Words similar to agonist-induced
Example sentences for: agonist-induced
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Indeed, this motif is not found in the alpha-2B subtype which does undergo agonist-induced down-regulation, although as noted above a highly acidic region appears to be important and could be related to the additional negative charge provided by phosphorylation.
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.
In adrenergic receptors, which have been characterized in detail, rapid endocytosis appears to be required for resensitization of receptors following agonist-induced phosphorylation ( 28).
The human alpha-2C receptor is somewhat unique among the alpha-2 receptors in that it does not appear to undergo agonist-induced down-regulation [ 11 ] . The human alpha-2A adrenergic receptor, which does undergo down-regulation, has an acidic serine motif (EESSSSD) in the third intracellular loop.
Sequentially mutating each of the four serines to alanine decreased the phosphorylation of the receptor by approximately 25% for each serine, and mutating either the first two or the last two serines to alanines prevented agonist-induced desensitization, but not agonist-induced sequestration/internalization [ 12 ] . The influence of mutations in this motif on down-regulation has not been investigated.
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