EMDB/PDB/SASBDBから引用されている文献のデータベース

キーワード
構造解析手法	All X線回折 NMR 電子顕微鏡小角散乱中性子線回折線維回折粉末回折赤外分光 EPR FRET 理論モデルハイブリッド
著者・登録者
ジャーナル
IF	>30 >20 >10 >5 all

タイトル	Structural basis for prostaglandin and drug transport via SLCO2A1.
ジャーナル・号・ページ	Nat Commun, Vol. 17, Issue 1, Year 2026
掲載日	2026年3月20日
著者	Chitra Joshi / Justin C Deme / Yoshinobu Nakamura / Wei-Tse Hsu / Jonathan D Goult / Takafumi Kato / Joanne L Parker / Philip C Biggin / Susan M Lea / Takeo Nakanishi / Simon Newstead /
PubMed 要旨	Organic anion-transporting polypeptide transporters (SLCO/OATPs) function as cellular gatekeepers, regulating intestinal absorption, hepatic and renal clearance, and the tissue distribution of drugs ...Organic anion-transporting polypeptide transporters (SLCO/OATPs) function as cellular gatekeepers, regulating intestinal absorption, hepatic and renal clearance, and the tissue distribution of drugs and metabolites in the human body. However, the mechanisms underlying substrate selection within the SLCO superfamily remain unclear, hampering efforts to rationalize the interaction of drugs and metabolites with these transporters. SLCO2A1 (also known as OATP2A1) is responsible for the distribution of eicosanoids, including prostaglandins (PGs) and thromboxanes, throughout the body, in addition to several families of nonsteroidal anti-inflammatory drugs (NSAIDs). Here, we present cryogenic electron microscopy structures of SLCO2A1 bound to endogenous PGs and to four widely prescribed medications for treating inflammation, chronic asthma, and Parkinson's disease (PD). Complementary molecular dynamics and in vivo cellular assays elucidate the molecular basis for PG and drug recognition. Our study reports essential mechanistic details that underpin substrate selection and subfamily adaptation within the broader SLCO superfamily of drug and metabolite transporters.
リンク	Nat Commun / PubMed:41862483 / PubMed Central
手法	EM (単粒子)
解像度	2.9 - 3.4 Å
構造データ	53472 9qzo EMDB-53472, PDB-9qzo: Cryo-EM structure of rat SLCO2A1 in the apo state. 手法: EM (単粒子) / 解像度: 2.9 Å 53481 9r07 EMDB-53481, PDB-9r07: Cryo-EM structure of rat SLCO2A1 bound to zafirlukast. 手法: EM (単粒子) / 解像度: 3.2 Å 53482 9r0a EMDB-53482, PDB-9r0a: Cryo-EM structure of rat SLCO2A1 bound to fentiazac. 手法: EM (単粒子) / 解像度: 3.1 Å 53483 9r0i EMDB-53483, PDB-9r0i: Cryo-EM structure of rat SLCO2A1 bound to losartan. 手法: EM (単粒子) / 解像度: 3.1 Å 53484 9r0m EMDB-53484, PDB-9r0m: Cryo-EM structure of rat SLCO2A1 bound to prostaglandin E2. 手法: EM (単粒子) / 解像度: 3.2 Å 53485 9r0n EMDB-53485, PDB-9r0n: Cryo-EM structure of rat SLCO2A1 bound to dinoprost. 手法: EM (単粒子) / 解像度: 3.4 Å 53486 9r0o EMDB-53486, PDB-9r0o: Cryo-EM structure of rat SLCO2A1 bound to tolcapone. 手法: EM (単粒子) / 解像度: 3.1 Å
化合物	ChemComp-Y01: CHOLESTEROL HEMISUCCINATE / コレステリルヘミスクシナ-ト ChemComp-ZLK: zafirlukast / ザフィルルカスト / アンタゴニストYM PDB-1jbl: Solution structure of SFTI-1, A cyclic trypsin inhibitor from sunflower seeds ChemComp-AV0: Lauryl Maltose Neopentyl Glycol / ラウリルマルト-スネオペンチルグリコ-ル ChemComp-LSN: [2-butyl-5-chloranyl-3-[[4-[2-(2H-1,2,3,4-tetrazol-5-yl)phenyl]phenyl]methyl]imidazol-4-yl]methanol / ロサルタン ChemComp-P2E: (Z)-7-[(1R,2R,3R)-3-hydroxy-2-[(E,3S)-3-hydroxyoct-1-enyl]-5-oxo-cyclopentyl]hept-5-enoic acid / プロスタグランジンE₂ / 薬剤YM ChemComp-UGU: (Z)-7-[(1R,2R,3R,5S)-3,5-bis(oxidanyl)-2-[(E,3S)-3-oxidanyloct-1-enyl]cyclopentyl]hept-5-enoic acid / プロスタグランジンF_2α / ホルモンYM ChemComp-TCW: Tolcapone / 薬剤, 阻害剤YM
由来	rattus norvegicus (ドブネズミ)
キーワード	MEMBRANE PROTEIN / OATP2A1 / plasma membrane localized / prostaglandin transporter / PGT / major facilitator superfamily. / plasma membrane localised