ArticleBritish journal of pharmacology2024
A novel EGFR inhibitor, HNPMI, regulates apoptosis and oncogenesis by modulating BCL-2/BAX and p53 in colon cancer.
Article in British journal of pharmacology, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 20 citations in OpenAlex.
- Targeting molecular and genetic pathways driving tumorigenesis for precision therapy in colorectal cancer.Cancer biology & therapy · 2026Review
- Rational structure-guided identification of a Bcl-2-targeting peptide with antiproliferative effects on colorectal cancer cells.Journal of enzyme inhibition and medicinal chemistry · 2026Article
- 10-Hydroxy-2-decenoic Acid Suppresses Colorectal Cancer Progression by Inhibiting Wnt/β-Catenin Signaling and Promoting Apoptosis.Foods (Basel, Switzerland) · 2026Article
- An AI-derived peptide PCa2 suppresses pancreatic cancer growth via modulation of the ErbB/PI3K/AKT/mTOR/MYC signaling axis.Cell communication and signaling : CCS · 2026Article
- Targeting cell death: a promising approach for colorectal cancer therapy.Cancer cell international · 2026Review
- Quercetagetin-rich flavonoids from marigold induce apoptosis inhibit metastasis of non-small cell lung cancer via the p53/p21 signaling pathway.Frontiers in oncology · 2026Article
- Apoptotic and Molecular Mechanisms of Carthamidin in Breast Cancer Therapy: An Integrated In Vitro and In Silico Study.Molecular biotechnology · 2025Article
- Advances in Understanding Renin-Angiotensin System-Mediated Anti-Tumor Activity of Natural Polyphenols.Biomolecules · 2025Review
- Bioinformatics analysis reveals CTSF suppresses tumor cell malignant phenotype and CD8 + T cell exhaustion by downregulating Bcl- 2 protein in the microenvironment of bladder cancer.Naunyn-Schmiedeberg's archives of pharmacology · 2025Article
- p53 in colorectal cancer: from a master player to a privileged therapy target.Journal of translational medicine · 2025Review
- Therapeutic Potential of Quadrigemine I Against Lymphoma: Mechanistic Insights from Cell Lines and Xenograft Models Demonstrating DNA Damage, Oxidative Stress, and Pathway Regulation.International journal of molecular sciences · 2025Article
- Polyherbal Formulation as a Therapeutic Strategy for Lung Cancer: Phytochemical Profiling, Molecular Docking, and Pharmacological Evaluation.Asian Pacific journal of cancer prevention : APJCP · 2025Article
- Network Pharmacology, Molecular Docking, and in vitro Experiments Reveal the Role and Mechanism of Tanshinone IIA in Colorectal Cancer Treatment Through the PI3K/AKT Pathway.Drug design, development and therapy · 2025Article
- A quinoline-2-thione derivative as a novel chemotherapy drug candidate displays anti-tumor activity in vitro and in vivo.BMC cancer · 2024Article
- Exploration of the Molecular Mechanism ofACS omega · 2024Article
- A novel EGFR inhibitor, HNPMI, regulates apoptosis and oncogenesis by modulating BCL-2/BAX and p53 in colon cancer.British journal of pharmacology · 2024Article
- Deciphering the role of apoptosis signature on the immune dynamics and therapeutic prognosis in breast cancer: Implication for immunotherapy.Frontiers in genetics · 2024Article
- Deciphering hepatocellular carcinoma pathogenesis and therapeutics: a study on anoikis, ceRNA regulatory network and traditional Chinese medicine.Frontiers in pharmacology · 2023Article
Corrections and comments
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Authors and funding
15 authors at 7 institutions in 6 countries.
Funding
Abstract
background and purposeColorectal cancer (CRC) is the second most lethal disease, with high mortality due to its heterogeneity and chemo-resistance. Here, we have focused on the epidermal growth factor receptor (EGFR) as an effective therapeutic target in CRC and studied the effects of polyphenols known to modulate several key signalling mechanisms including EGFR signalling, associated with anti-proliferative and anti-metastatic properties. EXPERIMENTAL APPROACH: Using ligand- and structure-based cheminformatics, we developed three potent, selective alkylaminophenols, 2-[(3,4-dihydroquinolin-1(2H)-yl)(p-tolyl)methyl]phenol (THTMP), 2-[(1,2,3,4-tetrahydroquinolin-1-yl)(4-methoxyphenyl)methyl]phenol (THMPP) and N-[2-hydroxy-5-nitrophenyl(4'-methylphenyl)methyl]indoline (HNPMI). These alkylaminophenols were assessed for EGFR interaction, EGFR-pathway modulation, cytotoxic and apoptosis induction, caspase activation and transcriptional and translational regulation. The lead compound HNPMI was evaluated in mice bearing xenografts of CRC cells. KEY
resultsOf the three alkylaminophenols tested, HNPMI exhibited the lowest IC CONCLUSIONS AND IMPLICATIONS: HNPMI is a promising EGFR inhibitor for clinical translation. HNPMI regulated apoptosis and oncogenesis by modulating BCL-2/BAX and p53 in CRC cell lines, showing potential as a therapeutic agent in the treatment of CRC.
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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.