Emerging Strategies to Overcome Chemoresistance: Structural Insights and Therapeutic Targeting of Multidrug Resistance-Linked ATP-Binding Cassette Transporters

The ATP-binding cassette (ABC) transporter superfamily, one of the largest membrane protein families, plays a crucial role in multidrug resistance (MDR) in cancer by mediating the efflux of various chemotherapeutic agents, thereby lowering their intracellular concentrations and diminishing therapeut...

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Main Authors: Raghavendra Sashi Krishna Nagampalli, Gangadhar P. Vadla, Eswar Kumar Nadendla
Format: Article
Language:English
Published: MDPI AG 2025-01-01
Series:International Journal of Translational Medicine
Subjects:
Online Access:https://www.mdpi.com/2673-8937/5/1/6
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author Raghavendra Sashi Krishna Nagampalli
Gangadhar P. Vadla
Eswar Kumar Nadendla
author_facet Raghavendra Sashi Krishna Nagampalli
Gangadhar P. Vadla
Eswar Kumar Nadendla
author_sort Raghavendra Sashi Krishna Nagampalli
collection DOAJ
description The ATP-binding cassette (ABC) transporter superfamily, one of the largest membrane protein families, plays a crucial role in multidrug resistance (MDR) in cancer by mediating the efflux of various chemotherapeutic agents, thereby lowering their intracellular concentrations and diminishing therapeutic effectiveness. Beyond drug efflux, these transporters are also involved in vital biological processes, such as signal transduction in cancer. Over the past few decades, extensive structural and functional research has provided valuable insights into ABC transporters’ broad substrate specificity and transport mechanisms, leading to promising strategies for overcoming MDR. This review will provide a structural understanding of the interactions between ABC transporters and inhibitors to develop novel cancer therapeutics. Additionally, we focus on methods such as irradiation-based immune therapies, thermal therapies, nanomedicine, CRISPR-Cas, and natural therapies that can genetically modify ABC transporters to reduce their expression or reverse the drug efflux ability. Knowledge gained from these approaches can then be translated into the development of new cancer therapeutics that can combat chemotherapy resistance.
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spelling doaj-art-e67f074aa1fc4f6d979488252444e05e2025-08-20T01:49:00ZengMDPI AGInternational Journal of Translational Medicine2673-89372025-01-0151610.3390/ijtm5010006Emerging Strategies to Overcome Chemoresistance: Structural Insights and Therapeutic Targeting of Multidrug Resistance-Linked ATP-Binding Cassette TransportersRaghavendra Sashi Krishna Nagampalli0Gangadhar P. Vadla1Eswar Kumar Nadendla2Department of Immunology, St. Jude Children’s Research Hospital, Memphis, TN 38105, USADepartment of Veterinary Pathobiology, Bond Life Sciences Center, 1201 Rollins Street, Columbia, MI 65211, USADepartment of Immunology, St. Jude Children’s Research Hospital, Memphis, TN 38105, USAThe ATP-binding cassette (ABC) transporter superfamily, one of the largest membrane protein families, plays a crucial role in multidrug resistance (MDR) in cancer by mediating the efflux of various chemotherapeutic agents, thereby lowering their intracellular concentrations and diminishing therapeutic effectiveness. Beyond drug efflux, these transporters are also involved in vital biological processes, such as signal transduction in cancer. Over the past few decades, extensive structural and functional research has provided valuable insights into ABC transporters’ broad substrate specificity and transport mechanisms, leading to promising strategies for overcoming MDR. This review will provide a structural understanding of the interactions between ABC transporters and inhibitors to develop novel cancer therapeutics. Additionally, we focus on methods such as irradiation-based immune therapies, thermal therapies, nanomedicine, CRISPR-Cas, and natural therapies that can genetically modify ABC transporters to reduce their expression or reverse the drug efflux ability. Knowledge gained from these approaches can then be translated into the development of new cancer therapeutics that can combat chemotherapy resistance.https://www.mdpi.com/2673-8937/5/1/6ABC transportersmultidrug resistance (MDR)ABC transporter inhibitorscancer therapeuticsdrug efflux mechanism
spellingShingle Raghavendra Sashi Krishna Nagampalli
Gangadhar P. Vadla
Eswar Kumar Nadendla
Emerging Strategies to Overcome Chemoresistance: Structural Insights and Therapeutic Targeting of Multidrug Resistance-Linked ATP-Binding Cassette Transporters
International Journal of Translational Medicine
ABC transporters
multidrug resistance (MDR)
ABC transporter inhibitors
cancer therapeutics
drug efflux mechanism
title Emerging Strategies to Overcome Chemoresistance: Structural Insights and Therapeutic Targeting of Multidrug Resistance-Linked ATP-Binding Cassette Transporters
title_full Emerging Strategies to Overcome Chemoresistance: Structural Insights and Therapeutic Targeting of Multidrug Resistance-Linked ATP-Binding Cassette Transporters
title_fullStr Emerging Strategies to Overcome Chemoresistance: Structural Insights and Therapeutic Targeting of Multidrug Resistance-Linked ATP-Binding Cassette Transporters
title_full_unstemmed Emerging Strategies to Overcome Chemoresistance: Structural Insights and Therapeutic Targeting of Multidrug Resistance-Linked ATP-Binding Cassette Transporters
title_short Emerging Strategies to Overcome Chemoresistance: Structural Insights and Therapeutic Targeting of Multidrug Resistance-Linked ATP-Binding Cassette Transporters
title_sort emerging strategies to overcome chemoresistance structural insights and therapeutic targeting of multidrug resistance linked atp binding cassette transporters
topic ABC transporters
multidrug resistance (MDR)
ABC transporter inhibitors
cancer therapeutics
drug efflux mechanism
url https://www.mdpi.com/2673-8937/5/1/6
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