Multi-pathway therapeutics in colorectal cancer: targeting EMT, CSCs, and non-apoptotic cell death for drug resistance reversal

Colorectal cancer (CRC) is a leading global malignancy, with therapeutic outcomes hampered by chemoresistance from epithelial-mesenchymal transition (EMT), colorectal cancer stem cells (CR-CSCs) and apoptosis evasion. Evidence highlights the therapeutic value of non-apoptotic cell death pathways such as paraptosis, ferroptosis, cuproptosis and autophagy as strategies to overcome resistance. This review evaluates natural and synthetic scaffolds targeting EMT-driven chemoresistance in CRC by inducing regulated cell death pathways and disrupting stemness-associated survival mechanisms. Studies from the last decade were analysed, focusing on EMT regulation, CR-CSC markers (Sox2, Oct4, Nanog), chemoresistance proteins (P-gp, ERCC1) and cell death-inducing agents. Emphasis was placed on compounds modulating Wnt/β-catenin, TGF-β, JAK2/STAT3/GPX4 and p38α pathways. Natural compounds (neferine, ajoene, baicalein, isoliensinine, curcumin analogs) and synthetic drugs (5-FU, oxaliplatin, irinotecan, norcantharidin, cordycepin) modulate EMT and trigger ferroptosis, cuproptosis, paraptosis and autophagy. Mechanistic pathways include HUWE1-TOMM20 axis, CDH17-LGR5 signalling and mitochondrial reprogramming under acidic stress. Additionally, c-Fos-driven stemness, p38α-mediated survival and JAK2/STAT3-regulated GPX4 inhibition were intervention points. Simultaneous targeting of EMT, CR-CSC maintenance and chemoresistance using multifunctional natural and synthetic agents represents a promising strategy in CRC therapy. Induction of alternative cell death pathways may improve response, minimise relapse and enable combinatorial regimens for resistant tumours.

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Publication Details

Journal
Journal of drug targeting
Published
2025-12-09
DOI
https://doi.org/10.1080/1061186x.2025.2600679
Primary Topic
Cancer Cells and Metastasis
Type
article
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article

Multi-pathway therapeutics in colorectal cancer: targeting EMT, CSCs, and non-apoptotic cell death for drug resistance reversal

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Journal of drug targeting
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Multi-pathway therapeutics in colorectal cancer: targeting EMT, CSCs, and non-apoptotic cell death for drug resistance reversal

P. R. Hemanth Vikram, Zhiwei Tang, Lianghui Li, Narasimha M. Beeraka, Bhupalam Pradeepkumar, T. Gayathri, Ruixiang Xu, Jiegang Hu, Dilipkumar Reddy Kandula, Ruofan Wang, Xiang Zhao, Zhongshi He, Junqi Liu, Padmanabha Reddy Y, Bhavana Jayadevappa
article en

Abstract

Colorectal cancer (CRC) is a leading global malignancy, with therapeutic outcomes hampered by chemoresistance from epithelial-mesenchymal transition (EMT), colorectal cancer stem cells (CR-CSCs) and apoptosis evasion. Evidence highlights the therapeutic value of non-apoptotic cell death pathways such as paraptosis, ferroptosis, cuproptosis and autophagy as strategies to overcome resistance. This review evaluates natural and synthetic scaffolds targeting EMT-driven chemoresistance in CRC by inducing regulated cell death pathways and disrupting stemness-associated survival mechanisms. Studies from the last decade were analysed, focusing on EMT regulation, CR-CSC markers (Sox2, Oct4, Nanog), chemoresistance proteins (P-gp, ERCC1) and cell death-inducing agents. Emphasis was placed on compounds modulating Wnt/β-catenin, TGF-β, JAK2/STAT3/GPX4 and p38α pathways. Natural compounds (neferine, ajoene, baicalein, isoliensinine, curcumin analogs) and synthetic drugs (5-FU, oxaliplatin, irinotecan, norcantharidin, cordycepin) modulate EMT and trigger ferroptosis, cuproptosis, paraptosis and autophagy. Mechanistic pathways include HUWE1-TOMM20 axis, CDH17-LGR5 signalling and mitochondrial reprogramming under acidic stress. Additionally, c-Fos-driven stemness, p38α-mediated survival and JAK2/STAT3-regulated GPX4 inhibition were intervention points. Simultaneous targeting of EMT, CR-CSC maintenance and chemoresistance using multifunctional natural and synthetic agents represents a promising strategy in CRC therapy. Induction of alternative cell death pathways may improve response, minimise relapse and enable combinatorial regimens for resistant tumours.

Journal of drug targeting
Hubei University of Medicine (CN), Tabriz University of Medical Sciences (IR), Sechenov University (RU), University of Mysore (IN), Shri Jagdishprasad Jhabarmal Tibrewala University (IN), Amity University (AE), First Affiliated Hospital of Zhengzhou University (CN), Xiang Yang No.1 People's Hospital (CN), Southern Medical University (CN), Saveetha University (IN)
Openalex Percentile: Top 45%
Cancer Cells and Metastasis
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