ArticleCell research2023
Cryo-EM structures of human organic anion transporting polypeptide OATP1B1.
Article in Cell research, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 43 papers.
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Who cites it
43 citing papers in PubMed, 74 citations in OpenAlex.
- Hepatic drug transporters in pharmacotherapy: mechanisms, therapeutic targeting, and clinical translation.Naunyn-Schmiedeberg's archives of pharmacology · 2026Review
- Regulation of organic anion transporting polypeptide 1B1 transport function by lysine deacetylase 6.Molecular pharmacology · 2026Article
- Structures of the neutral amino acid transporter LAT4 provide insights into antitumor effects of its inhibitor tubeimoside-1.The EMBO journal · 2026Article
- Article
- Cryo-Structural Insights into Enzymatic Peptide Self-Assembly Driving Extrinsic Lytic Cell Death.Journal of the American Chemical Society · 2026Article
- Structural basis for prostaglandin and drug transport via SLCO2A1.Nature communications · 2026Article
- Contribution of organic anion transporting polypeptides to bile acid uptake in the Caco-2 cell monolayer and gastrointestinal tract.The Journal of biological chemistry · 2026Article
- Post-translational regulation of organic anion transporting polypeptide 1B3 transport function by lysine acetylation and lysine deacetylase 6 inhibition.Drug metabolism and disposition: the biological fate of chemicals · 2026Article
- A conserved salt bridge network stabilizes the hepatic organic anion transporters OATP1B1 and OATP1B3.The Journal of biological chemistry · 2026Article
- Article
- p16EMBO reports · 2026Article
- Review
- Article
- The SLC-ome of membrane transport: From molecular discovery to physiology and clinical applications.Physiological reviews · 2025Review
- Hepatic uptake of estradiol-3-glucuronide and estradiol-3-sulfate-17β-glucuronide by human organic anion transporting polypeptides 1B1, 1B3, and 2B1.Drug metabolism and disposition: the biological fate of chemicals · 2025Article
- Structure and transport mechanism of the human prostaglandin transporter SLCO2A1.Nature communications · 2025Article
- Cryo-EM ligand building using AlphaFold3-like model and molecular dynamics.PLoS computational biology · 2025Article
- Structure and post-translational modification of the prostaglandin transporter.Communications biology · 2025Article
- Molecular chameleons adaptability in target binding.Structural dynamics (Melville, N.Y.) · 2025Article
- The Effect of Radixin on the Function and Expression of Organic Anion Transporting Polypeptide 1B1.Biology · 2025Article
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Authors and funding
11 authors at 4 institutions in 2 countries.
Funding
Abstract
Members of the solute carrier organic anion transporting polypeptide (OATPs) family function as transporters for a large variety of amphipathic organic anions including endogenous metabolites and clinical drugs, such as bile salts, steroids, thyroid hormones, statins, antibiotics, antivirals, and anticancer drugs. OATP1B1 plays a vital role in transporting such substances into the liver for hepatic clearance. FDA and EMA recommend conducting in vitro testing of drug-drug interactions (DDIs) involving OATP1B1. However, the structure and working mechanism of OATPs still remains elusive. In this study, we determined cryo-EM structures of human OATP1B1 bound with representative endogenous metabolites (bilirubin and estrone-3-sulfate), a clinical drug (simeprevir), and a fluorescent indicator (2',7'-dichlorofluorescein), in both outward- and inward-open states. These structures reveal major and minor substrate binding pockets and conformational changes during transport. In combination with mutagenesis studies and molecular dynamics simulations, our work comprehensively elucidates the transport mechanism of OATP1B1 and provides the structural basis for DDI predictions involving OATP1B1, which will greatly promote our understanding of OATPs.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.