9FXM

TRPC4 in complex with Z-AzPico

これはPDB形式変換不可エントリーです。

9FXM の概要

• エントリーDOI: 10.2210/pdb9fxm/pdb
• 関連するPDBエントリー: 9FXL
• EMDBエントリー: 50851
• 分子名称: Transient receptor potential cation channel subfamily c member 4a, (Z)-7-(4-chlorobenzyl)-1-(3-hydroxypropyl)-3-methyl-8-(4-(phenyldiazenyl)-3-(trifluoromethoxy)phenoxy)-3,7-dihydro-1H-purine-2,6-dione (2 entities in total)
• 機能のキーワード: transport protein, calcium channel, membrane protein
• 由来する生物種: Danio rerio (zebrafish)
• タンパク質・核酸の鎖数: 4
• 化学式量合計: 435640.01

構造登録者

Vinayagam, D.,Raunser, S. (登録日: 2024-07-01, 公開日: 2025-07-09, 最終更新日: 2026-01-28)

主引用文献

Muller, M.,Niemeyer, K.,Ojha, N.K.,Porav, S.A.,Vinayagam, D.,Urban, N.,Buchau, F.,Oleinikov, K.,Makke, M.,Bauer, C.C.,Johnson, A.V.,Muench, S.P.,Zufall, F.,Bruns, D.,Schwarz, Y.,Raunser, S.,Leinders-Zufall, T.,Bon, R.S.,Schaefer, M.,Thorn-Seshold, O.
Ideal efficacy photoswitching for chromocontrol of TRPC4/5 channel functions in live tissues.
Nat.Chem.Biol., 2026

PubMed Abstract: Precisely probing the endogenous roles of target proteins is crucial for biological research. Photochemical tools can be photoactuated with high spatiotemporal resolution but often they are unreliable in vivo because spatiotemporal variations of reagent concentration result in inhomogeneous bioactivity. We now describe ideal efficacy photoswitching, a paradigm that internally compensates for reagent concentration by self-competitive binding, allowing purely wavelength-dependent chromocontrol over bioactivity that is consistent from cell culture to deep tissues. We demonstrate this with photoswitches for endogenous transient receptor potential (TRP) C4 and C5 ion channels, reproducibly delivering strong agonism under 360-nm illumination, weak agonism under 385-nm illumination and strong antagonism under 440-nm illumination. These ligands unlock a range of high-precision investigations in TRP biology, from neuronal activity to exocytosis, reproductive signaling and smooth muscle contractility. The ideal efficacy photoswitching paradigm should also unlock high-performance chromocontrol over a wide range of sensory or signaling channels and receptors even in vivo.

PubMed: 41545580
DOI: 10.1038/s41589-025-02085-x

実験手法

ELECTRON MICROSCOPY (3.1 Å)