ArticleNature communications2020
ABCG2 transports anticancer drugs via a closed-to-open switch.
Article in Nature communications, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 101 papers.
What it found
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Who cites it
101 citing papers in PubMed, 208 citations in OpenAlex.
- Identification of the Acetamide-Chalcone Derivative That Selectively Inhibits ABCG2 Transport Activity.ACS omega · 2026Article
- Capivasertib Combines with Trastuzumab Deruxtecan to Enhance Antitumor Activity in HER2-Positive and HER2-Low Tumors.Molecular cancer therapeutics · 2026Article
- Review
- Structure and druggable conformation of the homodimeric lipoprotein transporter of Acinetobacter baumannii.Nature communications · 2026Article
- Natural Coumarins Galbanic Acid and Auraptene Improved the Efficacy of Alkeran on Human Osteosarcoma Cells by Targeting ABC Transporters.Chemistry & biodiversity · 2026Article
- ABCG2 Genetic Variability in Drug Exposure and Toxicity: Implications for Clinical Practice.Toxics · 2026Review
- Article
- Biotransformation of Maclekarpine E in Rats: CYP2C19-Mediated Metabolism, Fecal Enrichment, and Network Pharmacology-Based Anti-Ulcerative Colitis Prediction.Current issues in molecular biology · 2026Article
- Polymethoxylated N-Carboranyl Isoquinolinones: A New Scaffold for ABCG2 Inhibitors.ChemMedChem · 2026Article
- Novel Dorsomorphin Derivatives: Molecular Modeling, Synthesis, and Bioactivity Evaluation.Biomolecules · 2026Article
- Pan-cancer multi-omics analysis of pharmacogenomic alterations.Frontiers in bioinformatics · 2026Article
- Liver enzyme elevations during statin-ezetimibe therapy inFrontiers in pharmacology · 2026Article
- Transcriptomic studies on the product stress response revealed that YCF1 is a beneficial factor for progesterone production inSynthetic and systems biotechnology · 2025Article
- Elucidating the binding specificity of interactive compounds targeting ATP-binding cassette subfamily G member 2 (ABCG2).Molecular diversity · 2025Article
- ABCG2 Transporter: From Structure to Function-Current Insights and Open Questions.International journal of molecular sciences · 2025Review
- Conformational cycle and small-molecule inhibition mechanism of a plant ABCB transporter in lipid membranes.Science advances · 2025Article
- Selective Inhibition of the ABCG2 Transporter by Primaquine Derivatives Reverses the Multidrug Resistance of Tumor Cells.International journal of molecular sciences · 2025Article
- In Silico Approach to Design of New Multi-Targeted Inhibitors Based on Quinoline Ring with Potential Anticancer Properties.International journal of molecular sciences · 2025Article
- Message hidden in α-helices-toward a better understanding of plant ABCG transporters' multispecificity.Plant physiology · 2025Article
- Revisiting the Role of the Leucine Plug/Valve in the Human ABCG2 Multidrug Transporter.International journal of molecular sciences · 2025Article
41 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
2 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
ABCG2 is an ABC transporter that extrudes a variety of compounds from cells, and presents an obstacle in treating chemotherapy-resistant cancers. Despite recent structural insights, no anticancer drug bound to ABCG2 has been resolved, and the mechanisms of multidrug transport remain obscure. Such a gap of knowledge limits the development of novel compounds that block or evade this critical molecular pump. Here we present single-particle cryo-EM studies of ABCG2 in the apo state, and bound to the three structurally distinct chemotherapeutics. Without the binding of conformation-selective antibody fragments or inhibitors, the resting ABCG2 adopts a closed conformation. Our cryo-EM, biochemical, and functional analyses reveal the binding mode of three chemotherapeutic compounds, demonstrate how these molecules open the closed conformation of the transporter, and establish that imatinib is particularly effective in stabilizing the inward facing conformation of ABCG2. Together these studies reveal the previously unrecognized conformational cycle of ABCG2.
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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.