| Chapter title |
Approaches to Assess Functional Selectivity in GPCRs: Evaluating G Protein Signaling in an Endogenous Environment
|
|---|---|
| Chapter number | 12 |
| 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_12 |
| Pubmed ID | |
| Book ISBNs |
978-1-4939-2913-9, 978-1-4939-2914-6
|
| Authors |
Laura M. Bohn, Lei Zhou, Jo-Hao Ho, Bohn, Laura M., Zhou, Lei, Ho, Jo-Hao |
| Abstract |
Ligand-directed signaling, biased agonism, and functional selectivity are terms that describe the propensity of a ligand to drive signaling toward one GPCR pathway over another. Most of the early examples demonstrated to date examine the divergence between GPCR signaling to G protein coupling and βarrestin2 recruitment. As biased agonists begin to become available based on cell-based screening criteria, a need arises to determine if G protein signaling biases will be maintained in the endogenous setting, wherein receptors are functioning to control relevant biological responses. This report presents our method and offers tips for evaluating G protein signaling in endogenous tissues. Predominately, brain tissues are discussed here; optimization points that can be applied to any tissues are highlighted. |
X Demographics
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|---|---|---|
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Demographic breakdown
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| Members of the public | 1 | 100% |
Mendeley readers
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|---|---|---|
| United States | 1 | 6% |
| Unknown | 17 | 94% |
Demographic breakdown
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|---|---|---|
| Researcher | 3 | 17% |
| Other | 3 | 17% |
| Student > Doctoral Student | 2 | 11% |
| Student > Ph. D. Student | 2 | 11% |
| Professor | 1 | 6% |
| Other | 4 | 22% |
| Unknown | 3 | 17% |
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|---|---|---|
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| Medicine and Dentistry | 1 | 6% |
| Other | 1 | 6% |
| Unknown | 6 | 33% |