Tools for GPCR drug discovery
G-protein-coupled receptors (GPCRs) mediate many important physiological functions and are considered as one of the most successful therapeutic targets for a broad spectrum of diseases. The design and implementation of high-throughput GPCR assays that allow the cost-effective screening of large comp...
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| Format: | Online |
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Nature Publishing Group
2012
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| Online Access: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3312097/ |
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pubmed-33120972012-03-26 Tools for GPCR drug discovery Zhang, Ru Xie, Xin Review G-protein-coupled receptors (GPCRs) mediate many important physiological functions and are considered as one of the most successful therapeutic targets for a broad spectrum of diseases. The design and implementation of high-throughput GPCR assays that allow the cost-effective screening of large compound libraries to identify novel drug candidates are critical in early drug discovery. Early functional GPCR assays depend primarily on the measurement of G-protein-mediated 2nd messenger generation. Taking advantage of the continuously deepening understanding of GPCR signal transduction, many G-protein-independent pathways are utilized to detect the activity of GPCRs, and may provide additional information on functional selectivity of candidate compounds. With the combination of automated imaging systems and label-free detection systems, such assays are now suitable for high-throughput screening (HTS). In this review, we summarize the most widely used GPCR assays and recent advances in HTS technologies for GPCR drug discovery. Nature Publishing Group 2012-03 2012-01-23 /pmc/articles/PMC3312097/ /pubmed/22266728 http://dx.doi.org/10.1038/aps.2011.173 Text en Copyright © 2012 CPS and SIMM http://creativecommons.org/licenses/by-nc-nd/3.0/ This work is licensed under the Creative Commons Attribution-NonCommercial-No Derivative Works 3.0 Unported License. To view a copy of this license, visit http://creativecommons.org/licenses/by-nc-nd/3.0/ |
| repository_type |
Open Access Journal |
| institution_category |
Foreign Institution |
| institution |
US National Center for Biotechnology Information |
| building |
NCBI PubMed |
| collection |
Online Access |
| language |
English |
| format |
Online |
| author |
Zhang, Ru Xie, Xin |
| spellingShingle |
Zhang, Ru Xie, Xin Tools for GPCR drug discovery |
| author_facet |
Zhang, Ru Xie, Xin |
| author_sort |
Zhang, Ru |
| title |
Tools for GPCR drug discovery |
| title_short |
Tools for GPCR drug discovery |
| title_full |
Tools for GPCR drug discovery |
| title_fullStr |
Tools for GPCR drug discovery |
| title_full_unstemmed |
Tools for GPCR drug discovery |
| title_sort |
tools for gpcr drug discovery |
| description |
G-protein-coupled receptors (GPCRs) mediate many important physiological functions and
are considered as one of the most successful therapeutic targets for a broad spectrum of
diseases. The design and implementation of high-throughput GPCR assays that allow the
cost-effective screening of large compound libraries to identify novel drug candidates are
critical in early drug discovery. Early functional GPCR assays depend primarily on the
measurement of G-protein-mediated 2nd messenger generation. Taking advantage of the
continuously deepening understanding of GPCR signal transduction, many
G-protein-independent pathways are utilized to detect the activity of GPCRs, and may
provide additional information on functional selectivity of candidate compounds. With the
combination of automated imaging systems and label-free detection systems, such assays are
now suitable for high-throughput screening (HTS). In this review, we summarize the most
widely used GPCR assays and recent advances in HTS technologies for GPCR drug
discovery. |
| publisher |
Nature Publishing Group |
| publishDate |
2012 |
| url |
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3312097/ |
| _version_ |
1611516603564818432 |