Please use this identifier to cite or link to this item:
http://hdl.handle.net/10397/105754
DC Field | Value | Language |
---|---|---|
dc.contributor | Department of Applied Biology and Chemical Technology | en_US |
dc.creator | Zheng, BX | en_US |
dc.creator | Long, W | en_US |
dc.creator | Zheng, W | en_US |
dc.creator | Zeng, Y | en_US |
dc.creator | Guo, XC | en_US |
dc.creator | Chan, KH | en_US |
dc.creator | She, MT | en_US |
dc.creator | Leung, ASL | en_US |
dc.creator | Lu, YJ | en_US |
dc.creator | Wong, WL | en_US |
dc.date.accessioned | 2024-04-17T03:43:43Z | - |
dc.date.available | 2024-04-17T03:43:43Z | - |
dc.identifier.issn | 0022-2623 | en_US |
dc.identifier.uri | http://hdl.handle.net/10397/105754 | - |
dc.language.iso | en | en_US |
dc.publisher | American Chemical Society | en_US |
dc.title | Mitochondria-selective dicationic small-molecule ligand targeting G-quadruplex structures for human colorectal cancer therapy | en_US |
dc.type | Journal/Magazine Article | en_US |
dc.description.otherinformation | Title on author's file: Mitochondria-selective dicationic small molecule ligand targeting G-quadruplex structures for human colorectal cancer therapy | en_US |
dc.identifier.doi | 10.1021/acs.jmedchem.3c02240 | en_US |
dcterms.abstract | Mitochondria are important drug targets for anticancer and other disease therapies. Certain human mitochondrial DNA sequences capable of forming G-quadruplex structures (G4s) are emerging drug targets of small molecules. Despite some mitochondria-selective ligands being reported for drug delivery against cancers, the ligand design is mostly limited to the triphenylphosphonium scaffold. The ligand designed with lipophilic small-sized scaffolds bearing multipositive charges targeting the unique feature of high mitochondrial membrane potential (MMP) is lacking and most mitochondria-selective ligands are not G4-targeting. Herein, we report a new small-sized dicationic lipophilic ligand to target MMP and mitochondrial DNA G4s to enhance drug delivery for anticancer. The ligand showed marked alteration of mitochondrial gene expression and substantial induction of ROS production, mitochondrial dysfunction, DNA damage, cellular senescence, and apoptosis. The ligand also exhibited high anticancer activity against HCT116 cancer cells (IC50, 3.4 μM) and high antitumor efficacy in the HCT116 tumor xenograft mouse model (∼70% tumor weight reduction). | en_US |
dcterms.accessRights | embargoed access | en_US |
dcterms.bibliographicCitation | Journal of medicinal chemistry, Publication Date: April 16, 2024, Articles ASAP, https://doi.org/10.1021/acs.jmedchem.3c02240 | en_US |
dcterms.isPartOf | Journal of medicinal chemistry | en_US |
dcterms.issued | 2024 | - |
dc.identifier.eissn | 1520-4804 | en_US |
dc.description.validate | 202404 bcch | en_US |
dc.description.oa | Not applicable | en_US |
dc.identifier.FolderNumber | a2679 | - |
dc.identifier.SubFormID | 48051 | - |
dc.description.fundingSource | RGC | en_US |
dc.description.pubStatus | Early release | en_US |
dc.date.embargo | 2025-04-16 | en_US |
dc.description.oaCategory | Green (AAM) | en_US |
Appears in Collections: | Journal/Magazine Article |
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