- |||||||||| QN-165 / Qualigen Therap
Journal: Albumin-conjugation enables improved tumor targeting of aptamers via SPECT imaging. (Pubmed Central) - Mar 14, 2025
The immunofluorescence staining of tumor tissues further indicated the improved tumor retention of AS1411 as a result of prolonged blood circulation. Therefore, the HSA-conjugated strategy has a promising prospect in improving aptamers' tumor targeting for clinical applications.
- |||||||||| QN-165 / Qualigen Therap, paclitaxel / Generic mfg.
Journal: Framework nucleic acid-programmed aptamer-paclitaxel conjugates as targeted therapeutics for triple-negative breast cancer. (Pubmed Central) - Mar 13, 2025
Furthermore, the AS1411-specifically modified FAPC further enhances the structure-dependent selective accumulation of drugs at tumor sites in a human xenograft model of triple-negative breast cancer, subsequently leading to significantly improved antitumor efficacy and reduced toxicity. The FAPC provides a precisely programmable platform for efficient targeted delivery of chemotherapeutic agents to malignancies.
- |||||||||| QN-165 / Qualigen Therap, Avastin (bevacizumab) / Roche
Journal: Nanoparticle Formulations for Intracellular Delivery in Colorectal Cancer Therapy. (Pubmed Central) - Mar 9, 2025
In vitro studies also demonstrated a significant reduction in cell viability in human colon tumor organoids exposed to AP-BEV?+?M1A-EXO. These findings highlight the potential of combining aptamer specificity with exosome-based delivery systems to enhance the precision and efficacy of colorectal cancer therapies, marking a promising step forward in cancer treatment innovation.
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Journal: Probing Structural Variants of Irregular DNA G-Tracts (N ? 2) Using MspA Nanopores. (Pubmed Central) - Mar 6, 2025
Our results demonstrated that in an electric field, the tumor-targeting element AS1411, along with its derivatives AT11 and Z-G4, strongly interacted with the M2-MspA nanopore, resulting in at least two distinct populations (types I and II events) characterized by different current blockage fractions and dwell times...Furthermore, voltage-dependent dynamics revealed that Z-G4 exhibited extended dwell times for docking and partial unwinding, unlike AT11. Our in-solution nanopore experiments and MD simulation results would benefit toward understanding the folding principles of complicated structural variants by sequences consisting of multiple short G-tracts, paving the way for the rapid identification of similar-sequence nucleic acid aptamers in molecular diagnostics and targeted therapies.
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Journal, PD(L)-1 Biomarker, IO biomarker: DNA origami-based composite nanosandwich for iteratively potentiated chemo-immunotherapy. (Pubmed Central) - Feb 16, 2025
Furthermore, the superior antitumor effect of DSWAC/siPD-L1 resulted in approximately 91?% inhibition of primary tumor growth and 93?% prevention of lung metastasis. Collectively, this study describes a siPD-L1-based sandwich DNA nanodevice functionalized with AS1411/CpG for enhanced cancer chemo-immunotherapy, inspiring the creation of more innovative drug nanocarriers and the exploitation of novel cancer therapies.
- |||||||||| QN-165 / Qualigen Therap, cabazitaxel / Generic mfg.
Journal: Construction of anticancer drug incorporated aptamer-functionalized cationic ?-lactoglobulin: induction of cell cycle arrest and apoptosis in colorectal cancer. (Pubmed Central) - Feb 11, 2025
A novel nanocarrier, aptamer (AS1411)-conjugated ?-lactoglobulin/poly-l-lysine (BLG/Ap/PL) nanoparticles, was developed in this study...By loading cabazitaxel (CTX) onto the nanocarriers, the therapeutic potential of BLG/Ap/PL could be demonstrated...Annexin V/propidium iodide (PI) flow cytometry analysis confirmed that CTX@BLG/Ap/PL induces apoptosis in HCT116 cells. Overall, this study proved that CTX@BLG/Ap/PL had several advantages over free chemotherapeutic drugs and showed promise as a solution to the clinical problems associated with targeted antitumor drug delivery systems.
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Journal: Nanoparticle-aptamer based cytosensing for the detection of human non-small cell lung cancer cells. (Pubmed Central) - Feb 6, 2025
The AS1411 aptamer can adsorb onto the surface of AuNPs, effectively preventing their aggregation...This proposed aptasensor platform demonstrates high specificity for A549 cells when compared to other control human normal cells. The method exhibits a dynamic range of 101 to 106 cells per mL, with a detection limit of 7 cells per mL.
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Preclinical, Journal: Evaluation of a Radioiodinated G-quadruplex Binder in Cervical Cancer Models. (Pubmed Central) - Dec 16, 2024
The respective supramolecular conjugate with the AS1411 aptamer ([125I]-C8/AS1411) led to a slower blood clearance in the same animal tumor model, although without improving the tumor uptake. To take advantage of the radiotoxicity of [125I]-C8 against cervical cancer cells other strategies need to be studied, based namely on alternative nanodelivery carriers and/or
- |||||||||| QN-165 / Qualigen Therap
Journal: Development of hybrid aptamers-engineered PROTACs for degrading VEGF165 in both tumor- and vascular endothelial cells. (Pubmed Central) - Dec 1, 2024
The aptamer AS1411 is notable for its ability to selectively recognize and enter both tumor and vascular endothelial cells by targeting the cell surface nucleolin (NCL)...The PROTACs inhibit the growth of tumor cells and also impede angiogenesis, without causing toxicity to normal tissues. The hybrid aptamers-engineered PROTACs provide an avenue for disrupting the tumor-angiogenesis interplay through modulation of VEGF165 in both tumor and vascular endothelial cells.
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Journal: Engineering Nano-Pills to Inhibit Ovarian Cancer Proliferation and Migration through a Combination of Chemical/Nucleic Acid Therapy. (Pubmed Central) - Nov 22, 2024
Nano-pills are nanospheres assembled from miRNA and doxorubicin (DOX) with the help of ferrous ions (Fe2+)...The navigation element is the cholesterol-conjugated AS1411 aptamer...The results demonstrate the homing effect of tumor microenvironment-derived macrophage cell membrane and the targeting effect of aptamer, leading to precise drug targeting and immune compatibility, thereby enhancing therapeutic efficacy. The success of this strategy paves the way for metastasis inhibition and targeted cancer therapy.
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Journal: Engineering small extracellular vesicles with multivalent DNA probes for precise tumor targeting and enhanced synergistic therapy. (Pubmed Central) - Nov 19, 2024
Multivalent DNA probes, comprising abundant AS1411 aptamers and telomerase primers, were innovatively modified on the sEV membrane (M-D-sEV) for precise tumor targeting...In vitro and in vivo studies demonstrated the remarkable targeting ability of multivalent DNA probes and excellent therapeutic effect of this strategy. The engineered strategy of sEVs provide a promising approach for precise tumor therapy and hold great potential for the development of efficient, safe, and personalized drug delivery systems.
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Journal: An intelligent poly aptamer-encoded DNA nanoclew for tumor site activated mitochondria-targeted photodynamic therapy and MR imaging. (Pubmed Central) - Nov 14, 2024
Herein, a poly-AS1411 aptamer DNA nanoclew (AS-AMD) synthesized via rolling circle amplification (RCA) is developed, incorporating mitochondria-targeted PSs (APNO) and paramagnetic Mn2+ for mitochondria-targeted PDT and magnetic resonance imaging (MRI)...Additionally, AS-AMD exhibits effective tumor targeting in the 4T1-tumor-bearing mice model, significantly enhanced MRI performance and PDT efficacy. Therefore, this study introduces an interesting strategy to achieve efficient mitochondrial-targeted delivery of cationic PSs and provides a versatile biocompatible DNA nanoplatform for the development of nanotheranostic agents.
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Journal, Tumor cell: Acidic Extracellular pH-Activated Allosteric DNA Nanodevice for Fluorescence Imaging of APE1 Activity in Tumor Cells. (Pubmed Central) - Nov 13, 2024
Inspired by allosteric regulation of natural molecules, we present a Y-shaped allosteric DNA nanodevice, termed YssAP, that was pH-responsive and functionalized with the AS1411 aptamer for accurate fluorescence imaging of human apurinic/apyrimidinic endonuclease (APE1) activity in tumor cells...Compared with the direct construction of the APE1 substrate, allosteric DNA nanodevices have more accurate imaging effects, which can be precisely adjusted by changing the switching state. We anticipate that this strategy will be applied in the screening of APE1 inhibitors and precise tumor diagnosis.
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Journal: Extracellular vesicles-hitchhiking boosts the deep penetration of drugs to amplify anti-tumor efficacy. (Pubmed Central) - Nov 13, 2024
This vector includes the AS1411 aptamer for tumor-specific targeting, the vesicular stomatitis virus glycoprotein (VSV-G) for tumor cell membrane fusion, and a photosensitizer as the therapeutic agent while ensuring optimal drug encapsulation and stability...The results suggest that this EVs-hitchhiking strategy enables photosensitizers to penetrate deeply into tumor tissue, thereby enhancing the efficacy of phototherapy. This study offers broad application prospects for delivering drugs deeply into tumor tissues.
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Journal: Enzymatic interlocking aptamer-micelles for enhanced cellular internalization and nucleus-targeted cancer phototherapy. (Pubmed Central) - Oct 26, 2024
In addition, the multivalent AS1411 aptamers tethered in the hydrophilic shell can simultaneously increase the specific binding affinity of DNA micelles and induce nucleus-targeted accumulation for DNA damage-triggered apoptosis. This DNA micelle achieves "best of both worlds" with enhanced biostability for cellular internalization and improved NIR photothermal conversion efficiency for nucleus-targeted therapy, which provides a promising formulation strategy for precision cancer treatment.
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Journal: Augmented the sensitivity of photothermal-ferroptosis therapy in triple-negative breast cancer through mitochondria-targeted nanoreactor. (Pubmed Central) - Oct 17, 2024
Unlike previously reported Fe-based nanomaterials, we have engineered a novel nanoreactor named IR780/Ce@EGCG/APT, which uses metal-polyphenols network (Ce@EGCG) based on rare-earth cerium and epigallocatechin gallate (EGCG) to encapsulate IR780 and modified with the aptamer (AS1411)...EGCG serves as a sensitizer, simultaneously enhancing the sensitivity of tumor cells to ferroptosis and photothermal therapy. After a single dose and three times of 808?nm laser irradiation for treatment, it has been observed that the nanoreactor induces dendritic cells (DCs) maturation, facilitates cytotoxic T lymphocyte infiltration, improves immunosuppressive microenvironment, activates the systemic immune system, and generates long-term immune memory.
- |||||||||| 5-fluorouracil / Generic mfg.
Journal: Delivery of 5-fluorouracil for cancer therapy using aptamer-based nonlinear hybridization chain reaction. (Pubmed Central) - Aug 24, 2024
This structure specifically targets cancer cells with overexpressed nucleolin on their surface, allowing the 5-FU to exert its anticancer effects and achieve therapeutic outcomes. Furthermore, we have also investigated the mechanistic action of this drug delivery system, aiming to establish a novel therapeutic platform for 5-FU treatment.
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Journal: Precise Preparation of Supramolecular Spherical Nucleic Acids for Nucleolin-Targeted Gene (Pubmed Central) - Aug 23, 2024
Specifically, we constructed a series of supramolecular self-assembly structures by coupling a cell membrane receptor (i.e., nucleolin)-recognizing aptamer (AS1411)-modified adamantine as targeting probe and human epithelial growth factor receptor 2 (HER2) antisense-functionalized ?-cyclodextrin to specifically inhibit the overexpression of HER2 proteins for gene regulations...We demonstrated that Supra-SNAs exhibited optimal cell suppression rates and cell apoptosis via a phosphatidylinositol 3-kinase/protein kinase B signaling pathway. The well-defined molecular structures provide an attractive platform for investigating interrelationship between structure and property at the molecular level.
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Journal: Japanese encephalitis virus NS5 protein interacts with nucleolin to enhance the virus replication. (Pubmed Central) - Aug 20, 2024
We show that the NCL-binding aptamer AS1411 containing the G-quadruplex (GQ) structure and the GQ ligand BRACO-19 caused significant inhibition of JEV replication...This may smoothen the movement of the replication complex along the genomic RNA, thereby facilitating the virus replication. This study is the first report on how NCL, a host protein, helps in JEV replication through GQ-binding.
- |||||||||| PFK-158 / Advanced Cancer Therap
Journal: Hypoxia activates macrophage-NLRP3 inflammasome promoting atherosclerosis via PFKFB3-driven glycolysis. (Pubmed Central) - Aug 3, 2024
In addition, we administered the PFKFB3 inhibitor PFK158 during atherosclerosis modeling...Our study demonstrated that the HIF-1?/PFKFB3/NLRP3 axis serves as a crucial mechanism for macrophage inflammation activation in the emergence of atherosclerosis. The therapeutic potential of PFKFB3 inhibition may represent a promising strategy for atheroprotection.
- |||||||||| QN-165 / Qualigen Therap
Preclinical, Journal: A DNA/Poly-(L-lysine) Hydrogel with Long Shelf-Time for 3D Cell Culture. (Pubmed Central) - Jul 20, 2024
DNA/PLL hydrogel provided a favorable microenvironment to support the proliferation of cells, which formed cell spheroid in 15 days. This protective coating strategy solves the long-standing problem on the shelf-time of DNA hydrogel, and is envisioned to promote the development of DNA hydrogel in more biomedical applications.
- |||||||||| QN-165 / Qualigen Therap
Journal: Selective inhibition of c-Met signaling pathways with a bispecific DNA nanoconnector for the targeted therapy of cancer. (Pubmed Central) - Jul 6, 2024
After c-Met-specific SL1 and nucleolin-specific AS1411 aptamers were integrated with STPA, STPA could bind to c-Met and nucleolin on the cell membrane...The results of in vivo experiments showed that STPA could specifically target to tumor site in xenograft mouse model, and inhibit tumor growth with low toxicity by downregulating c-Met pathways. This study provided a novel and simple strategy to develop c-Met-targeting drugs for the targeted therapy of cancer.
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Biomarker, Journal, Tumor microenvironment: Biointerface-Engineered Hybrid Nanovesicles for Targeted Reprogramming of Tumor Microenvironment. (Pubmed Central) - Jun 9, 2024
In this study, we have developed a hybrid nanovesicle by integrating M1-Exos with AS1411 aptamer-conjugated liposomes (AApt-Lips), termed M1E/AALs...By integrating multiple treatment modalities, P-I@M1E/AALs nanoplatform demonstrates a promising therapeutic approach for overcoming hypoxic and immunosuppressive TME by targeted TAM reprogramming and enhanced tumor photodynamic immunotherapy. This study highlights an innovative TAM-engineering hybrid nanovesicle platform for the treatment of tumors characterized by hypoxic and immunosuppressive TME.
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Biomarker, Journal, Tumor microenvironment: Energy-storing DNA-based hydrogel remodels tumor microenvironments for laser-free photodynamic immunotherapy. (Pubmed Central) - Jun 1, 2024
The system is constructed with two ultralong single-stranded DNA chains, which programmed partial complementary sequences and repeated G-quadruplex forming AS1411 aptamer for photosensitizer loading via hydrophobic interactions and ?-? stacking...In the mouse model of breast cancer, this hydrogel shows a remarkable tumor suppression rate of 78.3
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Journal: Formulation optimization of lyophilized aptamer-gold nanoparticles: Maintained colloidal stability and cellular uptake. (Pubmed Central) - May 22, 2024
Anti-nucleolin (NCL) aptamer AS1411 is the first anticancer aptamer tested in clinical trials...Quantitative PCR (qPCR) analysis of nucleolin-target gene expression also confirmed the effectiveness of AuNP/NCL-Apt. This study highlights the importance of selecting the proper type and concentration of cryoprotectant in the typical nanoparticle lyophilization process and contributes to our understanding of the physical and biological properties of functionalized nanoparticles upon lyophilization.
- |||||||||| QN-165 / Qualigen Therap
Journal: Multivalent dendritic DNA aptamer molecules for the enhancement of therapeutic effects. (Pubmed Central) - May 20, 2024
Integration of the antitumor aptamer AS1411 into DNA dendrons enhanced cellular uptake and antiproliferative activity in cancer cells. These findings demonstrate that the incorporation of multivalent aptamers into DNA dendrons can effectively boost their therapeutic effects.
- |||||||||| QN-165 / Qualigen Therap
Journal: Stimuli-Responsive Aptamer-Drug Conjugates for Targeted Drug Delivery and Controlled Drug Release. (Pubmed Central) - May 15, 2024
Specifically, we used different stimuli-responsive linkers to conjugate a tumor-targeting aptamer (i.e., AS1411) with drugs, forming the library of srApDCs for targeted cancer treatment...Our design hypothesis was validated by the experimental data, which indicated that the aptamer could selectively enhance uptake of the srApDCs and the linkers could be cleaved by pathological cues in the TME to release the drug payload, leading to a significant enhancement of therapeutic efficacy. These results underscore the potential of our approach, providing a promising methodology for cancer therapy.
- |||||||||| QN-165 / Qualigen Therap
An albumin coupling strategy improves aptamers' blood circulation and tumor targeting (Exhibit Hall D - Science Pavilion (Convention Center); Screen 8; In-Person Only) - May 8, 2024 - Abstract #SNMMI2024SNMMI_1798;
The albumin coupling strategy has greatly overcome the poor pharmacokinetics and unsatisfied tumor uptake of AS1411. Given the excellent biocompatibility of HSA, we strongly believe the strategy can improve the tumor targeting/therapeutic effect of aptamers and suggest excellent clinical application prospects.
- |||||||||| QN-165 / Qualigen Therap, SmarT cells / Nanjing Drum Tower Hospital, Endostar (recombinant human endostatin) / Simcere
Journal: A Reconfigurable DNA Framework Nanotube-Assisted Antiangiogenic Therapy. (Pubmed Central) - Apr 26, 2024
We also found that Endo-rDFN exhibited significant inhibition of angiogenesis and tumor growth, while also providing effective protection against multiorgan injury (heart, liver, spleen, kidney, lung, etc.) to some extent, without compromising the function of these organs. Our study demonstrates that rDFN represents a promising vector for reducing antiangiogenic therapy-induced multiorgan injury, highlighting its potential for promoting the clinical application of antiangiogenic agents.
- |||||||||| QN-165 / Qualigen Therap
Journal: A responsive disulfide bond switch aptamer prodrug exhibiting enhanced stability and anticancer efficacy. (Pubmed Central) - Apr 22, 2024
In this paper, the development of AS1411 prodrug-type aptamers for tumor treatment was introduced...Furthermore, in the reducing microenvironment of tumor cells, disulfide bonds triggered drug release, resulting in superior therapeutic effects in vitro and in vivo compared to original drugs. This paper proposes a novel approach for optimizing the structure of nucleic acid drugs, that promises to protect other oligonucleotides or secondary structures, thus opening up new possibilities for nucleic acid drug design.
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