Abstract：
:This review focuses on alpha(1)-adrenoceptor phosphorylation and function. Most of what is currently known is based on studies on the hamster alpha(1B)-adrenoceptor. It is known that agonist stimulation leads to homologous desensitization of these receptors and current evidence indicates that such decrease in receptor activity is associated with receptor phosphorylation. Such receptor phosphorylation seems to involve G protein-receptor kinases and the receptor phosphorylation sites have been located in the carboxyl tail (Ser(404), Ser(408), and Ser(410)). There is also evidence showing that in addition to desensitization, receptor phosphorylation is associated with internalization and roles of beta-arrestins have been observed. Direct activation of protein kinase C leads to receptor desensitization/internalization associated with phosphorylation; the protein-kinase-C-catalyzed receptor phosphorylation sites have been also located in the carboxyl tail (Ser(394) and Ser(400)). Activation of G(q)-coupled receptors, such as the endothelin ET(A) receptor induces alpha(1B)-adrenoceptor phosphorylation and desensitization. Such effect involves protein kinase C and a yet unidentified tyrosine kinase. Activation of G(i)-coupled receptors, such as the lysophosphatidic acid receptor, also induces alpha(1B)-adrenoceptor phosphorylation and desensitization. These effects involve protein kinase C and phosphatidyl inositol 3-kinase. Interestingly, activation of epidermal growth factor receptors also induces alpha(1B)-adrenoceptor phosphorylation and desensitization involving protein kinase C and phosphatidyl inositol 3-kinase. A pivotal role of these kinases in heterologous desensitization is evidenced.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
García-Sáinz JA,Vázquez-Prado J,del Carmen Medina Ldoi
10.1016/s0014-2999(99)00896-1keywords:
subject
Has Abstractpub_date
2000-02-11 00:00:00pages
1-12issue
1eissn
0014-2999issn
1879-0712pii
S0014-2999(99)00896-1journal_volume
389pub_type
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