9R0M

Cryo-EM structure of rat SLCO2A1 bound to prostaglandin E2.

9R0M の概要

• エントリーDOI: 10.2210/pdb9r0m/pdb
• EMDBエントリー: 53484
• 分子名称: Solute carrier organic anion transporter family member 2A1, (Z)-7-[(1R,2R,3R)-3-hydroxy-2-[(E,3S)-3-hydroxyoct-1-enyl]-5-oxo-cyclopentyl]hept-5-enoic acid, CHOLESTEROL HEMISUCCINATE (3 entities in total)
• 機能のキーワード: oatp2a1, plasma membrane localized, prostaglandin transporter, pgt, major facilitator superfamily., membrane protein
• 由来する生物種: Rattus norvegicus (Norway rat)
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 73454.31

構造登録者

Deme, J.C.,Goult, J.,Lea, S.M.,Newstead, S. (登録日: 2025-04-24, 公開日: 2026-02-11, 最終更新日: 2026-04-01)

主引用文献

Joshi, C.,Deme, J.C.,Nakamura, Y.,Hsu, W.T.,Goult, J.D.,Kato, T.,Parker, J.L.,Biggin, P.C.,Lea, S.M.,Nakanishi, T.,Newstead, S.
Structural basis for prostaglandin and drug transport via SLCO2A1.
Nat Commun, 17:-, 2026

PubMed Abstract: 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.

PubMed: 41862483
DOI: 10.1038/s41467-026-70227-3

実験手法

ELECTRON MICROSCOPY (3.2 Å)