Avtor/Urednik		Rezaei, K; Saar, R; Soomets, U; Valkna, A; Naesman, J; Zorko, M; Akerman, K; Schroeder, T; Bartfai, T; Langel, U
Naslov		Role of third intracellular loop of galanin receptor type 1 in signal transduction
Tip		članek
Vir		Neuropeptides
Vol. in št.		Letnik 34, št. 1
Leto izdaje		2000
Obseg		str. 25-31
Jezik		eng
Abstrakt		To determine the domains essential for G-protein coupling of the human galanin receptor type 1 (GalR1), we have used both GalR1 mutants and synthetic receptor-derived peptides in 125I-galanin and (35S)-GTPyS binding studies. Replacement of potential phosphorylation sites by Leu in the third intracellular loop (IC3) of GalR1 did not affect KD values for the receptor. Peptides derived form the IC3 loop, and especially the N-terminal part of it were able to increase the rate of (35S)-GTPyS binding to the trimeric Gia1By2, but not to GsAB1y2, whereas the peptides corresponding to the IC1 and IC2 loops had no such effect. IC3 loop peptides also inhibited the binding of 125I-galanin to GalR1 in membranes from Rin m5F cells. Our results suggest that the IC3 loop of GalR1, especially its N-terminal part, defines the coupling of the receptor to the Gia1By2 protein and consequently, to the signal transduction cascade.
Deskriptorji		SIGNAL TRANSDUCTION G-PROTEINS GALANIN RECEPTORS, NEUROPEPTIDE GUANOSINE 5'-O-(3-THIOTRIPHOSPHATE) BINDING SITES PHOSPHORYLATION CELL LINE POINT MUTATION