Chapter title |
High-Throughput Screening for Allosteric Modulators of GPCRs
|
---|---|
Chapter number | 15 |
Book title |
G Protein-Coupled Receptors in Drug Discovery
|
Published in |
Methods in molecular biology, January 2015
|
DOI | 10.1007/978-1-4939-2914-6_15 |
Pubmed ID | |
Book ISBNs |
978-1-4939-2913-9, 978-1-4939-2914-6
|
Authors |
Robert L. Bertekap, Neil T. Burford, Zhuyin Li, Andrew Alt, Bertekap, Robert L., Burford, Neil T., Li, Zhuyin, Alt, Andrew |
Abstract |
The continued evolution of our understanding of G protein-coupled receptor (GPCR) signaling has revealed new opportunities for drug discovery. Specifically, biased agonism at GPCRs and allosteric modulation of GPCRs both represent emerging areas of GPCR biology that hold promise for the development of novel GPCR-targeted therapeutics that may provide greater therapeutic efficacy and/or improved side-effect profiles. To obtain initial chemical leads, high-throughput screening (HTS) of a large compound library for the desired activity is often deployed during the early stages of a discovery program. The identification of allosteric modulators, in particular, poses significant challenges for HTS. We describe several HTS protocols designed for the identification of GPCR ligands, with a particular focus on the identification of allosteric modulators. |
Mendeley readers
Geographical breakdown
Country | Count | As % |
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Unknown | 13 | 100% |
Demographic breakdown
Readers by professional status | Count | As % |
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Student > Master | 3 | 23% |
Student > Ph. D. Student | 2 | 15% |
Other | 1 | 8% |
Researcher | 1 | 8% |
Professor > Associate Professor | 1 | 8% |
Other | 1 | 8% |
Unknown | 4 | 31% |
Readers by discipline | Count | As % |
---|---|---|
Pharmacology, Toxicology and Pharmaceutical Science | 4 | 31% |
Biochemistry, Genetics and Molecular Biology | 3 | 23% |
Agricultural and Biological Sciences | 1 | 8% |
Chemistry | 1 | 8% |
Unknown | 4 | 31% |