Download e-book for kindle: A Practical Guide to Assay Development and High-Throughput by Taosheng Chen

By Taosheng Chen

ISBN-10: 1420070509

ISBN-13: 9781420070507

The advance of compatible assays, the combination of applicable expertise, and the powerful administration of the fundamental infrastructure are all serious to the good fortune of any high-throughput screening (HTS) exercise. despite the fact that, few scientists have the multidisciplinary adventure had to keep watch over all elements of an HTS drug discovery venture. a realistic advisor to Assay improvement and High-Throughput Screening in Drug Discovery integrates the adventure of various specialists who provide primary and sensible suggestions throughout quite a few events. The publication first discusses assay advancements for vital aim sessions comparable to protein kinases and phosphatases, proteases, nuclear receptors, G protein-coupled receptors, ion channels, and warmth surprise proteins. It subsequent examines assay advancements for mobile viability, apoptosis, and infectious illnesses. The members discover the applying of rising applied sciences and platforms, together with image-based excessive content material screening, RNA interference, and first cells. eventually, they speak about the basic elements of the built-in HTS approach, equivalent to screening automation, compound library administration, the screening of common items from botanical assets, and screening informatics. Designed to encourage researchers to deliver extra advances to the sphere, this quantity offers sensible assistance on how one can begin, validate, optimize, and deal with a bioassay meant to display huge collections of compounds. Drawing at the wisdom from specialists actively inquisitive about assay improvement and HTS, this can be a source that's either accomplished and targeted.

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Extra info for A Practical Guide to Assay Development and High-Throughput Screening in Drug Discovery (Critical Reviews in Combinatorial Chemistry)

Sample text

And A. Schmid. 2007. Farnesyl pyrophosphate synthase: real-time kinetics and inhibition by nitrogen-containing bisphosphonates in a scintillation assay. Assay Drug Dev. Technol. 5, 205–214. A. et al. 2007. Development and implementation of a 384-well homogeneous fluorescence intensity high-throughput screening assay to identify mitogen-activated protein kinase phosphatase-1 dualspecificity protein phosphatase inhibitors. Assay Drug Dev. Technol. 5, 319–332. A. et al. 2007. Three mechanistically distinct kinase assays compared: measurement of intrinsic ATPase activity identified the most comprehensive set of ITK inhibitors.

In the intact peptidic substrate (amino acids symbolized by X, Y, and Z) labeled with a fluorophore at the C terminus, the intensity of fluorescence emission (light gray arrow) after excitation (dark gray arrow) is low. Through the cleavage of the substrate between the C terminal amino acid (Z) and the fluorophore by a protease, the intensity of fluorescence emission is strongly enhanced. An increase of fluorescence intensity over time dependent on the enzymatic velocity is observed. coumarin (AFC), and rhodamine 110 (Rh110) attached to the C terminus are frequently used.

The production of asymmetric Rh110-labeled bis-substituted peptides is much more difficult because the synthesis requires significantly more steps than required for symmetrically bis-substituted peptides. The critical step is the synthesis of the mono-substituted intermediate product Rh110-ZYX with low yield in most cases (personal communication). However, due to the fact that a strong fluorescence increase is only observed after the fluorophore has been cleaved off from both peptide chains of the symmetrically bis-substituted substrate (two-step proteolysis), the kinetics of the enzymatic reaction can be followed more accurately and easily with peptides comprising only one copy of the scissile bond.

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A Practical Guide to Assay Development and High-Throughput Screening in Drug Discovery (Critical Reviews in Combinatorial Chemistry) by Taosheng Chen


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