Repurposing Tyrosine Kinase Inhibitors to Overcome Multidrug Resistance in Cancer: A Focus on Transporters and Lysosomal Sequestration

Krchniakova, Maria; Skoda, Jan; Neradil, Jakub; Chlapek, Petr; Veselska, Renata

doi:10.3390/ijms21093157

Cited by 61Drug Transport and Resistance MechanismsAntibiotic Resistance in BacteriaPharmacogenetics and Drug Metabolism

Repurposing Tyrosine Kinase Inhibitors to Overcome Multidrug Resistance in Cancer: A Focus on Transporters and Lysosomal Sequestration

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Krchniakova, Maria, Skoda, Jan, Neradil, Jakub, Chlapek, Petr, Veselska, Renata·2020·International Journal of Molecular Sciences

DOI 10.3390/ijms21093157PMC PMC7247577

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Abstract

Tyrosine kinase inhibitors (TKIs) are being increasingly used to treat various malignancies. Although they were designed to target aberrant tyrosine kinases, they are also intimately linked with the mechanisms of multidrug resistance (MDR) in cancer cells. MDR-related solute carrier (SLC) and ATB-binding cassette (ABC) transporters are responsible for TKI uptake and efflux, respectively. However, the role of TKIs appears to be dual because they can act as substrates and/or inhibitors of these transporters. In addition, several TKIs have been identified to be sequestered into lysosomes either due to their physiochemical properties or via ABC transporters expressed on the lysosomal membrane. Since the development of MDR represents a great concern in anticancer treatment, it is important to elucidate the interactions of TKIs with MDR-related transporters as well as to improve the properties that would prevent TKIs from diffusing into lysosomes. These findings not only help to avoid MDR, but also help to define the possible impact of combining TKIs with other anticancer drugs, leading to more efficient therapy and fewer adverse effects in patients.

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Several kinase inhibitors, including FDA-approved kinase inhibitors, have been shown to directly inhibit MDR1 drug efflux activity.
“Several kinase inhibitors have been shown to directly inhibit MDR1 drug efflux activity, including a number of FDA-approved kinase inhibitors (35, 52).”
From The drug efflux pump MDR1 promotes intrinsic and acquired resistance to PROTACs in cancer cells (2022) · cites this paper as [52]

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Authors: Krchniakova, M., Skoda, J., Neradil, J., Chlapek, P., & Veselska, R.
Affiliations: Laboratory of Tumor Biology, Department of Experimental Biology, Faculty of Science, Masaryk University, 61137 Brno, Czech Republic
Masaryk University (CZ)
ORCID: Krchniakova, Maria
Skoda, Jan
Neradil, Jakub
Chlapek, Petr
Veselska, Renata
Venue: International Journal of Molecular Sciences
Publisher: MDPI AG
Published: 2020-04-30
Volume: 21
Issue: 9
Pages: 3157
ISSN: 1422-0067 (ISSN-L)
DOI: 10.3390/ijms21093157
PMC: PMC7247577
OpenAlex: W3022831706
Cited by: 61
References: 127
Citations by year: 2026: 7 · 2025: 12 · 2024: 11 · 2023: 9 · 2022: 12 · 2021: 9 · 2020: 1
FWCI: 0.83
Type: journal article
Language: en
Open access: gold
dx.doi.org
Licence: cc-by
creativecommons.org/licenses/by/4.0/ (vor)
Locations: International Journal of Molecular Sciences (publishedVersion, cc-by)
PubMed Central (publishedVersion, cc-by)
PubMed (publishedVersion)
DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
Funders: Ministry of Healthcare of the Czech Republic (17-33104A)
National Program of Sustainability II (MEYS CR) (LQ1605)
JCMM (Brno Ph.D. Talent 2017)
Topics: Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Medicine › Antibiotic Resistance in Bacteria
Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
Keywords: tyrosine kinase inhibitors, multidrug resistance, drug transporters, solute carrier transporters, ABC transporters, lysosomal sequestration, drug efflux, drug uptake, drug repurposing, combination cancer therapy
MeSH terms: Solute Carrier Proteins, Animals, Biological Transport, Clinical Trials as Topic, Humans, Lysosomes, Neoplasms, Treatment Outcome, Drug Resistance, Multiple, ATP-Binding Cassette Transporters, Drug Resistance, Neoplasm, Membrane Transport Proteins, Protein Kinase Inhibitors, Drug Repositioning

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Repurposing Tyrosine Kinase Inhibitors to Overcome Multidrug Resistance in Cancer: A Focus on Transporters and Lysosomal Sequestration

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