P Porter, Jonathan L Wright, Michael C Risk, Mark Garzotto, Olga Efimova, Laurie Barrett, Brygida Berse, Michael J Kemeter, Phillip G Febbo, Atreya Dash
BACKGROUND: Active surveillance (AS) has been widely implemented within Veterans Affairs' medical centers (VAMCs) as a standard of care for low-risk prostate cancer (PCa). Patient characteristics such as age, race, and Agent Orange (AO) exposure may influence advisability of AS in veterans. The 17-gene assay may improve risk stratification and management selection. OBJECTIVES: To compare management strategies for PCa at 6 VAMCs before and after introduction of the Oncotype DX Genomic Prostate Score (GPS) assay...
January 2018: American Journal of Managed Care
https://www.readbyqxmd.com/read/29337321/synthesis-spectroscopic-investigation-and-dft-study-of-n-n-disubstituted-ferrocene-based-thiourea-complexes-as-potent-anticancer-agents
#16
Faiza Asghar, Saira Fatima, Sadaf Rana, Amin Badshah, Ian S Butler, Muhammad Nawaz Tahir
In the present work, the synthesis, characterization (FT-IR, multinuclear (1H and 13C) NMR, AAS, Raman, and elemental analyses), DNA binding (cyclic voltammetry, UV-Vis spectroscopy), and in vitro biological screening of nine new ferrocene-incorporated thioureas (A1-A9) are reported. Furthermore, the single-crystal X-ray structure of compound A8 was also determined. The ferrocene-based N,N'-disubstituted thioureas were derived by allowing the ferrocenyl anilines to react with freshly prepared isothiocyanates under a N2 atmosphere in dry acetone...
January 16, 2018: Dalton Transactions: An International Journal of Inorganic Chemistry
https://www.readbyqxmd.com/read/29337270/the-cationic-tetradecapeptide-mastoparan-as-a-privileged-structure-for-drug-discovery-enhanced-antimicrobial-properties-of-mitoparan-analogues-modified-at-position-14
#17
John Howl, Lewis Howl, Sarah Jones
Mastoparan (MP) peptides, distributed in insect venoms, induce a local inflammatory response post envenomation. Most endogenous MPs share common structural elements within a tetradecapeptide sequence that adopts an amphipathic helix whilst traversing biological membranes and when bound to an intracellular protein target. Rational modifications to increase cationic charge density and amphipathic helicity engineered mitoparan (MitP), a mitochondriotoxic bioportide and potent secretagogue. Following intracellular translocation, MitP is accreted by mitochondria thus indicating additional utility as an antimicrobial agent...
January 11, 2018: Peptides
https://www.readbyqxmd.com/read/29337264/indirect-reciprocity-with-negative-assortment-and-limited-information-can-promote-cooperation
#18
Eleanor Brush, Åke Brännström, Ulf Dieckmann
Cooperation is ubiquitous in biological and social systems, even though cooperative behavior is often costly and at risk of exploitation by non-cooperators. Several studies have demonstrated that indirect reciprocity, whereby some members of a group observe the behaviors of their peers and use this information to discriminate against previously uncooperative agents in the future, can promote prosocial behavior. Some studies have shown that differential propensities of interacting among and between different types of agents (interaction assortment) can increase the effectiveness of indirect reciprocity...
January 11, 2018: Journal of Theoretical Biology
https://www.readbyqxmd.com/read/29336595/exploitation-of-microbial-antagonists-for-the-control-of-postharvest-diseases-of-fruits-a-review
#19
Ajinath Shridhar Dukare, Sangeeta Paul, V Eyarkai Nambi, Ram Kishore Gupta, Rajbir Singh, Kalyani Sharma, Rajesh Kumar Vishwakarma
Fungal diseases result in significant losses of fruits and vegetables during handling, transportation and storage. At present, post-production fungal spoilage is predominantly controlled by using synthetic fungicides. Under the global climate change scenario and with the need for sustainable agriculture, biological control methods of fungal diseases, using antagonistic microorganisms, are emerging as ecofriendly alternatives to the use of fungicides. The potential of microbial antagonists, isolated from a diversity of natural habitats, for postharvest disease suppression has been investigated...
January 16, 2018: Critical Reviews in Food Science and Nutrition
https://www.readbyqxmd.com/read/29336560/trifluoromethyl-substituted-iridium-iii-complexes-from-photophysics-to-photooxidation-of-a-biological-target
#20
Robin Bevernaegie, Lionel Marcélis, Baptiste Laramée-Milette, Julien De Winter, Koen Robeyns, Pascal Gerbaux, Garry S Hanan, Benjamin Elias
Photodynamic therapeutic agents are of key interest in developing new strategies to develop more specific and efficient anticancer treatments. In comparison to classical chemotherapeutic agents, the activity of photodynamic therapeutic compounds can be finely controlled thanks to the light triggering of their photoreactivity. The development of type I photosensitizing agents, which do not rely on the production of ROS, is highly desirable. In this context, we developed new iridium(III) complexes which are able to photoreact with biomolecules; namely, our Ir(III) complexes can oxidize guanine residues under visible light irradiation...
January 16, 2018: Inorganic Chemistry
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