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Agonist induced receptor internalization of neuropeptide Y receptor subtypes depends on third intracellular loop and C-terminus.

Abstract：

:Agonist stimulation of G-protein coupled receptors (GPCRs) results in the redistribution of the receptor from the cell surface into intracellular compartments through the process of endocytosis. Monitoring ligand-mediated internalization of GPCRs in living cells has become experimentally accessible by applying fluorescent reagents and fluorescence microscopy. By using cell lines that transiently, stably or endogenously express the human Y receptor (hYR) subtypes hY(1)R, hY(2)R, hY(4)R and hY(5)R and differently fluorescently tagged receptor proteins we were able to unravel further details concerning the internalization behavior of this multi-receptor/multi-ligand system. For the first time we could show that also the hY(2)R is internalized with a rate which is comparable to the hY(1)R and the hY(4)R. In contrast, the hY(5)R was internalized much slower and the rate remained unaffected by co-expression with other hYR subtypes. Furthermore receptor subtype co-expressing cells and selectively binding peptides revealed a receptor subtype selective internalization. By using novel hY(5)/hY(2) receptor chimera the receptor subtype dependent differences in hY receptor internalization could be identified on a molecular level.

journal_name

Cell Signal

journal_title

Cellular signalling

authors

Böhme I,Stichel J,Walther C,Mörl K,Beck-Sickinger AG

doi

10.1016/j.cellsig.2008.05.017

subject

Has Abstract

pub_date

2008-10-01 00:00:00

pages

1740-9

issue

10

eissn

0898-6568

issn

1873-3913

pii

S0898-6568(08)00161-7

journal_volume

20

pub_type

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