Download A Practical Guide to Assay Development and High-Throughput by Taosheng Chen PDF

By Taosheng Chen

ISBN-10: 1420070509

ISBN-13: 9781420070507

The improvement of appropriate assays, the mixing of acceptable expertise, and the potent administration of the fundamental infrastructure are all serious to the luck of any high-throughput screening (HTS) undertaking. besides the fact that, few scientists have the multidisciplinary event had to keep watch over all points of an HTS drug discovery undertaking. a realistic advisor to Assay improvement and High-Throughput Screening in Drug Discovery integrates the event of numerous specialists who supply primary and functional information throughout a number of occasions. The ebook first discusses assay advancements for very important objective periods similar to protein kinases and phosphatases, proteases, nuclear receptors, G protein-coupled receptors, ion channels, and warmth surprise proteins. It subsequent examines assay advancements for cellphone viability, apoptosis, and infectious ailments. The participants discover the applying of rising applied sciences and platforms, together with image-based excessive content material screening, RNA interference, and first cells. ultimately, they speak about the basic parts of the built-in HTS strategy, reminiscent of screening automation, compound library administration, the screening of traditional items from botanical assets, and screening informatics. Designed to inspire researchers to deliver extra advances to the sector, this quantity offers functional advice on the right way to begin, validate, optimize, and deal with a bioassay meant to monitor huge collections of compounds. Drawing at the wisdom from specialists actively fascinated about assay improvement and HTS, it is a source that's either finished and targeted.

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

Sample text

Coumarin (AFC), and rhodamine 110 (Rh110) attached to the C terminus are frequently used. 1 summarizes the key characteristics of this selection of fluorophores. Dipeptidylpeptidases like DPPIV cleave the peptide bond between the amino acids in P1 and P1b positions with the label attached to the P1b position. 2). This is possible with high catalytic efficiency (kcat/KM), because the aminopeptidases primarily recognize and bind to the N termini of their substrates. The dye attached to the C terminus does not alter the protease–substrate interaction.

A protocol that is suitable for one type of reader may not work as well in a second type of reader due to variations in the optics resulting in differences in dynamic range and sensitivity. Sensitivity is important because it aids in the miniaturization of assays and helps reduce the amounts of expensive reagents required. The ability to detect small quantities of product in an enzyme reaction means that less enzyme will be required. Dynamic range is important because a large dynamic range allows more flexibility in varying the kinetics and timing of the assay.

Screen. 12, 70–83. Koresawa, M. and T. Okabe. 2004. High-throughput screening with quantitation of ATP consumption: a universal non-radioisotope, homogeneous assay for protein kinase. Assay Drug Dev. Technol. 2, 153–160. R. 2006. Principles of Fluorescence Spectroscopy. 3rd ed. Berlin: Springer. S. and Q. Wang. 2007. Seeing is believing: peptide-based fluorescent sensors of protein tyrosine kinase activity. Chem. BioChem. 8, 373–378. F. Y. Zhang. 2001. Assays for protein-tyrosine phosphatases. Meth.

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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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