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Mechanisms involved in α 1B ‐adrenoceptor desensitization
Author(s) -
GarcíaSáinz, J. Adolfo,
RomeroÁvila María Teresa,
AlcántaraHernández Rocío
Publication year - 2011
Publication title -
iubmb life
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.132
H-Index - 113
eISSN - 1521-6551
pISSN - 1521-6543
DOI - 10.1002/iub.519
Subject(s) - protein kinase c , microbiology and biotechnology , protein kinase a , g protein coupled receptor , biology , chemistry , signal transduction , kinase
α 1B ‐Adrenergic receptors mediate many of the actions of the natural catecholamines, adrenaline and noradrenaline. They belong to the seven transmembrane domains G protein‐coupled receptor superfamily and exert their actions mainly through activation of Gq proteins and phosphoinositide turnover/calcium signaling. Many hormones and neurotransmitters are capable of inducing α 1B ‐adrenergic receptor phosphorylation and desensitization; among them: adrenaline and noradrenaline, phorbol esters, endothelin‐I, bradykinin, lysophosphatidic acid, insulin, EGF, PDGF, IGF‐I, TGF‐β, and estrogens. Key protein kinases for these effects are G protein coupled receptor kinases and protein kinase C. The lipid/protein kinase, phosphoinositide‐3 kinase also appears to play a key role, acting upstream of protein kinase C. In addition to the agents employed for cells stimulation, we observed that paracrine/autocrine mediators also participate; these processes include EGF transactivation and sphingosine‐1‐phosphate production and action. The complex regulation of these receptors unlocks opportunities for therapeutic intervention. © 2011 IUBMB IUBMB Life, 2011