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https://www.readbyqxmd.com/read/28437395/global-survey-of-the-immunomodulatory-potential-of-common-drugs
#1
Gregory I Vladimer, Berend Snijder, Nikolaus Krall, Johannes W Bigenzahn, Kilian V M Huber, Charles-Hugues Lardeau, Kumar Sanjiv, Anna Ringler, Ulrika Warpman Berglund, Monika Sabler, Oscar Lopez de la Fuente, Paul Knöbl, Stefan Kubicek, Thomas Helleday, Ulrich Jäger, Giulio Superti-Furga
Small-molecule drugs may complement antibody-based therapies in an immune-oncology setting, yet systematic methods for the identification and characterization of the immunomodulatory properties of these entities are lacking. We surveyed the immumomodulatory potential of 1,402 small chemical molecules, as defined by their ability to alter the cell-cell interactions among peripheral mononuclear leukocytes ex vivo, using automated microscopy and population-wide single-cell image analysis. Unexpectedly, ∼10% of the agents tested affected these cell-cell interactions differentially...
April 24, 2017: Nature Chemical Biology
https://www.readbyqxmd.com/read/28431519/semi-automatic-synthesis-and-biodistribution-of-n-2-18-f-fluoropropionyl-bis-zinc-ii-dipicolylamine-18-f-fp-dpazn2-for-ad-model-imaging
#2
Fuhua Wen, Dahong Nie, Kongzhen Hu, Ganghua Tang, Shaobo Yao, Caihua Tang
BACKGROUND: Phosphatidylserine (PS)-targeting positron emission tomography (PET) imaging with labeled small-molecule tracer is a crucial non-invasive molecule imaging method of apoptosis. In this study, semi-automatic radiosynthesis and biodistribution of N-(2-(18)F-fluoropropionyl)-bis(zinc(II)-dipicolylamine) ((18)F-FP-DPAZn2), as a potential small-molecule tracer for PET imaging of cell death in Alzheimer's disease (AD) model, were performed. METHODS: (18)F-FP-DPAZn2 was synthesized on the modified PET-MF-2V-IT-I synthesizer...
April 21, 2017: BMC Medical Imaging
https://www.readbyqxmd.com/read/28430366/cyclic-rgd-penta-peptides-crgdyk-derivatized-with-cyclopentadienyl-complexes-of-technetium-and-rhenium-as-radiopharmaceutical-probes
#3
Qaisar Nadeem, Yunjun Shen, Muhammad Farooq Warsi, Gulfam Nasar, Muhammad Abdul Qadir, Roger Alberto
The present study reports the syntheses of half-sandwich complexes of the type [M(η(5) -C5 H4 CONH-R)(CO)3 ] (M = Re,(99m) Tc;R = cyclic RGD peptide (cRGDyK) for potential imaging of αv β3 integrin expression. The (99m) Tc complex was prepared directly from the reaction of [(99m) Tc(OH2 )3 (CO)3 ](+) with cRGDyK, doubly conjugated to Thiele's acid [(C5 H5 COOH)2 ] in water. This approach extends the viability of metal-mediated retro Diels-Alder reactions for the preparation of small molecules such as linear tripeptides to a more complex cyclic peptide carrying a [(η(5) -C5 H4 )(99m) Tc(CO)3 ] tag...
April 21, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28428090/preparation-and-characterization-of-lipid-nanoparticle-pdna-complexes-for-stat3-downregulation-and-overcoming-chemotherapy-resistance-in-lung-cancer-cells
#4
Mustafa Kotmakçı, Vildan Bozok Çetintaş, A Gülten Kantarcı
Developments in the field of molecular oncology have revealed that resistance to chemotherapeutics is acqured through several mechanisms including overexpression of common oncogenic proteins. Signal Transducer and Activator of Transcription 3 (STAT3) is one of these oncogenes that is overexpressed in many cancer types. RNA interference (RNAi) is proven powerful tool for downregulating STAT3, allowing re-sensitization of resistant cancer cells. However, delivery of RNA interference-mediating molecules for STAT3 downregulation in lung cancer cells is limited to a small number of studies most of which employ commercially available transfection kits...
April 18, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28426978/visualizing-spatial-distribution-of-small-molecules-in-the-rhubarb-stalk-rheum-rhabarbarum-by-surface-transfer-mass-spectrometry-imaging
#5
Joanna Nizioł, Justyna Sekuła, Tomasz Ruman
Laser desorption/ionization mass spectrometry imaging (LDI-MSI) with gold nanoparticle-enhanced target (AuNPET) was used for visualization of small molecules in the rhubarb stalk (Rheum rhabarbarum L.). Analysis was focused on spatial distribution of biologically active compounds which are found in rhubarb species. Detected compounds belong to a very wide range of chemical compound classes such as anthraquinone derivatives and their glucosides, stilbenes, anthocyanins, flavonoids, polyphenols, organic acids, chromenes, chromanones, chromone glycosides and vitamins...
April 17, 2017: Phytochemistry
https://www.readbyqxmd.com/read/28426939/high-throughput-agonist-shift-assay-development-for-the-analysis-of-m1-positive-allosteric-modulators
#6
Michelle F Homsher, Douglas C Beshore, Jason Cassaday, Brian Squadroni, Elizabeth Mohammed, Michelle Hartnett, Stephen Day, Lei Ma, David Pechter, Michelle D Smith, Fredrick Monsma, Paul Zuck, Michael F Finley, Victor N Uebele, Jeffrey D Hermes
Agonist shift assays feature cross-titrations of allosteric modulators and orthosteric ligands. Information generated in agonist shift assays can include a modulator's effect on the orthosteric agonist's potency (alpha) and efficacy (beta), as well as direct agonist activity of the allosteric ligand (tauB) and the intrinsic binding affinity of the modulator to the unoccupied receptor (KB). Because of the heavy resource demand and complex data handling, these allosteric parameters are determined infrequently during the course of a drug discovery program and on a relatively small subset of compounds...
April 1, 2017: SLAS Discovery
https://www.readbyqxmd.com/read/28426025/modular-low-light-microscope-for-imaging-cellular-bioluminescence-and-radioluminescence
#7
Tae Jin Kim, Silvan Türkcan, Guillem Pratx
Low-light microscopy methods are receiving increased attention as new applications have emerged. One such application is to allow longitudinal imaging of light-sensitive cells with no phototoxicity and no photobleaching of fluorescent biomarkers. Another application is for imaging signals that are inherently dim and undetectable using standard microscopy techniques, such as bioluminescence, chemiluminescence or radioluminescence. In this protocol, we provide instructions on how to build a modular low-light microscope (1-4 d) by coupling two microscope objective lenses, back to back from each other, using standard optomechanical components...
May 2017: Nature Protocols
https://www.readbyqxmd.com/read/28425493/characterization-of-different-microbubbles-in-assisting-focused-ultrasound-induced-blood-brain-barrier-opening
#8
Sheng-Kai Wu, Po-Chun Chu, Wen-Yen Chai, Shih-Tsung Kang, Chih-Hung Tsai, Ching-Hsiang Fan, Chih-Kuang Yeh, Hao-Li Liu
Microbubbles (MBs) serve as a critical catalyst to amplify local cavitation in CNS capillary lumen to facilitate focused ultrasound (FUS) to transiently open the blood-brain barrier (BBB). However, limited understanding is available regarding the effect of different microbubbles to induce BBB opening. The aim of this study is to characterize different MBs on their effect in FUS-induced BBB opening. Three MBs, SonoVue, Definity, and USphere, were tested, with 0.4-MHz FUS exposure at 0.62-1.38 of mechanical index (MI) on rats...
April 20, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28418679/bioresponsive-polyoxometalate-cluster-for-redox-activated-photoacoustic-imaging-guided-photothermal-cancer-therapy
#9
Dalong Ni, Dawei Jiang, Hector F Valdovinos, Emily B Ehlerding, Bo Yu, Todd E Barnhart, Peng Huang, Weibo Cai
Although various types of imaging agents have been developed for photoacoustic (PA) imaging, relatively few imaging agents exhibit high selectivity/sensitivity to the tumor microenvironment for on-demand PA imaging and therapy. Herein, molybdenum-based polyoxometalate (POM) clusters with the highest oxidation state of Mo(VI) (denoted as Ox-POM) were designed as novel agents for redox-activated PA imaging-guided photothermal therapy. Capable of escaping from recognition and capture by the liver and spleen, these renal clearable clusters with ultrasmall size (hydrodynamic size: 1...
April 20, 2017: Nano Letters
https://www.readbyqxmd.com/read/28418642/structure-and-dynamics-of-individual-diastereomeric-complexes-on-platinum-surface-studies-related-to-heterogeneous-enantioselective-catalysis
#10
Yi Dong, Guillaume Goubert, Michael N Groves, Jean-Christian Lemay, Bjørk Hammer, Peter H McBreen
The modification of heterogeneous catalysts through the chemisorption of chiral molecules is a method to create catalytic sites for enantioselective surface reactions. The chiral molecule is called a chiral modifier by analogy to the terms chiral auxiliary or chiral ligand used in homogeneous asymmetric catalysis. While there has been progress in understanding how chirality transfer occurs, the intrinsic difficulties in determining enantioselective reaction mechanisms are compounded by the multisite nature of heterogeneous catalysts and by the challenges facing stereospecific surface analysis...
April 18, 2017: Accounts of Chemical Research
https://www.readbyqxmd.com/read/28416697/small-molecule-mediated-inhibition-of-myofibroblast-transdifferentiation-for-the-treatment-of-fibrosis
#11
Michael J Bollong, Baiyuan Yang, Naja Vergani, Brittney A Beyer, Emily N Chin, Claudio Zambaldo, Danling Wang, Arnab K Chatterjee, Luke L Lairson, Peter G Schultz
Fibrosis, a disease in which excessive amounts of connective tissue accumulate in response to physical damage and/or inflammatory insult, affects nearly every tissue in the body and can progress to a state of organ malfunction and death. A hallmark of fibrotic disease is the excessive accumulation of extracellular matrix-secreting activated myofibroblasts (MFBs) in place of functional parenchymal cells. As such, the identification of agents that selectively inhibit the transdifferentiation process leading to the formation of MFBs represents an attractive approach for the treatment of diverse fibrosis-related diseases...
April 17, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28414203/self-assembled-nanocomplex-between-polymerized-phenylboronic-acid-and-doxorubicin-for-efficient-tumor-targeted-chemotherapy
#12
Junseok Lee, Jinhwan Kim, Yeong Mi Lee, Dongsik Park, Sooseok Im, Eun Ho Song, Hansoo Park, Won Jong Kim
Since the discovery that nano-scaled particulates can easily be incorporated into tumors via the enhanced permeability and retention (EPR) effect, such nanostructures have been exploited as therapeutic small molecule delivery systems. However, the convoluted synthetic process of conventional nanostructures has impeded their feasibility and reproducibility in clinical applications. Herein, we report an easily prepared formulation of self-assembled nanostructures for systemic delivery of the anti-cancer drug doxorubicin (DOX)...
April 17, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28409274/toward-molecular-imaging-of-the-free-fatty-acid-receptor-1
#13
Ewa Hellström-Lindahl, Ola Åberg, Cecilia Ericsson, Gavin O'Mahony, Peter Johnström, Stanko Skrtic, Olof Eriksson
AIMS: Molecular imaging of the free fatty acid receptor 1 (FFAR1) would be a valuable tool for drug development by enabling in vivo target engagement studies in human. It has also been suggested as a putative target for beta cell imaging, but the inherent lipophilicity of most FFAR1 binders produces high off-target binding, which has hampered progress in this area. The aim of this study was to generate a suitable lead compound for further PET labeling. METHODS: In order to identify a lead compound for future PET labeling for quantitative imaging of FFAR1 in human, we evaluated tritiated small molecule FFAR1 binding probes ([(3)H]AZ1, [(3)H]AZ2 and [(3)H]TAK-875) for their off-target binding, receptor density and affinity in human pancreatic tissue (islets and exocrine) and rodent insulinoma...
April 13, 2017: Acta Diabetologica
https://www.readbyqxmd.com/read/28402886/three-dimensional-super-resolution-in-eukaryotic-cells-using-the-double-helix-point-spread-function
#14
Alexander R Carr, Aleks Ponjavic, Srinjan Basu, James McColl, Ana Mafalda Santos, Simon Davis, Ernest D Laue, David Klenerman, Steven F Lee
Single-molecule localization microscopy, typically based on total internal reflection illumination, has taken our understanding of protein organization and dynamics in cells beyond the diffraction limit. However, biological systems exist in a complicated three-dimensional environment, which has required the development of new techniques, including the double-helix point spread function (DHPSF), to accurately visualize biological processes. The application of the DHPSF approach has so far been limited to the study of relatively small prokaryotic cells...
April 11, 2017: Biophysical Journal
https://www.readbyqxmd.com/read/28400509/oncogene-kras-activates-fatty-acid-synthase-resulting-in-specific-erk-and-lipid-signatures-associated-with-lung-adenocarcinoma
#15
Arvin M Gouw, Livia S Eberlin, Katherine Margulis, Delaney K Sullivan, Georgia G Toal, Ling Tong, Richard N Zare, Dean W Felsher
KRAS gene mutation causes lung adenocarcinoma. KRAS activation has been associated with altered glucose and glutamine metabolism. Here, we show that KRAS activates lipogenesis, and this activation results in distinct proteomic and lipid signatures. By gene expression analysis, KRAS is shown to be associated with a lipogenesis gene signature and specific induction of fatty acid synthase (FASN). Through desorption electrospray ionization MS imaging (DESI-MSI), specific changes in lipogenesis and specific lipids are identified...
April 11, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28399446/enzyme-mediated-tagging-of-rna
#16
REVIEW
Lea Anhäuser, Andrea Rentmeister
RNA molecules can play diverse roles in the cell owing to their secondary structure dynamics and various binding modes. Studying localization and dynamics of RNA in vitro or in cells requires tagging with suitable reporter molecules-fluorophores being the most prominent ones. Enzymatic RNA labeling approaches are currently emerging as valuable alternatives to purely chemical synthesis and to binding- or hybridization-based RNA-imaging approaches. Different classes of enzymes allow for cotranscriptional or posttranscriptional installation of small functional groups in RNA...
April 8, 2017: Current Opinion in Biotechnology
https://www.readbyqxmd.com/read/28397803/tomatidine-enhances-lifespan-and-healthspan-in-c-elegans-through-mitophagy-induction-via-the-skn-1-nrf2-pathway
#17
Evandro F Fang, Tyler B Waltz, Henok Kassahun, Qiping Lu, Jesse S Kerr, Marya Morevati, Elayne M Fivenson, Bradley N Wollman, Krisztina Marosi, Mark A Wilson, Wendy B Iser, D Mark Eckley, Yongqing Zhang, Elin Lehrmann, Ilya G Goldberg, Morten Scheibye-Knudsen, Mark P Mattson, Hilde Nilsen, Vilhelm A Bohr, Kevin G Becker
Aging is a major international concern that brings formidable socioeconomic and healthcare challenges. Small molecules capable of improving the health of older individuals are being explored. Small molecules that enhance cellular stress resistance are a promising avenue to alleviate declines seen in human aging. Tomatidine, a natural compound abundant in unripe tomatoes, inhibits age-related skeletal muscle atrophy in mice. Here we show that tomatidine extends lifespan and healthspan in C. elegans, an animal model of aging which shares many major longevity pathways with mammals...
April 11, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28396286/altered-mitochondrial-and-peroxisomal-integrity-in-lipocalin-2-deficient-mice-with-hepatic-steatosis
#18
Anastasia Asimakopoulou, Annabelle Fülöp, Erawan Borkham-Kamphorst, Eddy Van de Leur, Nikolaus Gassler, Thorsten Berger, Birte Beine, Helmut E Meyer, Tak W Mak, Carsten Hopf, Corinna Henkel, Ralf Weiskirchen
Lipocalin-2 (LCN2) is a secreted adipokine that transports small hydrophobic molecules such as fatty acids and steroids. LCN2 limits bacterial growth by sequestering iron-containing siderophores and in mammalian liver protects against inflammation, infection, injury and other stressors. Because LCN2 modulates hepatic fat metabolism and homeostasis, we performed a comparative profiling of proteins and lipids of wild type (WT) and Lcn2-deficient mice fed either standard chow or a methionine- and choline-deficient (MCD) diet...
April 7, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28395970/dynamic-contrast-enhanced-mri-detects-changes-in-vascular-transport-rate-constants-following-treatment-with-thermally-sensitive-liposomal-doxorubicin
#19
Brett Z Fite, Azadeh Kheirolomoom, Josquin L Foiret, Jai W Seo, Lisa M Mahakian, Elizabeth S Ingham, Sarah M Tam, Alexander D Borowsky, Fitz-Roy E Curry, Katherine W Ferrara
Temperature-sensitive liposomal formulations of chemotherapeutics, such as doxorubicin, can achieve locally high drug concentrations within a tumor and tumor vasculature while maintaining low systemic toxicity. Further, doxorubicin delivery by temperature-sensitive liposomes can reliably cure local cancer in mouse models. Histological sections of treated tumors have detected red cell extravasation within tumors treated with temperature-sensitive doxorubicin and ultrasound. We hypothesize that the local release of drug into the tumor vasculature and resulting high drug concentration can alter vascular transport rate constants along with having direct tumoricidal effects...
April 7, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28395216/synthetic-approaches-to-radiochemical-probes-for-imaging-of-bacterial-infections
#20
REVIEW
Jyotibon Dutta, Tricia Naicker, Thomas Ebenhan, Hendrik G Kruger, Per I Arvidsson, Thavendran Govender
This present review provides an account on the available synthetic strategies employed to radiolabel commercial and potential bacteria-selective probes for tomographic imaging. These molecular probes encompass leukocytes, antibodies, small molecules, peptides, antibiotics, macrolides, vitamins, oligomers and siderophores. Although this technique has shown to be a valuable tool for non-invasive infection imaging, more development is required to create easy-to-radiolabel kit solutions/procedures for the preparation of the probes...
March 29, 2017: European Journal of Medicinal Chemistry
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