Evidence mapPaperPMID 40199401Full record

ArticleThe Journal of biological chemistry2025

Cyclosporine A sterically inhibits statin transport by solute carrier OATP1B1.

Min Woo Sung, Kuan Hu, Lea M Hurlimann, Joshua A Lees, Kimberly F Fennell, Mark A West, Chester Costales, Amilcar David Rodrigues, Iwan Zimmermann, Roger J P Dawson and 2 more

Abstract read
In one paragraph

Article in The Journal of biological chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

4 citing papers in PubMed.

  1. Article
  2. Article
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  4. Review
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

12 authors.

Min Woo SungDiscovery Sciences, Discovery & Early Development, Pfizer Inc, Groton, Connecticut, USA.
Kuan HuDiscovery Sciences, Discovery & Early Development, Pfizer Inc, Groton, Connecticut, USA.
Lea M HurlimannLinkster Therapeutics AG, Zurich, Switzerland.
Joshua A LeesDiscovery Sciences, Discovery & Early Development, Pfizer Inc, Groton, Connecticut, USA.
Kimberly F FennellDiscovery Sciences, Discovery & Early Development, Pfizer Inc, Groton, Connecticut, USA.
Mark A WestPharmacokinetics, Dynamics, and Metabolism, Discovery & Early Development, Pfizer Inc, Groton, Connecticut, USA.
Chester CostalesPharmacokinetics, Dynamics, and Metabolism, Discovery & Early Development, Pfizer Inc, Groton, Connecticut, USA.
Amilcar David RodriguesPharmacokinetics, Dynamics, and Metabolism, Discovery & Early Development, Pfizer Inc, Groton, Connecticut, USA.
Iwan ZimmermannLinkster Therapeutics AG, Zurich, Switzerland.
Roger J P DawsonLinkster Therapeutics AG, Zurich, Switzerland.
Shenping LiuDiscovery Sciences, Discovery & Early Development, Pfizer Inc, Groton, Connecticut, USA. Electronic address: shenping.liu@pfizer.com.
Seungil HanDiscovery Sciences, Discovery & Early Development, Pfizer Inc, Groton, Connecticut, USA. Electronic address: seungil.han@pfizer.com.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Members of the Organic Anion Transporter Polypeptides (OATP) are integral membrane proteins responsible for facilitating the transport of organic anions across the cell membrane. OATP1B1 (SLCO1B1), the prototypic OATP family member, is the most abundant uptake transporter in the liver and a key mediator of the hepatic uptake and clearance of numerous endogenous and xenobiotic compounds. It serves as a locus of important drug-drug interactions, such as those between statins and cyclosporine A, and carries the potential to enable liver-targeting therapeutics. In this study, we report cryo-EM structures of OATP1B1 and its complexes with one of its statin substrates, atorvastatin, and an inhibitor, cyclosporine A. This structural analysis has yielded insights into the mechanisms underlying the OATP1B1-mediated transport of statins and the inhibitory effect of cyclosporine A. These findings contribute to a better understanding of the molecular processes involved in drug transport and offer potential avenues for the development of targeted medications for liver-related conditions.

Indexed as

AtorvastatinCyclosporineHydroxymethylglutaryl-CoA Reductase InhibitorsLiver-Specific Organic Anion Transporter 1Biological TransportHEK293 CellsHumansAtorvastatinCyclosporineHydroxymethylglutaryl-CoA Reductase InhibitorsLiver-Specific Organic Anion Transporter 1SLCO1B1 protein, humancryo-electron microscopydrug transportmembrane proteinorganic anion channeltransporter

Identifiers

PMID40199401
PMCPMC12127550

What Socratic holds

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LicenceCC BY-NC-ND
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Registered trials

None linked

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 Socratic graph.