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https://www.readbyqxmd.com/read/29677513/nuclear-import-receptor-inhibits-phase-separation-of-fus-through-binding-to-multiple-sites
#1
Takuya Yoshizawa, Rustam Ali, Jenny Jiou, Ho Yee Joyce Fung, Kathleen A Burke, Seung Joong Kim, Yuan Lin, William B Peeples, Daniel Saltzberg, Michael Soniat, Jordan M Baumhardt, Rudolf Oldenbourg, Andrej Sali, Nicolas L Fawzi, Michael K Rosen, Yuh Min Chook
Liquid-liquid phase separation (LLPS) is believed to underlie formation of biomolecular condensates, cellular compartments that concentrate macromolecules without surrounding membranes. Physical mechanisms that control condensate formation/dissolution are poorly understood. The RNA-binding protein fused in sarcoma (FUS) undergoes LLPS in vitro and associates with condensates in cells. We show that the importin karyopherin-β2/transportin-1 inhibits LLPS of FUS. This activity depends on tight binding of karyopherin-β2 to the C-terminal proline-tyrosine nuclear localization signal (PY-NLS) of FUS...
April 19, 2018: Cell
https://www.readbyqxmd.com/read/29677450/complete-programmable-decoding-of-oxidized-5-methylcytosine-nucleobases-in-dna-by-chemoselective-blockage-of-universal-tale-binders
#2
Mario Giess, Anna Witte, Julia Jasper, Oliver Koch, Daniel Summerer
5-methylcytosine (5mC) and its oxidized derivatives are regulatory elements of mammalian genomes involved in development and disease. These nucleobases do not selectively modulate Watson-Crick pairing, preventing their programmable targeting and analysis by traditional hybridiza-tion probes. Transcription-activator-like effectors (TALEs) can be engineered for use as programmable probes with epi-genetic nucleobase selectivity. However, only partial selectivi-ties for oxidized 5mC have been achieved so far, preventing unambiguous target binding...
April 20, 2018: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/29677442/synthesis-and-pharmacological-evaluation-of-novel-c-8-substituted-tetrahydroquinolines-as-balanced-affinity-mu-delta-opioid-ligands-for-the-treatment-of-pain
#3
Anthony F Nastase, Nicholas W Griggs, Jessica P Anand, Thomas J Fernandez, Aubrie A Harland, Tyler J Trask, Emily M Jutkiewicz, John R Traynor, Henry I Mosberg
The use of opioids for the treatment of pain, while largely effective, is limited by detrimental side effects including analgesic tolerance, physical dependence, and euphoria, which may lead to opioid abuse. Studies have shown that compounds with a -opioid receptor (MOR) agonist/-opioid receptor (DOR) antagonist profile reduce or eliminate some of these side effects including development of tolerance and dependence. Herein we report the synthesis and pharmacological evaluation of a series of tetrahydroquinoline-based peptidomimetics with substitutions at the C-8 position...
April 20, 2018: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29676918/template-assisted-proximity-for-oligomerization-of-fullerenes
#4
Kum-Yi Cheng, Shern-Long Lee, Ting-Yang Kuo, Chih-Hsun Lin, Yen-Chen Chen, Ting-Hao Kuo, Cheng-Chih Hsu, Chun-Hsien Chen
Demonstrated herein is an unprecedented porous template-assisted reaction at the solid-liquid interface involving bond formation, which is typically collision-driven and occurs in the solution and gas phases. The template is a TMA (trimesic acid) monolayer with two-dimensional pores that host fullerenes, which otherwise exhibit an insignificant affinity to an undecorated graphite substrate. The confinement of C84 units in the TMA pores formulates a proximity that is ideal for bond formation. The oligomerization of C84 is triggered by an electric pulse via an STM (scanning tunneling microscope) tip...
April 20, 2018: Langmuir: the ACS Journal of Surfaces and Colloids
https://www.readbyqxmd.com/read/29676864/bioequivalence-of-canakinumab-injected-subcutaneously-via-an-autoinjector-device-or-a-prefilled-safety-syringe-device-in-healthy-subjects
#5
SivaNaga S Anumolu, Sam Lindgren, Janardhana Vemula, David Floch, Christine Reynolds, Hans-Joachim Wallny, Haiying Sun
Canakinumab, a high-affinity human anti-interleukin-1β monoclonal antibody, is being used for the treatment of a broad spectrum of inflammatory diseases. This phase 1 study compared the relative bioavailability of a single dose of subcutaneous canakinumab either self-administered with an autoinjector (AI) or administered by a health care professional (HCP) with a prefilled safety syringe (SS) in healthy subjects. The study enrolled 80 subjects randomized 1:1 to receive 150 mg/mL of a liquid formulation of canakinumab via an AI or SS into either the thigh or abdomen...
April 20, 2018: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/29676768/exposure-of-bacillus-subtilis-to-silver-inhibits-activity-of-cytochrome-c-oxidase-in-vivo-via-interaction-with-sco-the-cu-a-assembly-protein
#6
Shina Hussain, Diann Andrews, Bruce C Hill
Silver has long been used as an antimicrobial agent in general and medicinal use. Here, we observe that exposure of the Gram-positive, endospore-forming bacterium Bacillus subtilis to Ag(i) effects growth in a biphasic manner. In the first phase at Ag(i) concentrations below 50 μM B. subtilis growth is not affected, but activity of the respiratory enzyme cytochrome c oxidase is disrupted completely. Between 50 to 100 μM Ag(i) B. subtilis growth is drastically diminished and completely absent above 100 μM Ag(i)...
April 20, 2018: Metallomics: Integrated Biometal Science
https://www.readbyqxmd.com/read/29676749/removal-of-catechol-from-water-by-modified-dolomite-performance-spectroscopy-and-mechanism
#7
Aouda Khalfa, Senia Mellouk, Kheira Marouf-Khelifa, Amine Khelifa
Dolomite was treated at 800 °C (D800), characterized, and used in the adsorptive removal of catechol (1,2-dihydroxybenzene) from aqueous solutions. The performances of the D800 sample, named dolomitic solid, were compared with those of the raw material. A bibliographic review shows that the data on the adsorption of phenolic compounds by dolomites are non-existent. Kinetic data, equilibrium isotherms, thermodynamic parameters, and pH influence were reported. Special attention was paid to the spectroscopic study, before and after adsorption...
April 2018: Water Science and Technology: a Journal of the International Association on Water Pollution Research
https://www.readbyqxmd.com/read/29676660/new-tailored-substituted%C3%A2-benzothiazole-schiff-base-cu-ii-zn-ii-antitumor-drug-entities-effect-of-substituents-on-dna-binding-profile-antimicrobial-and-cytotoxic-activity
#8
Siffeen Zehra, Mohammad Shavez Khan, Iqbal Ahmad, Farukh Arjmand
New tailored Cu(II) & Zn(II) metal-based antitumor drug entities were synthesized from substituted benzothiazole o‒vanillin Schiff base ligands. The complexes were thoroughly characterized by elemental analysis, spectroscopic studies {IR, 1 H & 13 C NMR, ESI-MS, EPR} and magnetic susceptibility measurements. The structure activity relationship (SAR) studies of benzothiazole Cu(II) & Zn(II) complexes having molecular formulas [C30 H22 CuN5 O7 S2 ], [C30 H20 Cl2 CuN5 O7 S2 ], [C30 H20 CuF2 N5 O7 S2 ], [C30 H22 N4 O4 S2 Zn], [C30 H20 Cl2 N4 O4 S2 Zn] and [C30 H20 F2 N5 O7 S2 Zn], with CT‒DNA were performed by employing absorption, emission titrations and hydrodynamic measurements...
April 20, 2018: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/29676593/icos-costimulation-differentially-affects-t-cells-in-secondary-lymphoid-organs-and-inflamed-tissues
#9
Dana Vu Van, Laura Bauer, Richard A Kroczek, Andreas Hutloff
B cell interaction with follicular helper T cells and their subsequent differentiation into high-affinity antibody producing cells normally takes place in secondary lymphoid organs. The costimulator ICOS plays a key role in this process and is therefore considered as an attractive target to modulate exaggerated B cell responses in autoimmune or allergic diseases. Inflamed tissues were recently recognized as additional sites of active T cell/B cell interaction. To analyze whether ICOS costimulation is also important there, we employed a mouse airway inflammation model which allows to directly compare immune reactions in the lung-draining lymph node and the lung tissue and also to assess the relative importance of dendritic cells versus B cells as antigen-presenting cells...
April 20, 2018: American Journal of Respiratory Cell and Molecular Biology
https://www.readbyqxmd.com/read/29676519/development-of-machine-learning-models-to-predict-inhibition-of-3-dehydroquinate-dehydratase
#10
Maurício Boff de Ávila, Walter Filgueira de Azevedo
In the present study, we describe the development of new machine learning models to predict inhibition of the enzyme 3-dehydroquinate dehydratase (DHQD). This enzyme is the third step of the shikimate pathway and is responsible for the synthesis of chorismate, which is a natural precursor of aromatic amino acids The enzymes of shikimate pathway are absent in humans, which make them protein targets for the design of antimicrobial drugs. We focus our study on the crystallographic structures of DHQD in complex with competitive inhibitors, for which experimental inhibition constant data is available...
April 20, 2018: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/29676228/glaucoma-pathogenesis-and-neurotrophins-focus-on-the-molecular-and-genetic-basis-for-therapeutic-prospects
#11
Nitin Chitranshi, Yogita Dheer, Mojdeh Abbasi, Yuyi You, Stuart L Graham, Vivek Gupta
BACKGROUND: Retinal ganglion cell (RGC) degeneration is a major feature of glaucoma pathology. Neuroprotective approaches that delay or halt the progression of RGC loss are needed to prevent vision loss which can occur even after conventional medical or surgical treatments to lower intraocular pressure. OBJECTIVE: The aim of this review was to examine the progress in genetics and cellular mechanisms associated with endoplasmic reticulum (ER) stress, RGC dysfunction and cell death pathways in glaucoma...
April 19, 2018: Current Neuropharmacology
https://www.readbyqxmd.com/read/29676214/homozygous-mutation-in-human-serum-albumin-and-its-implication-on-thyroid-tests
#12
Mizuho S Mimoto, Anara Karaca, Neal Scherberg, Alexandra M Dumitrescu, Samuel Refetoff
An individual with familial dysalbuminemic hyperthyroxinemia (FDH) due to a homozygous mutation (c.653G>A, p.R218H) in the human serum albumin (HSA) gene is reported. The patient was identified during evaluation of abnormal thyroid tests in a large family with multiple levels of consanguinity. He showed a greater increase in total T4 relative to that observed in heterozygous family members. The higher affinity of mutant HSA for T4, together with the large molar excess of HSA relative to thyroid hormones in serum, results in preferential association of T4 with the mutant rather than wildtype HSA in heterozygous individuals...
April 20, 2018: Thyroid: Official Journal of the American Thyroid Association
https://www.readbyqxmd.com/read/29675916/serum-apoa4-levels-predicted-the-progression-of-renal-impairment-in-t2dm
#13
Chao-Wen Cheng, Che-Chang Chang, Hsiu-Wen Chen, Ching-Yu Lin, Jin-Shuen Chen
BACKGROUND: Among multiple causes, diabetic nephropathy (DN) is the major underlying renal disease that leads to end-stage renal disease (ESRD), and early diagnosis can effectively prevent or delay the progression to ESRD. Therefore, the current study aimed to develop non-invasive, accurate detection markers. MATERIALS & METHODS: For this study, 62 diabetes mellitus (DM) patients, 59 DN patients, and 21 healthy controls (HCs) were recruited. All participants' serum samples were subjected to concavanalin (Con) A affinity chromatography, which utilizes glycoproteins to discover potential markers...
April 19, 2018: European Journal of Clinical Investigation
https://www.readbyqxmd.com/read/29675746/cabazitaxel-is-more-active-than-first-generation-taxanes-in-abcb1-cell-lines-due-to-its-reduced-affinity-for-p-glycoprotein
#14
George E Duran, Volker Derdau, Dietmar Weitz, Nicolas Philippe, Jörg Blankenstein, Jens Atzrodt, Dorothée Sémiond, Diego A Gianolio, Sandrine Macé, Branimir I Sikic
PURPOSE: The primary aim of this study was to determine cabazitaxel's affinity for the ABCB1/P-glycoprotein (P-gp) transporter compared to first-generation taxanes. METHODS: We determined the kinetics of drug accumulation and retention using [14 C]-labeled taxanes in multidrug-resistant (MDR) cells. In addition, membrane-enriched fractions isolated from doxorubicin-selected MES-SA/Dx5 cells were used to determine sodium orthovanadate-sensitive ATPase stimulation after exposure to taxanes...
April 19, 2018: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/29675707/a-rapid-solution-based-method-for-determining-the-affinity-of-heroin-hapten-induced-antibodies-to-heroin-its-metabolites-and-other-opioids
#15
Oscar B Torres, Alexander J Duval, Agnieszka Sulima, Joshua F G Antoline, Arthur E Jacobson, Kenner C Rice, Carl R Alving, Gary R Matyas
We describe for the first time a method that utilizes microscale thermophoresis (MST) technology to determine polyclonal antibody affinities to small molecules. Using a novel type of heterologous MST, we have accurately measured a solution-based binding affinity of serum antibodies to heroin which was previously impossible with other currently available methods. Moreover, this mismatch approach (i.e., using a cross-reactive hapten tracer) has never been reported in the literature. When compared with equilibrium dialysis combined with ultra-performance liquid chromatography/tandem mass spectrometry (ED-UPLC/MS/MS), this novel MST method yields similar binding affinity values for polyclonal antibodies to the major heroin metabolites 6-AM and morphine...
April 19, 2018: Analytical and Bioanalytical Chemistry
https://www.readbyqxmd.com/read/29675559/truncated-aptamers-for-total-and-glycated-hemoglobin-and-their-integration-into-a-graphene-oxide-based-fluorometric-method-for-high-throughput-screening-for-diabetes
#16
Abrar Yousef Almusharraf, Shimaa Eissa, Mohammed Zourob
The authors describe the identification of an effective binding region of aptamers against glycated (HbA1c) and total haemoglobin (tHb) by using a fluorometric assay. Truncation of the originally selected aptamers from 60 to 46 and 34 nucleotides for HbA1c and tHb, respectively, enhances the affinity for their targets. Moreover, shortening the aptamer sequences leads to a better conformational change after target binding which enabled the integration of the aptamers in a graphene oxide (GO)-based fluorometric assay...
April 19, 2018: Mikrochimica Acta
https://www.readbyqxmd.com/read/29675532/stereodivergent-synthesis-of-5-aminopipecolic-acids-and-application-in-the-preparation-of-a-cyclic-rgd-peptidomimetic-as-a-nanomolar-%C3%AE-v-%C3%AE-3-integrin-ligand
#17
Lorenzo Sernissi, Luciano Ricci, Dina Scarpi, Francesca Bianchini, Daniela Arosio, Alessandro Contini, Ernesto G Occhiato
A stereodivergent strategy was devised to obtain enantiopure cis and trans 5-aminopipecolic acids (5-APAs) in suitably protected forms to be employed in peptide synthesis as conformationally constrained α- and δ-amino acids. The cis isomer was used as a δ-amino acid to construct a cyclic RGD-containing peptidomimetic, the ability of which to compete with biotinylated vitronectin for binding with the isolated αVβ3 integrin was measured (IC50 = 4.2 ± 0.9 nM). A complete 1H NMR and computational conformational analysis was performed to elucidate the reasons for the high affinity of this cyclic peptidomimetic in comparison with cilengitide...
April 20, 2018: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/29675356/-in-vivo-fluorescence-imaging-of-hepatocellular-carcinoma-using-a-novel-gpc3-specific-aptamer-probe
#18
Menglong Zhao, Lili Dong, Zhuang Liu, Shuohui Yang, Weizhong Wu, Jiang Lin
Background: Glypican-3 (GPC3) is highly expressed in most of the hepatocellular carcinomas (HCCs), even in small HCCs. It may be used as a potential biomarker for early detection of HCC. The aptamer is a promising targeting agent with unique advantages over antibody. This study was to introduce a novel GPC3 specific aptamer (AP613-1), to verify its specific binding property in vitro , and to evaluate its targeting efficiency in vivo by performing near-infrared (NIR) fluorescence imaging on an HCC xenograft model...
March 2018: Quantitative Imaging in Medicine and Surgery
https://www.readbyqxmd.com/read/29675232/diselenolane-mediated-cellular-uptake
#19
Nicolas Chuard, Amalia I Poblador-Bahamonde, Lili Zong, Eline Bartolami, Jana Hildebrandt, Wolfgang Weigand, Naomi Sakai, Stefan Matile
The emerging power of thiol-mediated uptake with strained disulfides called for a move from sulfur to selenium. We report that according to results with fluorescent model substrates, cellular uptake with 1,2-diselenolanes exceeds uptake with 1,2-dithiolanes and epidithiodiketopiperazines with regard to efficiency as well as intracellular localization. The diselenide analog of lipoic acid performs best. This 1,2-diselenolane delivers fluorophores efficiently to the cytosol of HeLa Kyoto cells, without detectable endosomal capture as with 1,2-dithiolanes or dominant escape into the nucleus as with epidithiodiketopiperazines...
February 21, 2018: Chemical Science
https://www.readbyqxmd.com/read/29675184/high-affinity-and-selective-detection-of-pyrophosphate-in-water-by-a-resorcinarene-salt-receptor
#20
Ngong Kodiah Beyeh, Isabel Díez, S Maryamdokht Taimoory, Daniel Meister, Andrew I Feig, John F Trant, Robin H A Ras, Kari Rissanen
Pyrophosphate (PPi) is a byproduct of DNA and RNA synthesis, and abnormal levels are indicative of disease. We report the high-affinity binding of PPi in water by N -alkyl ammonium resorcinarene chloride receptors. Experimental analysis using 1 H and 31 P NMR, isothermal titration calorimetry, mass spectrometry, and UV-vis spectroscopy all support exceptional selectivity of these systems for PPi in water. The measured affinity of K 1 = 1.60 × 107 M-1 for PPi is three orders of magnitude larger than that observed for binding to another phosphate, ATP...
February 7, 2018: Chemical Science
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