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9K20

Cryo-EM structure of ATP-bound P2Y purinoceptor 2-miniGo-scFv16 complex

9K20 の概要
エントリーDOI10.2210/pdb9k20/pdb
EMDBエントリー61986
分子名称P2Y purinoceptor 2, Guanine nucleotide-binding protein G(o) subunit alpha, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, ... (6 entities in total)
機能のキーワードg protein-coupled receptors, g-protein signaling, nucleotide receptors, membrane protein
由来する生物種Homo sapiens (human)
詳細
タンパク質・核酸の鎖数5
化学式量合計150873.33
構造登録者
Lan, B.,Zhang, S.,Liu, X.,Lin, B. (登録日: 2024-10-16, 公開日: 2025-06-11, 最終更新日: 2025-07-16)
主引用文献Lan, B.,Zhang, S.,Chen, K.,Dai, S.,Fei, J.,Gao, K.,Sun, X.,Lin, B.,Liu, X.
Structural insight into the self-activation and G-protein coupling of P2Y2 receptor.
Cell Discov, 11:47-47, 2025
Cited by
PubMed Abstract: Purinergic P2Y2 receptor (P2Y2R) represents a typically extracellular ATP and UTP sensor for mediating purinergic signaling. Despite its importance as a pharmacological target, the molecular mechanisms underlying ligand recognition and G-protein coupling have remained elusive due to lack of structural information. In this study, we determined the cryo-electron microscopy (cryo-EM) structures of the apo P2Y2R in complex with G, ATP-bound P2Y2R in complex with G or G, and UTP-bound P2Y4R in complex with G. These structures reveal the similarities and distinctions of ligand recognition within the P2Y receptor family. Furthermore, a comprehensive analysis of G-protein coupling reveals that P2Y2R exhibits promiscuity in coupling with both G and G proteins. Combining molecular dynamics simulations and signaling assays, we elucidate the molecular mechanisms by which P2Y2R differentiates pathway-specific G or G coupling through distinct structural components on the intracellular side. Strikingly, we identify a helix-like segment within the N-terminus that occupies the orthosteric ligand-binding pocket of P2Y2R, accounting for its self-activation. Taken together, these findings provide a molecular framework for understanding the activation mechanism of P2Y2R, encompassing ligand recognition, G-protein coupling, and a novel N-terminus-mediated self-activation mechanism.
PubMed: 40360475
DOI: 10.1038/s41421-025-00797-x
主引用文献が同じPDBエントリー
実験手法
ELECTRON MICROSCOPY (2.65 Å)
構造検証レポート
Validation report summary of 9k20
検証レポート(詳細版)ダウンロードをダウンロード

243531

件を2025-10-22に公開中

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