ArticleCancer communications (London, England)2020
Modulating the function of ABCB1: in vitro and in vivo characterization of sitravatinib, a tyrosine kinase inhibitor.
Article in Cancer communications (London, England), 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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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.
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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.
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Who cites it
20 citing papers in PubMed, 37 citations in OpenAlex.
- CGF induces ROS-mediated metabolic reprogramming and mitochondrial dysfunction to suppress colorectal cancer progression.iScience · 2026Article
- Flavonoids and miRNA Modulation: A Novel Approach to Managing Cancer, Diabetes, Depression, and Neurological Disorders.BioMed research international · 2026Review
- Investigating of harmane, harmine, and norharman as inhibitors of MDR1 and MRP1 to overcome chemotherapy resistance in cancer cells.Scientific reports · 2025Article
- From pathogenesis to therapeutic targeting: new insight into TAM receptors in rheumatoid arthritis.Cell & bioscience · 2025Review
- Polyphyllin H Reverses Paclitaxel Resistance in Breast Cancer by Binding Membrane Cholesterol to Inhibit Both ABCB1 and ABCC3.Pharmaceuticals (Basel, Switzerland) · 2025Article
- Sitravatinib combined with venetoclax exerts effective synergy to eliminate acute myeloid leukemia cells with FLT3-ITD mutations.Translational oncology · 2025Article
- Small-molecule and peptide inhibitors of m6A regulators.Frontiers in oncology · 2025Review
- Sitravatinib as a potent FLT3 inhibitor can overcome gilteritinib resistance in acute myeloid leukemia.Biomarker research · 2023Article
- The AKT inhibitor, MK-2206, attenuates ABCG2-mediated drug resistance in lung and colon cancer cells.Frontiers in pharmacology · 2023Article
- Toad venom-derived bufadienolides and their therapeutic application in prostate cancers: Current status and future directions.Frontiers in chemistry · 2023Review
- ABCB1 limits the cytotoxic activity of TAK-243, an inhibitor of the ubiquitin-activating enzyme UBA1.Frontiers in bioscience (Landmark edition) · 2022Article
- MG53 inhibits cellular proliferation and tumor progression in colorectal carcinoma.International journal of biological sciences · 2022Article
- The Resistance of Cancer Cells to Palbociclib, a Cyclin-Dependent Kinase 4/6 Inhibitor, is Mediated by the ABCB1 Transporter.Frontiers in pharmacology · 2022Article
- Lapatinib Suppresses HER2-Overexpressed Cholangiocarcinoma and Overcomes ABCB1- Mediated Gemcitabine Chemoresistance.Frontiers in oncology · 2022Article
- Meclofenamic Acid Restores Gefinitib Sensitivity by Downregulating Breast Cancer Resistance Protein and Multidrug Resistance Protein 7Frontiers in oncology · 2022Article
- Scaffold fragmentation and substructure hopping reveal potential, robustness, and limits of computer-aided pattern analysis (C@PA).Computational and structural biotechnology journal · 2021Article
- Overexpression of ABCC1 Confers Drug Resistance to Betulin.Frontiers in oncology · 2021Article
- Article
- Modulating the function of ABCB1: in vitro and in vivo characterization of sitravatinib, a tyrosine kinase inhibitor.Cancer communications (London, England) · 2020Article
- Reversal of Cancer Multidrug Resistance (MDR) Mediated by ATP-Binding Cassette Transporter G2 (ABCG2) by AZ-628, a RAF Kinase Inhibitor.Frontiers in cell and developmental biology · 2020Article
Corrections and comments
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Authors and funding
10 authors at 2 institutions in 2 countries.
Funding
Abstract
backgroundOverexpression of ATP-binding cassette (ABC) transporter is a major contributor to multidrug resistance (MDR), in which cancer cells acquire resistance to a wide spectrum of chemotherapeutic drugs. In this work, we evaluated the sensitizing effect of sitravatinib, a broad-spectrum tyrosine kinase inhibitor (TKI), on ATP-binding cassette subfamily B member 1 (ABCB1)- and ATP-binding cassette subfamily C member 10 (ABCC10)-mediated MDR.
methodsMTT assay was conducted to examine cytotoxicity and evaluate the sensitizing effect of sitravatinib at non-toxic concentrations. Tritium-labeled paclitaxel transportation, Western blotting, immunofluorescence analysis, and ATPase assay were carried out to elucidate the mechanism of sitravatinib-induced chemosensitization. The in vitro findings were translated into preclinical evaluation with the establishment of xenograft models.
resultsSitravatinib considerably reversed MDR mediated by ABCB1 and partially antagonized ABCC10-mediated MDR. Our in silico docking simulation analysis indicated that sitravatinib strongly and stably bound to the transmembrane domain of ABCB1 human-mouse chimeric model. Furthermore, sitravatinib inhibited hydrolysis of ATP and synchronously decreased the efflux function of ABCB1. Thus, sitravatinib could considerably enhance the intracellular concentration of anticancer drugs. Interestingly, no significant alterations of both expression level and localization of ABCB1 were observed. More importantly, sitravatinib could remarkably restore the antitumor activity of vincristine in ABCB1-mediated xenograft model without observable toxic effect.
conclusionsThe findings in this study suggest that the combination of sitrvatinib and substrate antineoplastic drugs of ABCB1 could attenuate the MDR mediated by the overexpression of ABCB1.
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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.