6RZ6

Crystal structure of the human cysteinyl leukotriene receptor 2 in complex with ONO-2570366 (C2221 space group)

6RZ6 の概要

• エントリーDOI: 10.2210/pdb6rz6/pdb
• 分子名称: Cysteinyl leukotriene receptor 2,Soluble cytochrome b562,Cysteinyl leukotriene receptor 2, (2~{S})-8-[[4-[4-(2-chloranyl-5-fluoranyl-phenyl)butoxy]phenyl]carbonylamino]-4-(4-oxidanyl-4-oxidanylidene-butyl)-2,3- dihydro-1,4-benzoxazine-2-carboxylic acid, CHOLESTEROL, ... (8 entities in total)
• 機能のキーワード: gpcr, lcp, membrane protein, cysteinyl leukotriene, cyslt2, cysltr2, cyslt2r, asthma, bril, cysteinyl leukotriene receptor 2
• 由来する生物種: Homo sapiens (Human); 詳細
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 55885.25

構造登録者

Gusach, A.,Luginina, A.,Marin, E.,Brouillette, R.L.,Besserer-Offroy, E.,Longpre, J.M.,Ishchenko, A.,Popov, P.,Fujimoto, T.,Maruyama, T.,Stauch, B.,Ergasheva, M.,Romanovskaya, D.,Stepko, A.,Kovalev, K.,Shevtsov, M.,Gordeliy, V.,Han, G.W.,Sarret, P.,Katritch, V.,Borshchevskiy, V.,Mishin, A.,Cherezov, V. (登録日: 2019-06-12, 公開日: 2019-12-11, 最終更新日: 2024-11-06)

主引用文献

Gusach, A.,Luginina, A.,Marin, E.,Brouillette, R.L.,Besserer-Offroy, E.,Longpre, J.M.,Ishchenko, A.,Popov, P.,Patel, N.,Fujimoto, T.,Maruyama, T.,Stauch, B.,Ergasheva, M.,Romanovskaia, D.,Stepko, A.,Kovalev, K.,Shevtsov, M.,Gordeliy, V.,Han, G.W.,Katritch, V.,Borshchevskiy, V.,Sarret, P.,Mishin, A.,Cherezov, V.
Structural basis of ligand selectivity and disease mutations in cysteinyl leukotriene receptors.
Nat Commun, 10:5573-5573, 2019

PubMed Abstract: Cysteinyl leukotriene G protein-coupled receptors CysLT and CysLT regulate pro-inflammatory responses associated with allergic disorders. While selective inhibition of CysLTR has been used for treating asthma and associated diseases for over two decades, CysLTR has recently started to emerge as a potential drug target against atopic asthma, brain injury and central nervous system disorders, as well as several types of cancer. Here, we describe four crystal structures of CysLTR in complex with three dual CysLTR/CysLTR antagonists. The reported structures together with the results of comprehensive mutagenesis and computer modeling studies shed light on molecular determinants of CysLTR ligand selectivity and specific effects of disease-related single nucleotide variants.

PubMed: 31811124
DOI: 10.1038/s41467-019-13348-2

実験手法

X-RAY DIFFRACTION (2.43 Å)