Single Stabilizing Point Mutation Enables High-Resolution Co-Crystal Structures of the Adenosine A2A Receptor with Preladenant Conjugates,Angewandte Chemie International Edition

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Single Stabilizing Point Mutation Enables High-Resolution Co-Crystal Structures of the Adenosine A2A Receptor with Preladenant Conjugates
Angewandte Chemie International Edition ( IF 16.1 ) Pub Date : 2022-02-17 , DOI: 10.1002/anie.202115545
Tobias Claff ₁ , Tim A Klapschinski ₁ , Udaya K Tiruttani Subhramanyam _{2,

3} , Victoria J Vaaßen ₁ , Jonathan G Schlegel ₁ , Christin Vielmuth ₁ , Jan H Voß ₁ , Jörg Labahn _{2,

3} , Christa E Müller ₁

Affiliation

A super-stable adenosine A_2A receptor (A_2AAR) containing a single point mutation in the transmembrane regions was developed by imitating an allosteric Na⁺ through introduction of a basic amino acid residue. This allowed the determination of high-resolution co-crystal structures with newly designed PEGylated and fluorophore-labeled Preladenant derivatives, which belong to the most potent A_2AAR antagonists endowed with outstanding selectivity.

中文翻译：

单稳定点突变使腺苷 A2A 受体与 Preladenant 缀合物的高分辨率共晶结构成为可能

通过引入碱性氨基酸残基模拟变构Na ⁺，开发了在跨膜区域包含单点突变的超稳定腺苷A _2A受体（A _{2A AR）。}这允许使用新设计的聚乙二醇化和荧光团标记的 Preladenant 衍生物测定高分辨率共晶结构，这些衍生物属于最有效的 A _2A AR 拮抗剂，具有出色的选择性。

更新日期：2022-02-17

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