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GRK3 regulation during CRF- and urocortin-induced CRF1 receptor desensitization.

Abstract：

:The EC(50) values for concentration-dependent stimulation of cAMP accumulation by CRF (1.3nM) and urocortin (1.0nM) were equivalent in human retinoblastoma Y79 cells. The time course and magnitude of CRF- and urocortin-induced CRF(1) receptor desensitization were similar. A significant 3-fold increase in GRK3, but not GRK2, mRNA levels accompanied the emergence of CRF(1) receptor desensitization in Y79 cells exposed to CRF. In preliminary experiments, retinoblastoma GRK3 protein expression became upregulated during a 48-h CRF exposure. Neither GRK3 nor GRK2 expression increased in Y79 cells exposed to urocortin for 10 min to 48 h. We hypothesize that GRK3 upregulation may be a cellular negative feedback process directed at maximizing CRF(1) receptor desensitization by heightening GRK3 phosphorylating capacity during prolonged exposure to high CRF. Regulation of GRK expression associated with urocortin- and CRF-induced CRF(1) receptor desensitization appears to differ, despite a similar level of signaling via the cAMP-protein kinase A pathway.

journal_name

Biochem Biophys Res Commun

journal_title

Biochemical and biophysical research communications

authors

Dautzenberg FM,Wille S,Braun S,Hauger RL

doi

10.1016/s0006-291x(02)02463-4

subject

Has Abstract

pub_date

2002-11-01 00:00:00

pages

303-8

issue

3

eissn

0006-291X

issn

1090-2104

pii

S0006291X02024634

journal_volume

298

pub_type

杂志文章

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