Words similar to agonist-induced
Example sentences for: agonist-induced
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The human alpha-2A adrenergic receptor has an acidic serine-rich motif (EESSSSD) in the third intracellular loop that has been shown to be important in agonist-induced desensitization but not in agonist-induced sequestration/internalization.
There are three subtypes of the alpha-2 adrenergic receptor: alpha-2A; alpha-2B; and alpha-2C [ 15 ] . The human alpha-2A subtype undergoes phosphorylation and short-term desensitization [ 11 12 ] , whereas the human alpha-2C subtype is not phosphorylated [ 16 ] and does not desensitize [ 11 ] . The human alpha-2C subtype, however, does undergo arrestin-dependent internalization [ 17 ] . Many studies [ 11 18 ] , including those from our laboratory [ 10 19 20 ] , have demonstrated agonist-induced down-regulation of alpha-2 receptors, although much less is known about the specific mechanisms for down-regulation as compared to the beta-2 receptor.
By contrast, a deletion of twelve residues of the human alpha-2A receptor (293-304) which includes the EESSSSE motif did not appear to prevent agonist-induced down-regulation [ 26 ] . Thus a phosphorylation pathway may not be involved in agonist-induced down-regulation of the alpha-2A adrenergic receptor.
All three alpha-2 adrenergic receptor subtypes from nearly all species that have been tested undergo agonist-induced down-regulation [ 24 25 ] . Interestingly, we have shown that the potency of norepinephrine to produce down-regulation differs among alpha-2 receptor subtypes [ 19 24 ] . The concentration of norepinephrine required to produce half-maximal down-regulation is approximately 2 μM for the alpha-2A receptor.
In adrenergic receptors, which have been characterized in detail, rapid endocytosis appears to be required for resensitization of receptors following agonist-induced phosphorylation ( 28).
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