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Tools for GPCR drug discovery
Open accessAbstract
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.
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Cites
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De Vrieze, L. M., Walton, S. E., Pottie, E., Papsun, D., Logan, B. K., Krotulski, A. J., Stove, C. P., & Vandeputte, M. M. (2024) · Archives of Toxicology · doi:10.1007/s00204-024-03774-7 · Cited by 58
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Metadata
- Authors
- Zhang, R., & Xie, X.
- Venue
- Acta Pharmacologica Sinica
- Published
- 2012-01-23
- Volume
- 33
- Issue
- 3
- Pages
- 372-384
- ISSN
- 0253-9756 (ISSN-L)
- 1671-4083
- 1745-7254
- OpenAlex
- W1981385111
- Cited by
- 317
- References
- 7
- FWCI
- 8.48
- Type
- journal article
- Language
- en
- Open access
- hybrid
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