Document Detail


Phosphatidylinositol 3-kinase-δ up-regulates L-type Ca2+ currents and increases vascular contractility in a mouse model of type 1 diabetes.
MedLine Citation:
PMID:  20942845     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
BACKGROUND AND PURPOSE: Vasculopathies represent the main cause of morbidity and mortality in diabetes. Vascular malfunctioning in diabetes is associated with abnormal vasoconstriction and Ca(2+) handling by smooth muscle cells (SMC). Phosphatidylinositol 3-kinases (PI3K) are key mediators of insulin action and have been shown to modulate the function of voltage-dependent L-type Ca(2+) channels (Ca(V) 1.2). In the present work, we investigated the involvement of PI3K signalling in regulating Ca(2+) current through Ca(V) 1.2 (I(Ca,L) ) and vascular dysfunction in a mouse model of type I diabetes.
EXPERIMENTAL APPROACH: Changes in isometric tension were recorded on myograph. Ca(2+) currents in freshly dissociated mice aortic SMCs were measured using the whole-cell patch-clamp technique. Antisense techniques were used to knock-down the PI3Kδ isoform. KEY RESULTS Contractile responses to phenylephrine and KCl were strongly enhanced in diabetic aorta independent of a functional endothelium. The magnitude of phenylephrine-induced I(Ca,L) was also greatly augmented. PI3Kδ expression, but not PI3Kα, PI3Kβ, PI3Kγ, was increased in diabetic aortas and treatment of vessels with a selective PI3Kδ inhibitor normalized I(Ca,L) and contractile response of diabetic vessels. Moreover, knock-down of PI3Kδin vivo decreased PI3Kδ expression and normalized I(Ca,L) and contractile response of diabetic vessels ex vivo.
CONCLUSIONS AND IMPLICATIONS: Phosphatidylinositol 3-kinase δ was essential to the increased vascular contractile response in our model of type I diabetes. PI3Kδ signalling was up-regulated and most likely accounted for the increased I(Ca,L,) leading to increased vascular contractility. Blockade of PI3Kδ may represent a novel therapeutic approach to treat vascular dysfunction in diabetic patients.
Authors:
J F Pinho; M A A Medeiros; L S A Capettini; B A Rezende; P P Campos; S P Andrade; S F Cortes; J S Cruz; V S Lemos
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  British journal of pharmacology     Volume:  161     ISSN:  1476-5381     ISO Abbreviation:  Br. J. Pharmacol.     Publication Date:  2010 Dec 
Date Detail:
Created Date:  2010-11-08     Completed Date:  2011-05-18     Revised Date:  2011-12-21    
Medline Journal Info:
Nlm Unique ID:  7502536     Medline TA:  Br J Pharmacol     Country:  England    
Other Details:
Languages:  eng     Pagination:  1458-71     Citation Subset:  IM    
Affiliation:
Department of Physiology and Biophysics, ICB, Federal University of Minas Gerais, Belo Horizonte, Brazil.
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MeSH Terms
Descriptor/Qualifier:
Animals
Aorta / physiopathology
Calcium / metabolism
Calcium Channels, L-Type / metabolism*
Diabetes Mellitus, Experimental / metabolism*,  physiopathology
Diabetes Mellitus, Type 1 / metabolism*,  physiopathology
Male
Mice
Mice, Inbred C57BL
Muscle Contraction
Muscle, Smooth, Vascular / physiopathology
Myocytes, Smooth Muscle / physiology
Patch-Clamp Techniques
Phosphatidylinositol 3-Kinases / antagonists & inhibitors,  metabolism*
Receptors, Adrenergic, alpha-1 / metabolism
Signal Transduction
Up-Regulation
Vasoconstriction
Vasodilation
Chemical
Reg. No./Substance:
0/Calcium Channels, L-Type; 0/Cav1.2 protein, mouse; 0/Receptors, Adrenergic, alpha-1; 7440-70-2/Calcium; EC 2.7.1.-/Phosphatidylinositol 3-Kinases; EC 2.7.1.137/Pik3cd protein, mouse
Comments/Corrections
Comment In:
Br J Pharmacol. 2010 Dec;161(7):1455-7   [PMID:  20726982 ]

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