7C61

Crystal structure of 5-HT1B-BRIL and SRP2070_Fab complex

7C61 の概要

• エントリーDOI: 10.2210/pdb7c61/pdb
• 分子名称: IGG LIGHT CHAIN, IGG HEAVY CHAIN, 5-hydroxytryptamine receptor 1B,Soluble cytochrome b562,5-hydroxytryptamine receptor 1B, ... (4 entities in total)
• 機能のキーワード: gpcr, bril, crystallization, antibody, signaling protein
• 由来する生物種: Mus musculus; 詳細
• タンパク質・核酸の鎖数: 3
• 化学式量合計: 104615.00

構造登録者

Suzuki, M.,Miyagi, H.,Asada, H.,Yasunaga, M.,Suno, C.,Takahashi, Y.,Saito, J.,Iwata, S. (登録日: 2020-05-21, 公開日: 2020-07-29, 最終更新日: 2024-10-23)

主引用文献

Miyagi, H.,Asada, H.,Suzuki, M.,Takahashi, Y.,Yasunaga, M.,Suno, C.,Iwata, S.,Saito, J.I.
The discovery of a new antibody for BRIL-fused GPCR structure determination.
Sci Rep, 10:11669-11669, 2020

PubMed Abstract: G-protein-coupled receptors (GPCRs)-the largest family of cell-surface membrane proteins-mediate the intracellular signal transduction of many external ligands. Thus, GPCRs have become important drug targets. X-ray crystal structures of GPCRs are very useful for structure-based drug design (SBDD). Herein, we produced a new antibody (SRP2070) targeting the thermostabilised apocytochrome b562 from Escherichia coli M7W/H102I/R106L (BRIL). We found that a fragment of this antibody (SRP2070Fab) facilitated the crystallisation of the BRIL-tagged, ligand bound GPCRs, 5HT and ATR. Furthermore, the electron densities of the ligands were resolved, suggesting that SPR2070Fab is versatile and adaptable for GPCR SBDD. We anticipate that this new tool will significantly accelerate structure determination of other GPCRs and the design of small molecular drugs targeting them.

PubMed: 32669569
DOI: 10.1038/s41598-020-68355-x

実験手法

X-RAY DIFFRACTION (3 Å)