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427 Newest Publications about the topic high-throughput screening
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Peroxisome Proliferation-Activated Receptor δ Agonist GW0742 Interacts Weakly with Multiple Nuclear Receptors, Including the Vitamin D Receptor
10-06-2013 | Premchendar Nandhikonda; Adam Yasgar; Athena M. Baranowski; Preetpal S. Sidhu; Megan M. McCallum; Alan J. Pawlak; Ke ..., Biochemistry, 2013
A high-throughput screening campaign was conducted to identify small molecules with the ability to inhibit the interaction between the vitamin D receptor (VDR) and steroid receptor coactivator 2. These inhibitors represent novel molecular probes for modulating gene regulation mediated by VDR. ...
Studies of Asymmetric Styrene Cyclopropanation with a Rhodium(II) Metallopeptide Catalyst Developed with a High-Throughput Screen
08-06-2013 | Ramya Sambasivan, Zachary T. Ball, Chirality, 2013
ABSTRACT Dirhodium metallopeptides have been developed as selective catalysts for asymmetric cyclopropanation reactions. A selective ligand sequence has been identified by screening on-bead metallopeptide libraries in a 96-well plate format. Efficient ligand synthesis and screening allows ...
Recent Trends and Future Prospects in Computational GPCR Drug Discovery: From Virtual Screening to Polypharmacology
05-06-2013 | Carrieri, Antonio; Perez-Nueno, Violeta I.; Lentini, Giovanni; Ritchie, David W., Current Topics in Medicinal Chemistry, 2013
Abstract: Extending virtual screening approaches to deal with multi-target drug design and polypharmacology is an increasingly important aspect in drug design. In light of this, the concept of accessible chemical space and its exploration should be reviewed. The great advantages of ...
Nitrilase Activity Screening on Structurally Diverse Substrates: Providing Biocatalytic Tools for Organic Synthesis
04-06-2013 | Carine Vergne‐Vaxelaire, Franck Bordier, Aurélie Fossey, Marielle Besnard‐Gonnet, Adrien Debard, Aline Mariage, Virg ..., Advanced Synthesis & Catalysis, 2013
Abstract A high‐throughput screening of candidate nitrilases against 25 structurally diverse substrates allowed us to create a wide collection of 125 experimentally validated nitrilases. The enzymes were selected by genomic approach from 700 diverse prokaryotic species and one metagenome ...
Combinatorial Approach to Turbine Bond Coat Discovery
30-05-2013 | Christopher Jason Metting; Jonathan Kenneth Bunn; Ellen Underwood; Stephen Smoak; Jason Hattrick-Simpers, Journal of Combinatorial Chemistry, 2013
A nondestructive method for the high-throughput screening of novel bond coat materials has been developed. By using a suite of characterization techniques, including Raman spectroscopy, fluorescence spectroscopy, and X-ray diffraction, a rapid determination of thermally grown oxide phases and ...
High-Throughput Screening of Si–Ni Flux for SiC Solution Growth Using a High-Temperature Laser Microscope Observation and Secondary Ion Mass Spectroscopy Depth Profiling
28-05-2013 | Shingo Maruyama; Aomi Onuma; Kazuhisa Kurashige; Tomohisa Kato; Hajime Okumura; Yuji Matsumoto, Journal of Combinatorial Chemistry, 2013
Screening of Si-based flux materials for solution growth of SiC single crystals was demonstrated using a thin film composition-spread technique. The reactivity and diffusion of carbon in a composition spread of the flux was investigated by secondary ion mass spectroscopy depth profiling of ...
Sulphonamido-quinoxalines: Search for anticancer agent
27-05-2013 | Author(s): Rahul Ingle , Rajendra Marathe , Dipak Magar , Harun M. Patel , Sanjay J. Surana, European Journal of Medicinal Chemistry, 2013
Publication date: July 2013 Source:European Journal of Medicinal Chemistry, Volume 65 Author(s): Rahul Ingle , Rajendra Marathe , Dipak Magar , Harun M. Patel , Sanjay J. Surana A series of new sulphonamido-quinoxaline derivatives 3(a–p) have been prepared which are structurally ...
Identification of Substituted Pyrimido[5,4-b]indoles as Selective Toll-Like Receptor 4 Ligands
24-05-2013 | Michael Chan; Tomoko Hayashi; Richard D. Mathewson; Afshin Nour; Yuki Hayashi; Shiyin Yao; Rommel I. Tawatao; Brian ..., Journal of Medicinal Chemistry, 2013
A cell-based high-throughput screen to identify small molecular weight stimulators of the innate immune system revealed substituted pyrimido[5,4-b]indoles as potent NFκB activators. The most potent hit compound selectively stimulated Toll-like receptor 4 (TLR4) in human and mouse cells. ...
Overcoming Compound Fluorescence in the FLiK Screening Assay with Red-Shifted Fluorophores
24-05-2013 | Ralf Schneider; Anne Gohla; Jeffrey R. Simard; Dharmendra B. Yadav; Zhizhou Fang; Willem A. L. van Otterlo; Daniel Rauh, Journal of the American Chemical Society, 2013
In the attempt to discover novel chemical scaffolds that can modulate the activity of disease-associated enzymes, such as kinases, biochemical assays are usually deployed in high-throughput screenings. First-line assays, such as activity-based assays, often rely on fluorescent molecules by ...
A Novel Near-infrared Fluorescence Chemosensor for Copper Ion Detection Using Click Ligation and Energy Transfer
22-05-2013 | Aeju Lee; Jungwook Chin; Ok Kyu Park; Hyunjin Chung; Jin Won Kim; Soo-Young Yoon; Kyeongsoon Park, Chemical Communication, 2013
A novel near-infrared (NIR) fluorescence copper sensor allows rapid and ultra-sensitive detection of copper ions with excellent selectivity and specificity due to the specificity of click ligation and effective dark-quenching mechanism. Moreover, it can be applied for high-throughput ...
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