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Journal: "Domino" cascade reactor based on DNA hydrogel for synergistic treatment of malignant tumor. (Pubmed Central) - Jun 2, 2023
At the same time, the G-quadruplex of AS1411 combined with hemin (AH) catalyzes the generation of oxygen from hydrogen peroxide to further improve the efficiency of PDT. The synergistic therapeutic effect of the cascade reactor is evaluated through in vivo and in vitro experiments, indicating that this cascade reactor has great potential advantages in the synergistic treatment of cancer.
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Journal: A non-G-Quadruplex DNA Aptamer Targeting NCL for Diagnosis and Therapy in Bladder Cancer. (Pubmed Central) - Jun 1, 2023
Circular dichroism spectroscopy revealed that TB-5 adopts a non-G-quadruplex structure, distinguishing it from the current aptamer AS1411, which also binds to NCL...Most importantly, we discovered that TB-5 disrupts mRNA transcription processes in cancer cells by binding to NCL, leading to the inhibition of cell proliferation and migration. These findings highlight the critical role of NCL in the pathological examination of BC and warrant more comprehensive investigations on anti-NCL aptamers in BC imaging and treatment.
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Journal: Assessment of Aptamer as a Potential Drug Targeted Delivery for Retinal Angiogenesis Inhibition. (Pubmed Central) - May 27, 2023
AT11-L0 is an aptamer derivative of AS1411 composed of G-rich sequences that can adopt a G-quadruplex (G4) structure and target nucleolin (NCL), a protein that acts as a co-receptor for several growth factors...The aptamer-functionalized liposomes loaded with ligands C and dexamethasone did not show cytotoxic effects in HUVEC cells compared with the free ligands and AT11-L0, as assessed by cell viability assays...In addition, AT11-L0 did not show anti-angiogenic effects at the concentrations tested. However, C shows potential as an angiogenesis inhibitor, which should be further developed and optimized in future experiments.
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Journal: Computable structured aptamer for targeted treatment of ovarian cancer. (Pubmed Central) - May 19, 2023
Moreover, when injected into nude mice subcutaneous xenograft models, HA-6AS reached the peak in tumor more quickly than ST-6AS, and better expressed the active targeting ability of AS1411. Our study suggests that designing appropriate DNA tiles to assemble different aptamers to deliver different chemotherapeutic drugs is a promising treatment for ovarian cancer.
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Journal, Tumor cell: Engineering of An Aptamer-Functionalized Fluorescent DNA Sensor for Cu(II) Responding in Living Tumor Cells. (Pubmed Central) - May 17, 2023
Herein, we propose an aptamer-functionalized DNA fluorescent sensor (AFDS) for accurate and specific detection of Cu(II) both in vitro and in cells by engineering the linkage of two DNA aptamers, namely, Lettuce aptamer and AS1411 aptamer, to achieve the manner of recognition response...The feasibility and superiority of the AFDS provide an opportunity to reveal both concentration-dependent and time-dependent intracellular Cu(II) responses in living cells. Therefore, the AFDS has achieved the novel detection performance of Cu(II) to exhibit great potential in exploring copper-related biological and pathological research.
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Journal: Parahydrogen-Induced Polarization of a Labeled, Cancer-Targeting DNA Aptamer. (Pubmed Central) - May 15, 2023
Finally, adjusting the polarity of AS1411 by complexing the DNA backbone with amino polyethylene glycol chains allowed the hydrogenation of the label with parahydrogen while the DNA structure remains stable to maintain its biological function. Our results are expected to advance hyperpolarized molecular imaging technology for disease detection in the future.
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Journal: Nucleolin promotes angiogenesis and endothelial metabolism along the onco-fetal axis in the human brain vasculature. (Pubmed Central) - Apr 25, 2023
Furthermore, inhibition of Nucleolin with the aptamer AS1411 decreased brain endothelial cell proliferation in vitro...These findings identify Nucleolin as a neurodevelopmental factor reactivated in glioma that promotes sprouting angiogenesis and endothelial metabolism, characterizing Nucleolin as an onco-fetal protein. Our findings have potential implications in the therapeutic targeting of glioma.
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Journal: A nucleolin-activated polyvalent aptamer nanoprobe for the detection of cancer cells. (Pubmed Central) - Apr 21, 2023
Then the RCA product acted as a scaffold chain to combine with multiple AS1411 sequences, which was doubly modified with fluorophore and quenching group, respectively...Furthermore, the binding affinity of PAN to B16 cells was proved to be 30 times higher than that of MAN by calculating the dissociation constants. The results indicated that PAN could specifically detect target cells, and this design concept has potential to become promising in cancer diagnosis.
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6-Phosphofructo-2-kinase in regulating DNA damage and repair in EGFR-driven lung cancer (Section 18; Poster Board #4) - Mar 14, 2023 - Abstract #AACR2023AACR_8351;
Moreover, a PFKFB3 inhibitor, PFK-158, increases oxidative stress in mutEGFR lung cancer cell lines and, as a result, promotes DNA damage. Importantly, we found that PFKFB3 plays an important role in the chromatin binding of scaffold proteins regulating the assembly of DNA repair complex.Our studies suggest that PFKFB3 plays an important role in DDR and provide a clear rationale to propose the use of PFKFB3 inhibitors in combination with EGFR inhibitors to increase the efficiency and/or overcome resistance to EGFR-TKIs.
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Magnetic and light activated nanocarriers in the treatment of childhood brain cancers (Illinois Street Ballrm East (Crown Plaza Indianapolis Downtown Union Square)) - Feb 14, 2023 - Abstract #ACSSp2023ACS_SP_1659;
An increased antitumor effect of nanocarriers is observed under magnetic and light field at a low concentration. These data prove the externally stimulated magneto-plasmonic nanocarriers is highly useful for next generation cancer therapies for childhood cancers.Magnetic and Light activated nanocarriers3D Multicellular cancer spheroids for childhood brain cancer
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Journal: Novel targeted pH-responsive drug delivery systems based on PEGMA-modified bimetallic Prussian blue analogs for breast cancer chemotherapy. (Pubmed Central) - Jan 31, 2023
Two kinds of bimetallic PBA, namely CuFe (copper-iron) PBA and CoFe (cobalt-iron) PBA, were synthesized by a coprecipitation method, followed by modification with polyethyleneglycol methacrylate (PEGMA) via surface-initiated atom transfer radical polymerization and immobilization with the AS1411 aptamer to obtain two kinds of novel BC-targeted nano-DDS...In vivo evaluation of anti-BC efficacy further confirmed that the obtained PBA-DDSs exhibited excellent therapeutic efficacy with limited side-effects. Therefore, the proposed novel PBA-DDSs can be used as secure and effective drug nano-DDSs for BC chemotherapy.
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Journal: Poly-thymine DNA templated MnO biomineralization as a high-affinity anchoring enabling tumor targeting delivery. (Pubmed Central) - Jan 31, 2023
Upon targeting delivery into tumor cells, the MnO acted as catalase-mimic nanozyme for oxygenation to sensitize photodynamic therapy, and the released Mn triggered chemodynamic therapy via Fenton-like reaction, achieving synergistic anti-tumor effect with full biocompatibility. This work provides a simple yet robust strategy to functionalize metal oxides nanomaterials for biological applications via DNA-templated biomineralization.
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Journal, Tumor cell: Cathodic Electrochemiluminesence Microscopy for Imaging of Single Carbon Nanotube and Nucleolin at Single Tumor Cell. (Pubmed Central) - Jan 4, 2023
After being modified with AS1411 aptamers, MWCNTs@AS1411 probes were incubated with tumor cells for specific ECL imaging of nucleolin on the plasma membrane, which permits cathodic ECL microscopy for label-free bioassays without ECL tags. The L012-based cathodic ECL microscopy with a moderate operating potential and label-free characteristics provides a universal approach in single nanomaterial and single-cell imaging and analyses.
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Journal: Folate-Functionalization Enhances Cytotoxicity of Multivalent DNA Nanocages on Triple-Negative Breast Cancer Cells. (Pubmed Central) - Dec 24, 2022
Double-functionalized nanocages (Fol-Apt-NC), loaded with doxorubicin, resulted in an increase of over 51% of the cytotoxic effect on MDA-MB-231 cells compared to free doxorubicin, demonstrating, besides selectivity, the ability of nanocages to overcome Dox chemoresistance. The higher efficiency of the folate-functionalized nanocages is due to the way of entrance, which induces more than four times higher intracellular stability and indicates that the folate-mediated route of cell entry is more efficient than the nucleolin-mediated one when both folate and AS1411 modifications are present.
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Journal: Aptamer-Engineered CuO Nanocubes as a Surface-Modulated Catalytic Optical Sensor for Lung Cancer Cell Detection. (Pubmed Central) - Dec 21, 2022
Herein, fine and homogeneous CuO nanocubes are synthesized and sensitized with a hairpin-structured AS1411 aptamer for the establishment of a biosensor for lung cancer cell detection...Real human serum samples spiked with cancer cells were also investigated, and a recovery rate of 87 ± 2.4% for 20 extracted cells validates the surface-modulated Apt-CuO nanocubes-based catalytic optical biosensor as a promising tool for the detection of circulating tumor cells. The establishment of the Apt-CuO nanocubes may allow for further studies on their use as a potential theranostics tool for cancer therapy.
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Journal: Cruciate DNA probes for amplified multiplexed imaging of microRNAs in living cells. (Pubmed Central) - Dec 13, 2022
Through the simultaneous detection of intracellular multiple miRNAs, the developed cruciate DNA probe could provide more accurate information and reduce the chances of false positive signals for cancer diagnosis. This approach offers a new opportunity for promoting the development of miRNA-related biomedical research and tumor diagnostic applications.
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Journal: Gallic Acid-Triethylene Glycol Aptadendrimers Synthesis, Biophysical Characterization and Cellular Evaluation. (Pubmed Central) - Nov 27, 2022
Herein, we describe the synthesis of an aptadendrimer by covalent bioconjugation of a gallic acid-triethylene glycol (GATG) dendrimer with the G-quadruplex (G4) AT11 aptamer (a modified version of AS1411) at the surface...MTT studies with prostate cancer cells and non-malignant cells evidenced high cytotoxicity mainly due to the C ligand. The rapid internalization of the aptadendrimers and the fluorescence properties make them attractive for the development of potential nanocarriers.
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Journal: Optimization of Tumor Targeting Gold Nanoparticles for Glioblastoma Applications. (Pubmed Central) - Nov 16, 2022
Resulting nanotherapies are therapy specific and show upwards of 75% inhibition in metabolic and proliferative activity with stark effects on cellular morphology. Ultimately, these gold nanotherapies are a good base for designing more multi-targeted approaches to fighting against glioblastoma.
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Journal: Simple Monovalent Metal Ion Logical Order to Regulate the Secondary Conformation of G-Quadruplex. (Pubmed Central) - Nov 8, 2022
In terms of this experiment, according to circular dichroism, the antiparallel quadrupole structure has the largest proportion among quadrupole structures, and 12 optimal DNA addition schemes and sequences have been obtained through exploration. It is worth mentioning that, on the whole, the best addition scheme of AS1411 and HT-V18 is a three-ion scheme, which provides an effective reference for similar experiments in the future.
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Journal: An assembly-inducing PDC enabling the efficient nuclear delivery of nucleic acid for cancer stem-like cell suppression. (Pubmed Central) - Nov 1, 2022
Significantly, due to the assembly-induced accumulation enhancement and retention, a safe single agent concentration of PDC showed unexpected synergy with AS1411 to augment the cancer cell suppression efficiency, exemplified by the downregulation of the stemness-related proteins and the upregulation of apoptosis-related proteins. Therefore, our work presents a powerful strategy for the nuclear delivery of nucleic acid drugs by leveraging cancer-suppressing PDC as assembly inducers, which provides a powerful combination regimen in treating cancer stem-like cells.
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Journal: Quantum Dot-Based Screening Identifies F3 Peptide and Reveals Cell Surface Nucleolin as a Therapeutic Target for Rhabdomyosarcoma. (Pubmed Central) - Oct 28, 2022
The expression of the nucleophosphoprotein nucleolin, the target of F3, on the surface of RMS cell lines was validated by competition with the natural ligand lactoferrin, by colocalization with the nucleolin-binding aptamer AS1411, and by the marked sensitivity of RMS cell lines to the growth inhibitory nucleolin-binding N6L pseudopeptide. Taken together, our results indicate that nucleolin-targeting by F3 peptide represents a potential therapeutic approach for RMS.
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Journal: AS1411 aptamer-functionalized exosomes in the targeted delivery of doxorubicin in fighting colorectal cancer. (Pubmed Central) - Oct 22, 2022
Subsequently, in-vivo experiments which were conducted on four groups of ectopic mouse models of colon cancer (5 in each group) demonstrated the tumor growth suppression through professional long-term accumulation and retention of DOX-Apt-Exo at the tumor site by ligand-receptor interaction. The results suggested that AS1411 aptamer-functionalized exosomes can be recommended as a safe and effective system to site-specific drug delivery in possible clinical applications of colon cancer.
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Journal: Insights into the binding mode of AS1411 aptamer to nucleolin. (Pubmed Central) - Oct 21, 2022
Our study provides the molecular basis of this specific binding and can guide rational AS1411-based aptamers design. Further insights require tight collaborations between the experiments and in silico studies.
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Journal: Development of a novel PROTAC using the nucleic acid aptamer as a targeting ligand for tumor selective degradation of nucleolin. (Pubmed Central) - Oct 18, 2022
To address this drawback, we developed a novel PROTAC ZL216 using aptamer AS1411 as a targeting ligand of nucleolin to conjugate with a small molecule ligand of E3 ligase VHL, which shows high aqueous solubility and serum stability...As a result, ZL216 inhibited the proliferation and migration of breast cancer cells. These studies demonstrate that in addition to peptides and small molecule compounds, nuclei acid aptamers can also be used to generate PROTACs, which broadens the toolbox constructing PROTACs and provides a promising strategy for development of tumor-selective PROTACs.
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Journal: In situ imaging miRNAs using multifunctional linear DNA nanostructure. (Pubmed Central) - Oct 14, 2022
The aptamer (AS1411) could media MLN-MB enter live cells without additional transfection reagents...With its outstanding stability, dual recognition, and biocompatibility, MLN-MB is capable of delivering into living cells to identify specific cancer cells. Therefore, our sensing approach, with high sensitivity, specificity, and simplicity advantages, holds great potential for early cancer diagnosis.
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Journal: Drug-Induced Self-Assembly Cascade Nanoreactor for Synergistic Tumor Therapy. (Pubmed Central) - Oct 7, 2022
Through active targeting and passive enhanced permeability and retention effect, the loading of AS1411 could promote the cascade bioreactors to effectively target nucleolin-overexpressed tumors...In vitro and in vivo studies showed that the cascaded nanoreactors could significantly enhance therapeutic efficacy through synergistic starvation therapy and enhanced PDT as well as chemotherapy. This cascade strategy will be demonstrated in clinical applications with huge potential.
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Journal: Gene-dosage effect of Pfkfb3 on monocyte/macrophage biology in atherosclerosis. (Pubmed Central) - Oct 6, 2022
This cascade strategy will be demonstrated in clinical applications with huge potential. Collectively, these findings suggest the existence of a double-edged sword effect of myeloid PFKFB3 on the pathogenesis of atherosclerosis and highlight the need for caution in developing anti-atherosclerotic strategies that target PFKFB3.
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Journal: PFKFB3 works on the FAK-STAT3-SOX2 axis to regulate the stemness in MPM. (Pubmed Central) - Oct 1, 2022
Collectively, these findings suggest the existence of a double-edged sword effect of myeloid PFKFB3 on the pathogenesis of atherosclerosis and highlight the need for caution in developing anti-atherosclerotic strategies that target PFKFB3. This study confers a comprehensive and mechanistic function of PFKFB3 in CSC maintenance that may foster exceptional opportunities for targeted small molecule blockade of the TICs in MPM.
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