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Current Medicinal Chemistry

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ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

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Review Article

Development and Application of Activity-based Fluorescent Probes for High-Throughput Screening

Author(s): Juan Cheng and Xin Li*

Volume 29, Issue 10, 2022

Published on: 24 August, 2021

Page: [1739 - 1756] Pages: 18

DOI: 10.2174/0929867328666210525141728

Price: $65

Abstract

High-throughput screening facilitates the rapid identification of novel hit compounds; however, it remains challenging to design effective high-throughput assays, partially due to the difficulty of achieving sensitivity in the assay techniques. Among the various analytical methods that are used, fluorescence-based assays dominate due to their high sensitivity and ease of operation. Recent advances in activity-based sensing/imaging have further expanded the availability of fluorescent probes as monitors for high-throughput screening of result outputs. In this study, we have reviewed various activity-based fluorescent probes used in high-throughput screening assays, with an emphasis on their structure-related working mechanisms. Moreover, we have explored the possibility of developing additional and better probes to boost hit identification and drug development against various targets.

Keywords: High-throughput screening, fluorescent probe, drug target, hit identification, enzyme, receptor, metabolite.

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