6H7M

ACTIVATED TURKEY BETA1 ADRENOCEPTOR WITH BOUND PARTIAL AGONIST SALBUTAMOL AND NANOBODY Nb6B9

6H7M の概要

• エントリーDOI: 10.2210/pdb6h7m/pdb
• 分子名称: Thioredoxin 1, Beta-1 adrenergic receptor, Camelid antibody fragment Nb6B9, ... (7 entities in total)
• 機能のキーワード: beta1 adrenoceptor, activated, partial agonist, nanobody, immune system
• 由来する生物種: Escherichia coli (strain K12); 詳細
• タンパク質・核酸の鎖数: 6
• 化学式量合計: 122828.23

構造登録者

Warne, T.,Edwards, P.C.,Dore, A.S.,Leslie, A.G.W.,Tate, C.G. (登録日: 2018-07-31, 公開日: 2018-10-17, 最終更新日: 2024-01-17)

主引用文献

Warne, T.,Edwards, P.C.,Dore, A.S.,Leslie, A.G.W.,Tate, C.G.
Molecular basis for high-affinity agonist binding in GPCRs.
Science, 364:775-778, 2019

PubMed Abstract: G protein-coupled receptors (GPCRs) in the G protein-coupled active state have higher affinity for agonists as compared with when they are in the inactive state, but the molecular basis for this is unclear. We have determined four active-state structures of the β-adrenoceptor (βAR) bound to conformation-specific nanobodies in the presence of agonists of varying efficacy. Comparison with inactive-state structures of βAR bound to the identical ligands showed a 24 to 42% reduction in the volume of the orthosteric binding site. Potential hydrogen bonds were also shorter, and there was up to a 30% increase in the number of atomic contacts between the receptor and ligand. This explains the increase in agonist affinity of GPCRs in the active state for a wide range of structurally distinct agonists.

PubMed: 31072904
DOI: 10.1126/science.aau5595

実験手法

X-RAY DIFFRACTION (2.76 Å)