Research Topic

Novel Small-Molecule Agents in Overcoming Multidrug Resistance in Cancers

About this Research Topic

While the treatment of cancer has significantly improved as a result of targeted therapy and cutting-edge immunotherapy, the development of multidrug resistance (MDR) significantly limits the efficacy of cancer treatment, and impacts patients’ survival and quality of life. Multidrug resistance (MDR), a phenomenon wherein cancer cells become resistant to multiple chemotherapeutics that are structurally and mechanistically different, is one of the major challenges in cancer treatment - accounting for 90% of cancer patient mortality. Drug resistance exists across all types of cancer and all modes of treatment, including targeted therapy, immunotherapy, and chemotherapy. Novel effective remedies are urgently needed to circumvent MDR. The mechanisms of MDR involve dynamic ATP-binding cassette (ABC) transporters, oncogenes mutations, microenvironment changes, reprogramed cancer cell metabolism, efficient DNA repairing, activated defense systems, and more. Each of these associated mechanisms can be targeted by small-molecule regulators which may hold promise in overcoming MDR. 


In light of this, the current Research topic focuses on recent progress made in developing small-molecule agents that have potential in either reversing or overcoming MDR in cancers. We are specifically interested in those novel drug candidates that are derived from the structural modification of natural products, other hit compounds identified from HTS, or de novo design. Rational structure design and mechanism study of novel agents targeting those well-recognized or newly discovered factors in MDR are also encouraged. Reviews of the progress of small-molecule agents in overcoming MDR are welcomed for submission.


Areas to be covered in this Research Topic may include, but are not limited to:


• Design, synthesis, and evaluation of small-molecule regulators targeting key players in regulating MDR

• Mechanistic study of novel agents that may reverse or overcome MDR

• Drug repurposing for the treatment of resistant cancers

• Natural products including their derivatives in the treatment of resistant cancers






Keywords: Multidrug resistance, Mechanism, Reversal agents, Medicinal chemistry, Drug discovery


Important Note: All contributions to this Research Topic must be within the scope of the section and journal to which they are submitted, as defined in their mission statements. Frontiers reserves the right to guide an out-of-scope manuscript to a more suitable section or journal at any stage of peer review.

While the treatment of cancer has significantly improved as a result of targeted therapy and cutting-edge immunotherapy, the development of multidrug resistance (MDR) significantly limits the efficacy of cancer treatment, and impacts patients’ survival and quality of life. Multidrug resistance (MDR), a phenomenon wherein cancer cells become resistant to multiple chemotherapeutics that are structurally and mechanistically different, is one of the major challenges in cancer treatment - accounting for 90% of cancer patient mortality. Drug resistance exists across all types of cancer and all modes of treatment, including targeted therapy, immunotherapy, and chemotherapy. Novel effective remedies are urgently needed to circumvent MDR. The mechanisms of MDR involve dynamic ATP-binding cassette (ABC) transporters, oncogenes mutations, microenvironment changes, reprogramed cancer cell metabolism, efficient DNA repairing, activated defense systems, and more. Each of these associated mechanisms can be targeted by small-molecule regulators which may hold promise in overcoming MDR. 


In light of this, the current Research topic focuses on recent progress made in developing small-molecule agents that have potential in either reversing or overcoming MDR in cancers. We are specifically interested in those novel drug candidates that are derived from the structural modification of natural products, other hit compounds identified from HTS, or de novo design. Rational structure design and mechanism study of novel agents targeting those well-recognized or newly discovered factors in MDR are also encouraged. Reviews of the progress of small-molecule agents in overcoming MDR are welcomed for submission.


Areas to be covered in this Research Topic may include, but are not limited to:


• Design, synthesis, and evaluation of small-molecule regulators targeting key players in regulating MDR

• Mechanistic study of novel agents that may reverse or overcome MDR

• Drug repurposing for the treatment of resistant cancers

• Natural products including their derivatives in the treatment of resistant cancers






Keywords: Multidrug resistance, Mechanism, Reversal agents, Medicinal chemistry, Drug discovery


Important Note: All contributions to this Research Topic must be within the scope of the section and journal to which they are submitted, as defined in their mission statements. Frontiers reserves the right to guide an out-of-scope manuscript to a more suitable section or journal at any stage of peer review.

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Submission Deadlines

19 July 2021 Abstract
15 November 2021 Manuscript

Participating Journals

Manuscripts can be submitted to this Research Topic via the following journals:

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Topic Editors

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Submission Deadlines

19 July 2021 Abstract
15 November 2021 Manuscript

Participating Journals

Manuscripts can be submitted to this Research Topic via the following journals:

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