| Item type |
デフォルトアイテムタイプ_（フル）(1) |
| 公開日 |
2023-03-18 |
| タイトル |
|
|
タイトル |
Distinct roles of the DRY motif in rat melanin-concentrating hormone receptor 1 in signaling control |
|
言語 |
en |
| 作成者 |
Aizaki, Yoshimi
Maruyama, Kei
Nakano-Tetsuka, Mitsue
Saito, Yumiko
|
| アクセス権 |
|
|
アクセス権 |
open access |
|
アクセス権URI |
http://purl.org/coar/access_right/c_abf2 |
| 権利情報 |
|
|
権利情報 |
Copyright (c) 2009 Elsevier Inc. |
| 主題 |
|
|
主題Scheme |
Other |
|
主題 |
G protein-coupled receptor |
| 主題 |
|
|
主題Scheme |
Other |
|
主題 |
DRY motif |
| 主題 |
|
|
主題Scheme |
Other |
|
主題 |
Melanin-concentrating hormone |
| 主題 |
|
|
主題Scheme |
Other |
|
主題 |
Calcium influx |
| 主題 |
|
|
主題Scheme |
Other |
|
主題 |
Site-directed mutagenesis |
| 主題 |
|
|
主題Scheme |
Other |
|
主題 |
Constitutive activation |
| 主題 |
|
|
主題Scheme |
NDC |
|
主題 |
460 |
| 内容記述 |
|
|
内容記述 |
Rhodopsin family (class A) G protein-coupled receptors possess common key residues or motifs that appear to be important for receptor function. To clarify the roles of the highly conserved amino acid triplet Asp3.49-Arg3.50-Tyr3.51 (DRY motif), we examined how single-substitution mutations of the amino acids in the motif influenced specific features of rat melanin-concentrating hormone receptor 1 (MCH1R) activity. Substitution of either Asp1403.49 or Tyr1423.51 to Ala resulted in nonfunctional receptors, despite the retention of apparent potencies for agonist binding. These loss-of-function phenotypes may be caused by the lack of stimulation for GDP-GTP exchange observed in GTPγS-binding assays. On the other hand, substitution of Arg1413.50 to Ala caused a 4-fold reduction in the agonist binding affinity and, concomitantly, a rightward shift of the dose-dependency curve for calcium mobilization and inhibition of cyclic AMP production. Although many experimental studies have suggested that the DRY motif is involved in maintaining the receptor in its ground state, none of the DRY motif substitutions to Ala in MCH1R led to constitutive activation, in terms of the basal signaling level for ERK1/2 activation or GTPγS binding. These data suggest that the major contribution of the DRY motif in MCH1R is to govern receptor conformation and G protein coupling/recognition. |
|
言語 |
en |
| 出版者 |
|
|
出版者 |
Elsevier Science Inc. |
| 言語 |
|
|
言語 |
eng |
| 資源タイプ |
|
|
資源タイプ識別子 |
http://purl.org/coar/resource_type/c_6501 |
|
資源タイプ |
journal article |
| 出版タイプ |
|
|
出版タイプ |
AO |
|
出版タイプResource |
http://purl.org/coar/version/c_b1a7d7d4d402bcce |
| 関連情報 |
|
|
|
識別子タイプ |
DOI |
|
|
関連識別子 |
10.1016/j.peptides.2009.01.017 |
| 関連情報 |
|
|
|
識別子タイプ |
DOI |
|
|
関連識別子 |
http://dx.doi.org/10.1016/j.peptides.2009.01.017 |
| 収録物識別子 |
|
|
収録物識別子タイプ |
ISSN |
|
収録物識別子 |
0196-9781 |
| 収録物識別子 |
|
|
収録物識別子タイプ |
NCID |
|
収録物識別子 |
AA10617807 |
| 開始ページ |
|
|
開始ページ |
974 |
| 書誌情報 |
Peptides
Peptides
巻 30,
号 5,
p. 974-981,
発行日 2009-05
|
| 旧ID |
26023 |
Peptides_2009_01_017.pdf (8.0 MB)
