Therapeutic implications of endothelin and thrombin G-protein-coupled receptor transactivation of tyrosine and serine/threonine kinase cell surface receptors

Kamato, Danielle, Burch, Micah L., Osman, Narin, Zheng, Wenhua and Little, Peter J. (2013) Therapeutic implications of endothelin and thrombin G-protein-coupled receptor transactivation of tyrosine and serine/threonine kinase cell surface receptors. Journal of Pharmacy and Pharmacology, 65 4: 465-473. doi:10.1111/j.2042-7158.2012.01577.x


Author Kamato, Danielle
Burch, Micah L.
Osman, Narin
Zheng, Wenhua
Little, Peter J.
Title Therapeutic implications of endothelin and thrombin G-protein-coupled receptor transactivation of tyrosine and serine/threonine kinase cell surface receptors
Journal name Journal of Pharmacy and Pharmacology   Check publisher's open access policy
ISSN 0022-3573
2042-7158
Publication date 2013-04-01
Sub-type Critical review of research, literature review, critical commentary
DOI 10.1111/j.2042-7158.2012.01577.x
Open Access Status Not Open Access
Volume 65
Issue 4
Start page 465
End page 473
Total pages 9
Place of publication Chichester, West Sussex United Kingdom
Publisher John Wiley & Sons
Language eng
Formatted abstract
Objectives  This review discusses the latest developments in G protein coupled receptor (GPCR) signalling related to the transactivation of cell surface protein kinase receptors and the therapeutic implications.

Key findings  Multiple GPCRs have been known to transactivate protein tyrosine kinase receptors for almost two decades. More recently it has been discovered that GPCRs can also transactivate protein serine/threonine kinase receptors such as that for transforming growth factor (TGF)-β. Using the model of proteoglycan synthesis and glycosaminoglycan elongation in human vascular smooth muscle cells which is a component of an in vitro model of atherosclerosis, the dual tyrosine and serine/threonine kinase receptor transactivation pathways appear to account for all of the response to the agonists, endothelin and thrombin.

Summary  The broadening of the paradigm of GPCR receptor transactivation explains the broad range of activities of these receptors and also the efficacy of GPCR antagonists in cardiovascular therapeutics. Deciphering the mechanisms of transactivation with the aim of identifying a common therapeutic target remains the next challenge.
Keyword GPCR
Protein serine/threonine kinases
Protein tyrosine kinases
Transactivation
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status Unknown

Document type: Journal Article
Sub-type: Critical review of research, literature review, critical commentary
Collection: School of Pharmacy Publications
 
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