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#34130349   2021/06/15 To Up

Tyrosine Kinase Inhibitor Sunitinib Delays Platelet-Induced Coagulation: Additive Effects of Aspirin.

 Sunitinib is a multitarget tyrosine kinase inhibitor (TKI) used for cancer treatment. In platelets, sunitinib affects collagen-induced activation under noncoagulating conditions. We investigated (1) the effects of sunitinib on thrombus formation induced by other TK-dependent receptors, and (2) the effects under coagulating conditions. Cardiovascular disease is a comorbidity in cancer patients, resulting in possible aspirin treatment. Sunitinib and aspirin are associated with increased bleeding risk, and therefore we also investigated (3) the synergistic effects of these compounds on thrombus and fibrin formation.
Bibian M E Tullemans, Delia I Fernández, Alicia Veninga, Constance C F M J Baaten, Linsey J F Peters, Maureen J B Aarts, Johannes A Eble, Elena Campello, Luca Spiezia, Paolo Simioni, Emiel P C van der Vorst, Paola E J van der Meijden, Johan W M Heemskerk, Marijke J E Kuijpers

1448 related Products with: Tyrosine Kinase Inhibitor Sunitinib Delays Platelet-Induced Coagulation: Additive Effects of Aspirin.

8 inhibitors5 inhibitors0.1ml96T7 inhibitors5 mg5 mg96T5 mg100ul5 mg

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#34130273   2021/06/15 To Up

Temporal order of mutations influences cancer initiation dynamics.

Cancer is a set of genetic diseases that are driven by mutations. It was recently discovered that the temporal order of genetic mutations affects the cancer evolution and even the nature of the disease itself. The mechanistic origin of these observations, however, remain not well understood. Here we present a theoretical model for cancer initiation dynamics that allows us to quantify the impact of the temporal order of mutations. In our approach, the cancer initiation process is viewed as a set of stochastic transitions between discrete states defined by the different numbers of mutated cells. Using a first-passage analysis, probabilities and times before the cancer initiation are explicitly evaluated for two alternative sequences of two mutations. It is found that the probability of cancer initiation is determined only by the first mutation, while the dynamics depends on both mutations. In addition, it is shown that the acquisition of a mutation with higher fitness before mutation with lower fitness increases the probability of the tumor formation but delays the cancer initiation. Theoretical results are explained using effective free-energy landscapes.
Hamid Teimouri, Anatoly B Kolomeisky

2926 related Products with: Temporal order of mutations influences cancer initiation dynamics.

6 ml Ready-to-use 100ug

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#34130235   2021/06/12 To Up

Advances in the study of GPCRs by F NMR.

Crystallography and cryo-electron microscopy have advanced atomic resolution perspectives of inactive and active states of G protein-coupled receptors (GPCRs), alone and in complex with G proteins or arrestin. F NMR can play a role in ascertaining activation mechanisms and understanding the complete energy landscape associated with signal transduction. Fluorinated reporters are introduced biosynthetically via fluorinated amino acid analogs or chemically, via thiol-specific fluorinated reporters. The chemical shift sensitivity of these reporters makes it possible to discern details of conformational ensembles. In addition to spectroscopic details, paramagnetic species can be incorporated through orthogonal techniques to obtain distance information on fluorinated reporters, while T-and T-based relaxation experiments provide details on exchange kinetics in addition to fluctuations within a given state.
Louis-Philippe Picard, Robert Scott Prosser

2342 related Products with: Advances in the study of GPCRs by F NMR.

0.1 mg0.2 mg500 ml1 Set100ug Lyophilized1 Set

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#34130231   2021/06/09 To Up

A simplified model for simulating anaerobic digesters: Application to valorisation of bagasse and distillery spent wash.

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Sanjay Nagarajan, Varaha Prasad Sarvothaman, Martin Knörich, Vivek V Ranade

2355 related Products with: A simplified model for simulating anaerobic digesters: Application to valorisation of bagasse and distillery spent wash.

100 ml0.1 mg25 µg 100ul0.1 mg 100ul0.1 ml0.25 mg0.2 mg1 ml 100ul250 ml

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#34130219   2021/06/07 To Up

Dismantling the bacterial glycocalyx: Chemical tools to probe, perturb, and image bacterial glycans.

The bacterial glycocalyx is a quintessential drug target comprised of structurally distinct glycans. Bacterial glycans bear unusual monosaccharide building blocks whose proper construction is critical for bacterial fitness, survival, and colonization in the human host. Despite their appeal as therapeutic targets, bacterial glycans are difficult to study due to the presence of rare bacterial monosaccharides that are linked and modified in atypical manners. Their structural complexity ultimately hampers their analytical characterization. This review highlights recent advances in bacterial chemical glycobiology and focuses on the development of chemical tools to probe, perturb, and image bacterial glycans and their biosynthesis. Current technologies have enabled the study of bacterial glycosylation machinery even in the absence of detailed structural information.
Phuong Luong, Danielle H Dube

2097 related Products with: Dismantling the bacterial glycocalyx: Chemical tools to probe, perturb, and image bacterial glycans.

100mgBacterial streak10020mg500 mlBacterial streak

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#34130217   2021/06/07 To Up

"Clicking" fragment leads to novel dual-binding cholinesterase inhibitors.

Cholinesterase inhibitors are potent therapeutics in the treatment of Alzheimer's disease. Among them, dual binding ligands have recently gained a lot of attention. We discovered novel dual-binding cholinesterase inhibitors, using "clickable" fragments, which bind to either catalytic active site (CAS) or peripheral anionic site (PAS) of the enzyme. Copper(I)-catalyzed azide-alkyne cycloaddition allowed to effectively synthesize a series of final heterodimers, and modeling and kinetic studies confirmed their ability to bind to both CAS and PAS. A potent acetylcholinesterase inhibitor with IC = 18 nM (compound 23g) was discovered. A target-guided approach to link fragments by the enzyme itself was tested using butyrylcholinesterase.
Zuzanna Molęda, Anna Zawadzka, Zbigniew Czarnocki, Leticia Monjas, Anna K H Hirsch, Armand Budzianowski, Jan K Maurin

1478 related Products with: "Clicking" fragment leads to novel dual-binding cholinesterase inhibitors.

1 ml100 µg5 g1 kit(96 Wells)1000 100 ml0.1 mg 2 ml Ready-to-use 0.2 mg1x96 well plate1 module50ug

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#34130216   2021/06/06 To Up

Synthetic fluorescent MYC probe: Inhibitor binding site elucidation and development of a high-throughput screening assay.

We report the discovery of a fluorescent small molecule probe. This probe exhibits an emission increase in the presence of the oncoprotein MYC that can be attenuated by a competing inhibitor. Hydrogen-deuterium exchange mass spectrometry analysis, rationalized by induced-fit docking, suggests it binds to the "coiled-coil" region of the leucine zipper domain. Point mutations of this site produced functional MYC constructs resistant to inhibition in an oncogenic transformation assay by compounds that displace the probe. Utilizing this probe, we have developed a high-throughput assay to identify MYC inhibitor scaffolds. Screening of a diversity library (N = 1408, 384-well) and a library of pharmacologically active compounds (N = 1280, 1536-well) yielded molecules with greater drug-like properties than the probe. One lead is a potent inhibitor of oncogenic transformation and is specific for MYC relative to resistant mutants and transformation-inducing oncogenes. This method is simple, inexpensive, and does not require protein modification, DNA binding, or the dimer partner MAX. This assay presents an opportunity for MYC inhibition researchers to discover unique scaffolds.
Ryan J Shirey, Jonathan R Hart, BanuPriya Sridharan, Scott J Novick, Lewis D Turner, Bin Zhou, Alexander L Nielsen, Lisa M Eubanks, Lynn Ueno, Mark S Hixon, Luke L Lairson, Timothy P Spicer, Louis D Scampavia, Patrick R Griffin, Peter K Vogt, Kim D Janda

2436 related Products with: Synthetic fluorescent MYC probe: Inhibitor binding site elucidation and development of a high-throughput screening assay.

400Tests100 assays4 Sample Kit1 kit

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#34130212   2021/06/08 To Up

Exosome-based hybrid nanostructures for enhanced tumor targeting and hyperthermia therapy.

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Su-Hyun Kwon, Hasan Al Faruque, Hyeonwoo Kee, Eunjoo Kim, Sukho Park

1375 related Products with: Exosome-based hybrid nanostructures for enhanced tumor targeting and hyperthermia therapy.

One 96-Well Microplate Ki100 TESTS1000 tests 96T/Kit 0.1 mg

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#34130205   2021/06/04 To Up

Fullerenol as a water-soluble MALDI-MS matrix for rapid analysis of small molecules and efficient quantification of saccharin sodium in foods.

Due to the strong background interferences in the low-mass region and poor reproducibility of conventional organic matrices, it is of great importance to develop a novel matrix for matrix-assisted laser desorption/ionization mass spectrometry (MALDI-MS) to qualitatively and quantitatively analyze small molecules. In this work, water-soluble fullerenol C(OH) was selected as a MALDI matrix for the analysis of low-molecular-weight compounds in consideration of optical absorption property, water solubility and stability. Compared with the traditional matrices, fullerenol demonstrated lower background interference and stronger peak intensity. In addition, the hydrophilic fullerenol could avoid the heterogeneous crystallization in sample preparation, increase the reproducibility and sensitivity of MALDI-MS, and ameliorate quantitative analysis of small molecules. With saccharin as model analyte, quantitative analysis was carried out using fullerenol as matrix. The results demonstrated satisfying reproducibility and good tolerance to salt. The limit-of-detection of the quantitative analysis was as low as 4 pmol, and the linear range is 1-100 μg mL with R greater than 0.99. The analytical results also showed excellent precision and accuracy, low matrix effect and good recovery rate. Fullerenol as a potential matrix was further validated in the quantification of saccharin sodium in different real food samples, such as nuts and drinks. This work not only confirms the potential of fullerenol for the quantitative analysis in food field, but also provides a new technique for rapid analysis of small molecules.
Xiao-Pan Liu, Wen-Qian Sun, Tong-Xin Liu, Bing-Bing Liu, Chang-Po Chen

2853 related Products with: Fullerenol as a water-soluble MALDI-MS matrix for rapid analysis of small molecules and efficient quantification of saccharin sodium in foods.

400Tests900 tests100 μg96 assays 96 assays1 kit

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