1LVR

IC3 of CB1 (L431A,A432L) Bound to G(alpha)i

1LVR の概要

• エントリーDOI: 10.2210/pdb1lvr/pdb
• 関連するPDBエントリー: 1LVQ
• 分子名称: Cannabinoid receptor 1 (1 entity in total)
• 機能のキーワード: intracellular loop 3 (ic3), cannabinoid 1 receptor (cb1), alpha domain of g protein i, transferred noes, signaling protein
• 細胞内の位置: Cell membrane; Multi-pass membrane protein: P21554
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 1030.26

構造登録者

Ulfers, A.L.,McMurry, J.L.,Miller, A.,Wang, L.,Kendall, D.A.,Mierke, D.F. (登録日: 2002-05-29, 公開日: 2002-12-11, 最終更新日: 2024-05-22)

主引用文献

Ulfers, A.L.,McMurry, J.L.,Miller, A.,Wang, L.,Kendall, D.A.,Mierke, D.F.
Cannabinoid receptor-G protein interactions: G(alphai1)-bound structures of IC3 and a mutant with altered G protein specificity.
Protein Sci., 11:2526-2531, 2002

PubMed Abstract: The structure of the C-terminal region of the third cytoplasmic loop (IC3) of the cannabinoid receptor one (CB1) bound to G(alphai1) has been determined using transferred nuclear Overhauser effects (NOEs). The wild-type IC3 sequence is helical when associated with G(alphai1). In contrast, a peptide containing the amino-acid inversion, Ala(341)-Leu(342) adopts a single turn. These findings correlate with the attenuated G(i) association of CB1 with the Ala(341)-Leu(342) mutation previously observed in vivo and the diminished stimulation of G(alphai1) GTPase activity by the corresponding peptide demonstrated in vitro here. These results, the first to report the structure of a GPCR domain while associated with G protein, imply the C-terminus of CB1 IC3, a region with high-sequence conservation among G-protein coupled receptors, must be helical for efficient coupling and activation of the G(i) protein.

PubMed: 12237474
DOI: 10.1110/ps.0218402

実験手法

SOLUTION NMR