Evidence map›Paper›PMID 32143347›Full record

ArticleCells2020

The Pyrazolo[3,4-d]pyrimidine Derivative, SCO-201, Reverses Multidrug Resistance Mediated by ABCG2/BCRP.

Sophie E B Ambjørner, Michael Wiese, Sebastian Christoph Köhler, Joen Svindt, Xamuel Loft Lund, Michael Gajhede, Lasse Saaby, Birger Brodin, Steffen Rump, Henning Weigt and 2 more

Open access · goldAbstract read
In one paragraph

Article in Cells, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.

0numbers the graph read from it
0cells of the map it votes in
11citing papers in PubMed
1.3field-weighted citation impact, top 18% of its field
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

11 citing papers in PubMed, 36 citations in OpenAlex.

  1. Review
  2. Inhibition of ABCG2 by SCO-101 Enhances Chemotherapy Efficacy in Cancer.International journal of molecular sciences · 2025
    Article
  3. Article
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  5. Review
  6. Article
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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 at 3 institutions in 2 countries.

Sophie E B AmbjørnerDepartment of Drug Design and Pharmacology, University of Copenhagen, 1165 Copenhagen, Denmark.
Michael WiesePharmaceutical Institute, University of Bonn, 53113 Bonn, Germany.
Sebastian Christoph KöhlerPharmaceutical Institute, University of Bonn, 53113 Bonn, Germany.
Joen SvindtDepartment of Biology, University of Copenhagen, 1165 Copenhagen, Denmark.
Xamuel Loft LundDepartment of Drug Design and Pharmacology, University of Copenhagen, 1165 Copenhagen, Denmark.
Michael GajhedeDepartment of Drug Design and Pharmacology, University of Copenhagen, 1165 Copenhagen, Denmark.
Lasse SaabyDepartment of Pharmacy, University of Copenhagen, 1165 Copenhagen, Denmark.
Birger BrodinDepartment of Pharmacy, University of Copenhagen, 1165 Copenhagen, Denmark.
Steffen RumpSRConsulting, 31319 Sehnde, Germany.
Henning WeigtDivision of Chemical Safety and Toxicity, Fraunhofer Institute of Toxicology and Experimental Medicine, 30625 Hannover, Germany.
Nils BrünnerDepartment of Drug Design and Pharmacology, University of Copenhagen, 1165 Copenhagen, Denmark.
Jan StenvangDepartment of Drug Design and Pharmacology, University of Copenhagen, 1165 Copenhagen, Denmark.
University of Copenhagen · DKUniversity of Bonn · DEFraunhofer Institute for Toxicology and Experimental Medicine · DE

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

ATP-binding cassette (ABC) transporters, such as breast cancer resistance protein (BCRP), are key players in resistance to multiple anti-cancer drugs, leading to cancer treatment failure and cancer-related death. Currently, there are no clinically approved drugs for reversal of cancer drug resistance caused by ABC transporters. This study investigated if a novel drug candidate, SCO-201, could inhibit BCRP and reverse BCRP-mediated drug resistance. We applied in vitro cell viability assays in SN-38 (7-Ethyl-10-hydroxycamptothecin)-resistant colon cancer cells and in non-cancer cells with ectopic expression of BCRP. SCO-201 reversed resistance to SN-38 (active metabolite of irinotecan) in both model systems. Dye efflux assays, bidirectional transport assays, and ATPase assays demonstrated that SCO-201 inhibits BCRP. In silico interaction analyses supported the ATPase assay data and suggest that SCO-201 competes with SN-38 for the BCRP drug-binding site. To analyze for inhibition of other transporters or cytochrome P450 (CYP) enzymes, we performed enzyme and transporter assays by in vitro drug metabolism and pharmacokinetics studies, which demonstrated that SCO-201 selectively inhibited BCRP and neither inhibited nor induced CYPs. We conclude that SCO-201 is a specific, potent, and potentially non-toxic drug candidate for the reversal of BCRP-mediated resistance in cancer cells.

Indexed as

Antineoplastic AgentsATP-Binding Cassette TransportersATP Binding Cassette Transporter, Subfamily G, Member 2Biological TransportCell Line, TumorDrug Resistance, MultipleDrug Resistance, NeoplasmHumansIrinotecanNeoplasm ProteinsAntineoplastic AgentsATP-Binding Cassette TransportersATP Binding Cassette Transporter, Subfamily G, Member 2IrinotecanNeoplasm ProteinsATP-binding cassette transporterbreast cancer resistance protein (BCRP), ABCG2drug efflux pumpsmultidrug resistance in cancerpyrazolo-pyrimidine derivativeSCO-201

Identifiers

PMID32143347
PMCPMC7140522
OpenAlexW3009348364

What OpenQuestion holds

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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 OpenQuestion graph.