Journal ArticleDOI
High-throughput screening assays for the identification of chemical probes
James Inglese,Ronald L. Johnson,Anton Simeonov,Menghang Xia,Wei Zheng,Christopher P. Austin,Douglas S. Auld +6 more
TLDR
High-throughput screening (HTS) assays enable the testing of large numbers of chemical substances for activity in diverse areas of biology as mentioned in this paper, including signal transduction pathways and complex networks functioning in cellular environments.Abstract:
High-throughput screening (HTS) assays enable the testing of large numbers of chemical substances for activity in diverse areas of biology. The biological responses measured in HTS assays span isolated biochemical systems containing purified receptors or enzymes to signal transduction pathways and complex networks functioning in cellular environments. This Review addresses factors that need to be considered when implementing assays for HTS and is aimed particularly at investigators new to this field. We discuss assay design strategies, the major detection technologies and examples of HTS assays for common target classes, cellular pathways and simple cellular phenotypes. We conclude with special considerations for configuring sensitive, robust, informative and economically feasible HTS assays.read more
Citations
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Journal ArticleDOI
Bright Ideas for Chemical Biology
Luke D. Lavis,Ronald T. Raines +1 more
TL;DR: The chemical and photophysical properties of oft-used fluorophores are examined and classic and contemporary examples in which utility has been built upon these scaffolds are highlighted.
Journal ArticleDOI
SwissTargetPrediction: A web server for target prediction of bioactive small molecules
David Gfeller,Aurélien Grosdidier,Matthias Wirth,Antoine Daina,Olivier Michielin,Vincent Zoete +5 more
TL;DR: SwissTargetPrediction is introduced, a web server to accurately predict the targets of bioactive molecules based on a combination of 2D and 3D similarity measures with known ligands, which can be carried out in five different organisms.
Journal ArticleDOI
Target identification and mechanism of action in chemical biology and drug discovery
TL;DR: This work focuses on target-identification and mechanism-of-action studies, which allow small-molecule action to be tested in a more disease-relevant setting at the outset, but require follow-up studies to determine the precise protein target or targets responsible for the observed phenotype.
Journal ArticleDOI
Target identification using drug affinity responsive target stability (DARTS)
Brett Lomenick,Rui Hao,Nao Jonai,Randall Chin,Mariam Aghajan,Sarah Warburton,Jianing Wang,Raymond Wu,Fernando Gomez,Joseph A. Loo,James A. Wohlschlegel,Thomas M. Vondriska,Jerry Pelletier,Harvey R. Herschman,Jon Clardy,Catherine F. Clarke,Jing Huang +16 more
TL;DR: In this paper, drug affinity responsive target stability (DARTS) is proposed to identify known small-molecule-protein interactions and reveal the eukaryotic translation initiation machinery as a molecular target for the longevity enhancing plant natural product resveratrol.
Journal ArticleDOI
Combinatorial Strategies in Fluorescent Probe Development
TL;DR: This poster presents a poster presented at the 2016 Singapore International Conference of the American Association for the Advancement of Science and Technology (A*STAR) entitled “Advances in Bioimaging Probe Development: Foundations of a scalable, scalable and reproducible Nanofiltration Probe for Matrix-based Assays.”
References
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Book
Principles of fluorescence spectroscopy
TL;DR: This book describes the fundamental aspects of fluorescence, the biochemical applications of this methodology, and the instrumentation used in fluorescence spectroscopy.
Journal ArticleDOI
Quantum dot bioconjugates for imaging, labelling and sensing
TL;DR: This review looks at current methods for preparing QD bioconjugates as well as presenting an overview of applications, and concludes that the potential of QDs in biology has just begun to be realized and new avenues will arise as the ability to manipulate these materials improves.
Journal ArticleDOI
The druggable genome
Andrew L. Hopkins,Colin R. Groom +1 more
TL;DR: An assessment of the number of molecular targets that represent an opportunity for therapeutic intervention is crucial to the development of post-genomic research strategies within the pharmaceutical industry.
Journal ArticleDOI
The fluorescent toolbox for assessing protein location and function
TL;DR: The focus is on protein detection in live versus fixed cells: determination of protein expression, localization, activity state, and the possibility for combination of fluorescent light microscopy with electron microscopy.
Patent
High throughput screen
TL;DR: In this paper, a high throughput screen for determining the effect of test compounds on ion channel or transporter activity was proposed, and a method for monitoring ion channel activity in a membrane.