keyword
MENU ▼
Read by QxMD icon Read
search

MicroScale Thermophoresis

keyword
https://www.readbyqxmd.com/read/28522394/interaction-research-on-an-antiviral-molecule-that-targets-the-coat-protein-of-southern-rice-black-streaked-dwarf-virus
#1
Longlu Ran, Yan Ding, Liangzhi Luo, Xiuhai Gan, Xiangyang Li, Yongzhong Chen, Deyu Hu, Baoan Song
Southern rice black-streaked dwarf virus (SRBSDV) coat protein (P10) is the key protein required for viral transmission and host plant infection and is thus a promising target for anti-SRBSDV agent screening. In this study, P10 was obtained from Escherichia coli through cloning, expression, and purification. The antiviral agent Ningnanmycin was selected as control, and a series of antiviral compounds based on the structural scaffold of ferulic acid were analyzed. Size-exclusion chromatography analysis results showed that compound F27 can alter the aggregation of P10 proteins...
May 15, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28499498/aptatope-mapping-of-the-binding-site-of-a-progesterone-aptamer-on-the-steroid-ring-structure
#2
Vasso Skouridou, Thomas Schubert, Abdulaziz S Bashammakh, Mohammad S El-Shahawi, Abdulrahman O Alyoubi, Ciara K O'Sullivan
In this work we report the mapping of the binding site of the only progesterone aptamer published to date, in an approach referred to as aptatope mapping. By linking the binding data obtained from microscale thermophoresis analysis to the structural differences on the ring structure of a range of steroids, we elucidated the moieties involved in aptamer-progesterone binding. This approach can be further exploited for the characterization of aptamer specificity and ultimately facilitate the development of aptamer-based assays depending on the desired specificity...
May 10, 2017: Analytical Biochemistry
https://www.readbyqxmd.com/read/28459633/identification-of-human-ump-cmp-kinase-1-as-doxorubicin-binding-target-using-protein-microarray
#3
Shuxian Chen, Xu Wang, Xianghui Ye, Donghui Ma, Caiwei Chen, Junlong Cai, Yongfeng Fu, Xunjia Cheng, Yun Chen, Xiaohai Gong, Jian Jin
Doxorubicin (DOX) is a leading anthracycline drug with exceptional efficacy; however, little is known about the molecular mechanisms of its side effects, which include heart muscle damage, noncancerous cell death, and drug resistance. A total of 17,950 human proteins expressed in HEK293 cells were screened and yielded 14 hits. Competitive and binding experiments further verified the binding of DOX to UMP/CMP kinase 1 (CMPK1), and microscale thermophoresis showed that DOX binds to CMPK1 with a Kd of 1216 nM...
April 1, 2017: SLAS Discovery
https://www.readbyqxmd.com/read/28449373/biophysical-analysis-of-the-dynamics-of-calmodulin-interactions-with-neurogranin-and-ca2-calmodulin-dependent-kinase-ii
#4
Christian Seeger, Vladimir O Talibov, U Helena Danielson
Calmodulin (CaM) functions depend on interactions with CaM-binding proteins, regulated by Ca2+. Induced structural changes influence the affinity, kinetics, and specificities of the interactions. The dynamics of CaM interactions with neurogranin (Ng) and the CaM-binding region of Ca2+/calmodulin-dependent kinase II (CaMKII290-309 ) have been studied using biophysical methods. These proteins have opposite Ca2+ dependencies for CaM binding. Surface plasmon resonance biosensor analysis confirmed that Ca2+ and CaM interact very rapidly, and with moderate affinity ( KDSPR=3μM)...
April 27, 2017: Journal of Molecular Recognition: JMR
https://www.readbyqxmd.com/read/28449085/guanine-quadruplex-monoclonal-antibody-1h6-cross-reacts-with-restrained-thymidine-rich-single-stranded-dna
#5
Hinke G Kazemier, Katrin Paeschke, Peter M Lansdorp
Previously we reported the production and characterization of monoclonal antibody 1H6 raised against (T4G4)2 intermolecular guanine quadruplex (G4) DNA structures (Henderson A. et al. (2014) Nucleic Acids Res., 42, 860-869; Hoffmann R.F. et al. (2016) Nucleic Acids Res., 44, 152-163). It was shown that 1H6 strongly stains nuclei and has exquisite specificity for heterochromatin by immuno-electron microscopy. Here we extend our studies of 1H6 reactivity using enzyme-linked immunosorbent assay (ELISA) and microscale thermophoresis (MST)...
April 25, 2017: Nucleic Acids Research
https://www.readbyqxmd.com/read/28427443/benserazide-a-dopadecarboxylase-inhibitor-suppresses-tumor-growth-by-targeting-hexokinase-2
#6
Wei Li, Mengzhu Zheng, Shuangping Wu, Suyu Gao, Mei Yang, Zhimei Li, Qiuxia Min, Weiguang Sun, Lixia Chen, Guangya Xiang, Hua Li
BACKGROUND: Hexokinase (HK) is the rate-limiting enzyme in the first reaction of glycolysis. And Hexokinase 2 (HK2) is most closely related to malignant tumor which expresses at higher level compared with normal cells. HK2 plays a pivotal role in tumor initiation and maintenance, which provides a new target for cancer therapy. METHODS: Structure-based virtual ligand screening was used in hit identification from ZINC Drug Database. Microscale thermophoresis assay was performed to evaluate the binding affinity...
April 20, 2017: Journal of Experimental & Clinical Cancer Research: CR
https://www.readbyqxmd.com/read/28417365/quantifying-cbm-carbohydrate-interactions-using-microscale-thermophoresis
#7
Haiyang Wu, Cédric Y Montanier, Claire Dumon
MicroScale Thermophoresis (MST) is an emerging technology for studying a broad range of biomolecular interactions with high sensitivity. The affinity constant can be obtained for a wide range of molecules within minutes based on reactions in microliters. Here, we describe the application of MST in quantifying two CBM-carbohydrate interactions, a CBM3a toward cellulose nanocrystals and a CBM4 against xylohexaose.
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/28404919/paeonol-suppresses-solar-ultraviolet-induced-skin-inflammation-by-targeting-t-lak-cell-originated-protein-kinase
#8
Peipei Xue, Yong Wang, Fanfan Zeng, Ruijuan Xiu, Jingwen Chen, Jinguang Guo, Ping Yuan, Lin Liu, Juanjuan Xiao, Hui Lu, Dan Wu, Huaxiong Pan, Mingmin Lu, Feng Zhu, Fei Shi, Qiuhong Duan
Excessive exposure to solar UV (SUV) is related with numerous human skin disorders, such as skin inflammation, photoaging and carcinogenesis. T-LAK cell- originated protein kinase (TOPK), an upstream of p38 mitogen-activated protein kinase (p38) and c-Jun N-terminal kinases (JNKs), plays an important role in SUV -induced skin inflammation, and targeting TOPK has already been a strategy to prevent skin inflammation. In this study, we found that the expression of TOPK, phosphorylation of p38 or JNKs was increased in human solar dermatitis tissues...
April 18, 2017: Oncotarget
https://www.readbyqxmd.com/read/28344555/drug-repurposing-of-the-anthelmintic-niclosamide-to-treat-multidrug-resistant-leukemia
#9
Sami Hamdoun, Philipp Jung, Thomas Efferth
Multidrug resistance, a major problem that leads to failure of anticancer chemotherapy, requires the development of new drugs. Repurposing of established drugs is a promising approach for overcoming this problem. An example of such drugs is niclosamide, a known anthelmintic that is now known to be cytotoxic and cytostatic against cancer cells. In this study, niclosamide showed varying activity against different cancer cell lines. It revealed better activity against hematological cancer cell lines CCRF-CEM, CEM/ADR5000, and RPMI-8226 compared to the solid tumor cell lines MDA-MB-231, A549, and HT-29...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28300592/new-peptide-inhibitors-modulate-the-self-assembly-of-islet-amyloid-polypeptide-residues-11-20-in-vitro
#10
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...
June 5, 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
#11
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
#12
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
#13
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...
April 4, 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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
keyword
keyword
66625
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"