| Status | 已發表Published |
| Integrating the GPCR transactivation-dependent and biased signalling paradigms in the context of PAR-1 signalling | |
Zheng, W.
| |
| 2016-10-01 | |
| Source Publication | Br J Pharmacol
 |
| ISSN | 0007-1188 |
| Pages | 2992-3000 |
| Abstract | Classically, receptor-mediated signalling was conceived as a linear process involving one agonist, a variety of potential targets within a receptor family (e.g. alpha- and beta-adrenoceptors) and a second messenger (e.g. cyclic AMP)-triggered response. If distinct responses were stimulated by the same receptor in different tissues (e.g. lipolysis in adipocytes versus increased beating rate in the heart caused by adrenaline), the differences were attributed to different second messenger targets in the different tissues. It is now realized that an individual receptor can couple to multiple effectors (different G-proteins; different beta-arrestins), even in the same cell, to drive very distinct responses. Further, tailored agonists can mould the receptor conformation to activate one signal pathway versus another by a process termed "biased signalling". Complicating issues further, we now know that activating one receptor can rapidly trigger the local release of agonists for a second receptor via a process termed "transactivation". Thus, the end response can represent a cooperative signalling process involving two or more receptors linked by transactivation. This overview, with a focus on the G-protein-coupled receptor, protease-activated receptor-1, integrates both of these processes to envision the complex array of responses that can arise when biased receptor signalling also involves the receptor transactivation process. The therapeutic implications of this signalling matrix are also briefly discussed. This article is protected by copyright. All rights reserved. |
| Keyword | GPCR transactivation-dependent biased signalling paradigms |
| Language | 英語English |
| The Source to Article | PB_Publication |
| PUB ID | 16668 |
| Document Type | Journal article |
| Collection | University of Macau |
| Corresponding Author | Zheng, W. |
| Recommended Citation GB/T 7714 | Zheng, W.. Integrating the GPCR transactivation-dependent and biased signalling paradigms in the context of PAR-1 signalling[J]. Br J Pharmacol, 2016, 2992-3000. |
| APA | Zheng, W..(2016). Integrating the GPCR transactivation-dependent and biased signalling paradigms in the context of PAR-1 signalling. Br J Pharmacol, 2992-3000. |
| MLA | Zheng, W.."Integrating the GPCR transactivation-dependent and biased signalling paradigms in the context of PAR-1 signalling".Br J Pharmacol (2016):2992-3000. |
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