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MicroScale Thermophoresis

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https://www.readbyqxmd.com/read/28300592/new-peptide-inhibitors-modulate-the-self-assembly-of-islet-amyloid-polypeptide-residues-11-20-in-vitro
#1
Yexuan Mao, Lanlan Yu, Ran Yang, Chuanguo Ma, Lingbo Qu, Peter de B Harrington
The structural transition and misfolding of human islet amyloid polypeptide may cause a common metabolic disease Type 2 diabetes mellitus. Seventeen peptides have been synthesized, possessing different lengths, compositions, and peptide conformation. In this study, the mechanism of these peptides on inhibiting the formation of hIAPP11-20 amyloid fibrils was investigated using a conventional ThT fluorescence assay and microscale thermophoresis. The results showed that short peptides AT, SA, RF, KS, KT and KN, and cyclic peptides cyclic-KS, cyclic-KT and cyclic-KN displayed considerable inhibitory effect on hIAPP11-20 fibril formation and a strong affinity for hIAPP11-20...
March 11, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28273560/overcoming-drug-resistance-by-cell-penetrating-peptide-mediated-delivery-of-a-doxorubicin-dimer-with-high-dna-binding-affinity
#2
Marco Lelle, Christoph Freidel, Stefka Kaloyanova, Ilja Tabujew, Alexander Schramm, Michael Musheev, Christof Niehrs, Klaus Müllen, Kalina Peneva
We describe the synthesis and characterization of a novel bioconjugate, consisting of an octaarginine cell-penetrating peptide and a highly DNA-affine doxorubicin dimer. The linkage between the two components is composed of a cleavable disulfide bond, which enables the efficient intracellular delivery of the cytotoxic payload within the reductive environment of the cytosol, mediated through glutathione. To determine the DNA-binding affinity of the dimeric drug molecule, microscale thermophoresis was applied...
April 21, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28273138/itc-derived-binding-affinity-may-be-biased-due-to-titrant-nano-aggregation-binding-of-halogenated-benzotriazoles-to-the-catalytic-domain-of-human-protein-kinase-ck2
#3
Maria Winiewska, Ewa Bugajska, Jarosław Poznański
The binding of four bromobenzotriazoles to the catalytic subunit of human protein kinase CK2 was assessed by two complementary methods: Microscale Thermophoresis (MST) and Isothermal Titration Calorimetry (ITC). New algorithm proposed for the global analysis of MST pseudo-titration data enabled reliable determination of binding affinities for two distinct sites, a relatively strong one with the Kd of the order of 100 nM and a substantially weaker one (Kd > 1 μM). The affinities for the strong binding site determined for the same protein-ligand systems using ITC were in most cases approximately 10-fold underestimated...
2017: PloS One
https://www.readbyqxmd.com/read/28265093/common-coding-variant-in-serpina1-increases-the-risk-for-large-artery-stroke
#4
Rainer Malik, Therese Dau, Maria Gonik, Anirudh Sivakumar, Daniel J Deredge, Evgeniia V Edeleva, Jessica Götzfried, Sander W van der Laan, Gerard Pasterkamp, Nathalie Beaufort, Susana Seixas, Steve Bevan, Lisa F Lincz, Elizabeth G Holliday, Annette I Burgess, Kristiina Rannikmäe, Jens Minnerup, Jennifer Kriebel, Melanie Waldenberger, Martina Müller-Nurasyid, Peter Lichtner, Danish Saleheen, Peter M Rothwell, Christopher Levi, John Attia, Cathie L M Sudlow, Dieter Braun, Hugh S Markus, Patrick L Wintrode, Klaus Berger, Dieter E Jenne, Martin Dichgans
Large artery atherosclerotic stroke (LAS) shows substantial heritability not explained by previous genome-wide association studies. Here, we explore the role of coding variation in LAS by analyzing variants on the HumanExome BeadChip in a total of 3,127 cases and 9,778 controls from Europe, Australia, and South Asia. We report on a nonsynonymous single-nucleotide variant in serpin family A member 1 (SERPINA1) encoding alpha-1 antitrypsin [AAT; p.V213A; P = 5.99E-9, odds ratio (OR) = 1.22] and confirm histone deacetylase 9 (HDAC9) as a major risk gene for LAS with an association in the 3'-UTR (rs2023938; P = 7...
March 6, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28261854/oligog-cf-5-20-normalizes-cystic-fibrosis-mucus-by-chelating-calcium
#5
Anna Ermund, Christian V Recktenwald, Gudmund Skjåk-Braek, Lauren N Meiss, Edvar Onsøyen, Philip D Rye, Arne Dessen, Astrid Hilde Myrset, Gunnar C Hansson
The goal of this study was to determine whether the guluronate (G) rich alginate OligoG CF-5/20 (OligoG) could detach cystic fibrosis (CF) mucus by calcium chelation, which is also required for normal mucin unfolding. Since bicarbonate secretion is impaired in CF, leading to insufficient mucin unfolding and thereby attached mucus and since bicarbonate has the ability to bind calcium, we hypothesized that the calcium chelating property of OligoG would lead to detachment of CF mucus. Indeed, OligoG could compete with the N-terminus of the MUC2 mucin for calcium binding as shown by microscale thermophoresis...
March 6, 2017: Clinical and Experimental Pharmacology & Physiology
https://www.readbyqxmd.com/read/28252952/new-iminodiacetate-thiosemicarbazone-hybrids-and-their-copper-ii-complexes-are-potential-ribonucleotide-reductase-r2-inhibitors-with-high-antiproliferative-activity
#6
Mirela F Zaltariov, Marta Hammerstad, Homayon J Arabshahi, Katarina Jovanović, Klaus W Richter, Maria Cazacu, Sergiu Shova, Mihaela Balan, Niels H Andersen, Siniša Radulović, Jóhannes Reynisson, K Kristoffer Andersson, Vladimir B Arion
As ribonucleotide reductase (RNR) plays a crucial role in nucleic acid metabolism, it is an important target for anticancer therapy. The thiosemicarbazone Triapine is an efficient R2 inhibitor, which has entered ∼20 clinical trials. Thiosemicarbazones are supposed to exert their biological effects through effectively binding transition-metal ions. In this study, six iminodiacetate-thiosemicarbazones able to form transition-metal complexes, as well as six dicopper(II) complexes, were synthesized and fully characterized by analytical, spectroscopic techniques (IR, UV-vis; (1)H and (13)C NMR), electrospray ionization mass spectrometry, and X-ray diffraction...
March 2, 2017: Inorganic Chemistry
https://www.readbyqxmd.com/read/28220417/steady-state-and-kinetics-based-affinity-determination-in-effector-effector-target-interactions
#7
André Reinhard, Thorsten Nürnberger
Dissecting the functional basis of pathogenicity and resistance in the context of plant innate immunity benefits greatly from detailed knowledge about biomolecular interactions, as both resistance and virulence depend on specific interactions between pathogen and host biomolecules. While in vivo systems provide biological context to host-pathogen interactions, these experiments typically cannot provide quantitative biochemical characterization of biomolecular interactions. However, in many cases, the biological function does not only depend on whether an interaction occurs at all, but rather on the "intensity" of the interaction, as quantified by affinity...
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/28117825/mapping-the-binding-site-of-an-aptamer-on-atp-using-microscale-thermophoresis
#8
Clemens Entzian, Thomas Schubert
Characterization of molecular interactions in terms of basic binding parameters such as binding affinity, stoichiometry, and thermodynamics is an essential step in basic and applied science. MicroScale Thermophoresis (MST) is a sensitive biophysical method to obtain this important information. Relying on a physical effect called thermophoresis, which describes the movement of molecules through temperature gradients, this technology allows for the fast and precise determination of binding parameters in solution and allows the free choice of buffer conditions (from buffer to lysates/sera)...
January 7, 2017: Journal of Visualized Experiments: JoVE
https://www.readbyqxmd.com/read/28112513/novel-beta-tubulin-immobilized-nanoparticles-affinity-material-for-screening-%C3%AE-tubulin-inhibitors-from-a-complex-mixture
#9
Qing-Shan Liu, Ran Deng, Qing-Fang Yan, Lin Cheng, Yongming Luo, Keqin Li, Xiaoying Yin, Xiaoyan Qin
In order to efficiently screen and isolate β-tubulin inhibitors, β-tubulin was immobilized on core-shell PMMA/CS (poly(methyl methacrylate)/Chitosan) nanoparticles to produce a new type of immobilized affinity material named β-tubulin-immobilized nanoparticles (β-TIN). The selectivity and adsorption performance of β-TIN were characterized using various control drugs. The β-TIN, the paclitaxel molecularly imprinted ploymers (MIP), and the C18 adsorbing material were compared for selectivity and enrichment ratio...
February 22, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28110167/chiral-separation-of-new-sulfonamide-derivatives-and-evaluation-of-their-enantioselective-affinity-for-human-carbonic-anhydrase-ii-by-microscale-thermophoresis-and-surface-plasmon-resonance
#10
Tiphaine Rogez-Florent, Catherine Foulon, Anne-Sophie Drucbert, Nadège Schifano, Perrine Six, Stéphanie Devassine, Patrick Depreux, Pierre-Marie Danzé, Laurence Goossens, Cécile Danel, Jean-François Goossens
The aim of this study was to develop a method combining chiral separation and biophysical techniques to evaluate the enantioselective affinity of original sulfonamide derivatives towards their therapeutic target, the human carbonic anhydrase II (hACII). The first step consisted in the preparation of the enantiomers by chromatographic separation. The performances of HPLC and Supercritical Fluid Chromatography (SFC) were studied at the analytical scale by optimization of various experimental conditions using adsorbed polysaccharide chiral stationary phases (amylose AD-H and cellulose OD-H)...
January 9, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28067769/identification-of-a-potent-allosteric-inhibitor-of-human-protein-kinase-ck2-by-bacterial-surface-display-library-screening
#11
Christian Nienberg, Claudia Garmann, Andreas Gratz, Andre Bollacke, Claudia Götz, Joachim Jose
Human protein kinase CK2 has emerged as promising target for the treatment of neoplastic diseases. The vast majority of kinase inhibitors known today target the ATP binding site, which is highly conserved among kinases and hence leads to limited selectivity. In order to identify non-ATP competitive inhibitors, a 12-mer peptide library of 6 × 10⁵ variants was displayed on the surface of E. coli by autodisplay. Screening of this peptide library on variants with affinity to CK2 was performed by fluorophore-conjugated CK2 and subsequent flow cytometry...
January 5, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28067010/hit-validation-methodologies-for-ligands-isolated-from-dna-encoded-chemical-libraries
#12
Gunther Zimmermann, Yizhou Li, Ulrike Rieder, Martin Mattarella, Dario Neri, Jörg Scheuermann
DNA-encoded chemical libraries (DECLs) are large collections of compounds linked to DNA fragments, serving as amplifiable barcodes, which can be screened on target proteins of interest. In typical DECL selections, preferential binders are identified by high-throughput DNA sequencing, comparing their frequency before and after the affinity capture step. Hits identified in this procedure need to be confirmed, by resynthesis and by performing affinity measurements. In this article, we present novel methods, based on the hybridization of oligonucleotide conjugates with fluorescently-labeled complementary oligonucleotides, which facilitate the determination of affinity constants and kinetic dissociation constants...
January 9, 2017: Chembiochem: a European Journal of Chemical Biology
https://www.readbyqxmd.com/read/27993133/synthesis-and-functionalization-of-protease-activated-nanoparticles-with-tissue-plasminogen-activator-peptides-as-targeting-moiety-and-diagnostic-tool-for-pancreatic-cancer
#13
Sophie Dobiasch, Szilard Szanyi, Aleko Kjaev, Jens Werner, Albert Strauss, Christian Weis, Lars Grenacher, Katya Kapilov-Buchman, Liron-Limor Israel, Jean-Paul Lellouche, Erica Locatelli, Mauro Comes Franchini, Jennifer Vandooren, Ghislain Opdenakker, Klaus Felix
BACKGROUND: Functionalized nanoparticles (NPs) are one promising tool for detecting specific molecular targets and combine molecular biology and nanotechnology aiming at modern imaging. We aimed at ligand-directed delivery with a suitable target-biomarker to detect early pancreatic ductal adenocarcinoma (PDAC). Promising targets are galectins (Gal), due to their strong expression in and on PDAC-cells and occurrence at early stages in cancer precursor lesions, but not in adjacent normal tissues...
December 19, 2016: Journal of Nanobiotechnology
https://www.readbyqxmd.com/read/27943531/identification-of-core-subunits-of-photosystem%C3%A2-ii-as-action-sites-of-hsp21-which-is-activated-by-the-gun5-mediated-retrograde-pathway-in-arabidopsis
#14
Si-Ting Chen, Ning-Yu He, Juan-Hua Chen, Fang-Qing Guo
Photosystem II (PSII) is the most thermolabile photosynthetic complex. Physiological evidence suggests that the small chloroplast heat-shock protein 21 (HSP21) is involved in plant thermotolerance, but the molecular mechanism of its action remains largely unknown. Here, we have provided genetic and biochemical evidence that HSP21 is activated by the GUN5-dependent retrograde signaling pathway, and stabilizes PSII by directly binding to its core subunits such as D1 and D2 proteins under heat stress. We further demonstrate that the constitutive expression of HSP21 sufficiently rescues the thermosensitive stability of PSII and survival defects of the gun5 mutant with dramatically improving granal stacking under heat stress, indicating that HSP21 is a key chaperone protein in maintaining the integrity of the thylakoid membrane system under heat stress...
December 10, 2016: Plant Journal: for Cell and Molecular Biology
https://www.readbyqxmd.com/read/27941022/basic-residues-of-%C3%AE-sheet-a-contribute-to-heparin-binding-and-activation-of-vaspin-serpin-a12
#15
David Ulbricht, Kathrin Oertwig, Kristin Arnsburg, Anja Saalbach, Jan Pippel, Norbert Sträter, John T Heiker
Many members of the serine protease inhibitor (serpin) family are activated by glycosaminoglycans (GAGs). Visceral adipose tissue-derived serpin (vaspin), serpin A12 of the serpin family, and its target protease kallikrein 7 (KLK7) are heparin-binding proteins, and inhibition of KLK7 by vaspin is accelerated by heparin. However, the nature of GAG binding to vaspin is not known. Here, we measured vaspin binding of various glycosaminoglycans and low molecular weight heparins by microscale thermophoresis and analyzed acceleration of protease inhibition by these molecules...
January 20, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/27763725/targeting-epha2-sam-and-its-interactome-design-and-evaluation-of-helical-peptides-enriched-in-charged-residues
#16
Flavia A Mercurio, Daniela Marasco, Concetta Di Natale, Luciano Pirone, Susan Costantini, Emilia M Pedone, Marilisa Leone
The EphA2 receptor controls diverse physiological and pathological conditions and its levels are often upregulated in cancer. Targeting receptor overexpression, through modulation of endocytosis and consequent degradation, appears to be an appealing strategy for attacking tumor malignancy. In this scenario, the Sam domain of EphA2 plays a pivotal role because it is the site where protein regulators of endocytosis and stability are recruited by means of heterotypic Sam-Sam interactions. Because EphA2-Sam heterotypic complexes are largely based on electrostatic contacts, we have investigated the possibility of attacking these interactions with helical peptides enriched in charged residues...
October 20, 2016: Chembiochem: a European Journal of Chemical Biology
https://www.readbyqxmd.com/read/27746356/binding-interactions-between-enantiomeric-%C3%AE-aminophosphonate-derivatives-and-tobacco-mosaic-virus-coat-protein
#17
Weiying Zhang, Xiangyang Li, Guoping Zhang, Yan Ding, Longlu Ran, Liangzhi Luo, Jian Wu, Deyu Hu, Baoan Song
Tobacco mosaic virus (TMV) is an important plant virus that can cause considerable crop loss. Our group synthesized a series of enantiomeric α-aminophosphonate derivatives with high anti-TMV activities. The activity of (R)-diphenyl-1-(4-methylbenzothiazole-2-amino)-1-(thiphene-2-yl)-methylphosphonate (Q-R) was found to be superior to that of (S)-diphenyl-1-(4-methyl benzothiazole-2-amino)-1-(thiphene-2-yl)-methylphosphonate (Q-S). However, the mechanism for inhibition of the R-isomer (Q-R) of infection activity is not clear...
January 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/27739542/quantitative-analysis-of-protease-recognition-by-inhibitors-in-plasma-using-microscale-thermophoresis
#18
T Dau, E V Edeleva, S A I Seidel, R A Stockley, D Braun, D E Jenne
High abundance proteins like protease inhibitors of plasma display a multitude of interactions in natural environments. Quantitative analysis of such interactions in vivo is essential to study diseases, but have not been forthcoming, as most methods cannot be directly applied in a complex biological environment. Here, we report a quantitative microscale thermophoresis assay capable of deciphering functional deviations from in vitro inhibition data by combining concentration and affinity measurements. We obtained stable measurement signals for the substrate-like interaction of the disease relevant inhibitor α-1-antitrypsin (AAT) Z-variant with catalytically inactive elastase...
October 14, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27717713/biophysical-approaches-promote-advances-in-the-understanding-of-von-willebrand-factor-processing-and-function
#19
REVIEW
Achim Löf, Jochen P Müller, Martin Benoit, Maria A Brehm
The large multimeric plasma glycoprotein von Willebrand factor (VWF) is essential for primary hemostasis by recruiting platelets to sites of vascular injury. VWF multimers respond to elevated hydrodynamic forces by elongation, thereby increasing their adhesiveness to platelets. Thus, the activation of VWF is force-induced, as is its inactivation. Due to these attributes, VWF is a highly interesting system from a biophysical point of view, and is well suited for investigation using biophysical approaches. Here, we give an overview on recent studies that predominantly employed biophysical methods to gain novel insights into multiple aspects of VWF: Electron microscopy was used to shed light on the domain structure of VWF and the mechanism of VWF secretion...
September 28, 2016: Advances in Biological Regulation
https://www.readbyqxmd.com/read/27681596/small-molecule-inhibition-of-the-ubiquitin-specific-protease-usp2-accelerates-cyclin-d1-degradation-and-leads-to-cell-cycle-arrest-in-colorectal-cancer-and-mantle-cell-lymphoma-models
#20
Mindy I Davis, Rajan Pragani, Jennifer T Fox, Min Shen, Kalindi Parmar, Emily F Gaudiano, Li Liu, Cordelle Tanega, Lauren McGee, Matthew D Hall, Crystal McKnight, Paul Shinn, Henrike Nelson, Debasish Chattopadhyay, Alan D D'Andrea, Douglas S Auld, Larry J DeLucas, Zhuyin Li, Matthew B Boxer, Anton Simeonov
Deubiquitinases are important components of the protein degradation regulatory network. We report the discovery of ML364, a small molecule inhibitor of the deubiquitinase USP2 and its use to interrogate the biology of USP2 and its putative substrate cyclin D1. ML364 has an IC50 of 1.1 μm in a biochemical assay using an internally quenched fluorescent di-ubiquitin substrate. Direct binding of ML364 to USP2 was demonstrated using microscale thermophoresis. ML364 induced an increase in cellular cyclin D1 degradation and caused cell cycle arrest as shown in Western blottings and flow cytometry assays utilizing both Mino and HCT116 cancer cell lines...
November 18, 2016: Journal of Biological Chemistry
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