期刊
CLINICAL SCIENCE
卷 126, 期 11-12, 页码 753-774出版社
PORTLAND PRESS LTD
DOI: 10.1042/CS20130414
关键词
angiotensin II; angiotensin II type 1 receptor (AT(1) receptor); biased agonism; bradykinin; G-protein-coupled receptor (GPCR); signaling pathway
资金
- Fundacao de Amparo a Pesquisa do Estado de Sao Paulo (FAPESP)
- Research Support Center of the University of Sao Paulo NAP-CISBi [12.1.17598.1.3]
- Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior (CAPES)
- Conselho Nacional de Desenvolvimento Cientffico e Tecnologico (CNPq)
- CNPq Research Fellowship
GPCRs (G-protein-coupled receptors) are among the most important targets for drug discovery due to their ubiquitous expression and participation in cellular events under both healthy and disease conditions. These receptors can be activated by a plethora of ligands, such as ions, odorants, small ligands and peptides, including angiotensins and kinins, which are vasoactive peptides that are classically involved in the pathophysiology of cardiovascular events. These peptides and their corresponding GPCRs have been reported to play roles in other systems and under pathophysiological conditions, such as cancer, central nervous system disorders, metabolic dysfunction and bone resorption. More recently, new mechanisms have been described for the functional regulation of GPCRs, including the transactivation of other signal transduction receptors and the activation of G-protein-independent pathways. The existence of such alternative mechanisms for signal transduction and the discovery of agonists that can preferentially trigger one signalling pathway over other pathways (called biased agonists) have opened new perspectives for the discovery and development of drugs with a higher specificity of action and, therefore, fewer side effects. The present review summarizes the current knowledge on the non-canonical signalling and roles of angiotensins and kinins.
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