QN-165 / Qualigen Therap, University of Louisville, Advanced Cancer Therap - LARVOL DELTA

Universal Microfluidic Platform for Multifunctional Surface Modification of Small Extracellular Vesicles. (PubMed, J Extracell Vesicles) - "Functionally, RGE peptide-modified sEVs exhibited a 54.13% increase in transmembrane transport efficiency in the in vitro model and enhanced infiltration into glioma spheroid, while AS1411 aptamer-conjugated sEVs showed 77.8% targeting specificity towards breast cancer cells, compared to 32.5% for normal breast cells...Unlike traditional donor-cell-dependent genetic modification approaches, ExoSE enables universal, scalable modification of sEVs from diverse sources, including highly abundant milk-derived sEVs, and accommodates diverse ligand types such as peptides, aptamers and proteins. This device represents a transformative advancement in sEV engineering, establishing a standardized and scalable framework for precision-targeted sEV therapeutics with enhanced clinical potential."

Journal • Brain Cancer • Breast Cancer • Glioma • Oncology • Solid Tumor

Dual-Mode Aptamer AP1-F Achieves Molecular-Morphological Precision in Cancer Diagnostics via Membrane NCL Targeting. (PubMed, Curr Issues Mol Biol) - "By means of rigorous optimization, AP1-F attained a greater than ten-fold fluorescence signal ratio between malignant and normal cells in co-cultures, exceeding the extensively researched AS1411...This combination biochemical-morphological approach accomplished subtype differentiation with a single-step, non-permeabilized process that maintained lower cytotoxicity and tissue integrity. AP1-F enhances diagnostic accuracy by utilizing spatial confinement to eradicate intracellular interference, connecting molecular specificity to intraoperative margin evaluation or biopsy categorization."

Journal • Oncology • NCL

A dual-enzyme-like nanozyme adjuvant alleviates tumor hypoxia to enhance photothermally ferroptosis-immune synergistic tumor therapy. (PubMed, Mater Today Bio) - "Herein, we developed a dual-enzyme-like nanozyme adjuvant (Mn3O4&MLT@PDA-AS1411, MMPA) through the integration of Mn3O4 nanozyme and melatonin (MLT) using polydopamine, which alleviates tumor hypoxia to enhance photothermally augmented ferroptosis-immune synergistic therapy...In vivo studies demonstrate that this strategy effectively alleviates tumor hypoxia, resulting in the complete suppression of distant tumors in a metastatic model. This approach also first explores the promotion of ferroptosis and immune activation of MLT, providing an innovative strategy for multi-mechanism synergistic treatment."

Journal • Immune Modulation • Immunology • Oncology • HIF1A

Enhancing the intracellular delivery of antisense oligonucleotides (ASO) : a comparative study of aptamer, vitamin E, and cholesterol ASO conjugates. (PubMed, RSC Adv) - "The ASO PNAT524 was conjugated to two DNA aptamers-AS1411 and S2.2-via thiol and triethylene glycol (TEG) linkers, respectively...These findings indicate that aptamer conjugation provides minimal benefit for ASO delivery, while cholesterol and vitamin E conjugation significantly enhance intracellular delivery and therapeutic activity. The 524-Chol conjugate holds strong potential for adaptation in ASOs targeting EGFR and other oncogenes, representing a promising avenue for ASO-based cancer therapeutics."

Journal • Oncology • EGFR

Nucleolin perturbation alters membrane lipid homeostasis. (PubMed, Mol Omics) - "Ratiometric imaging of Di-4-ANEPPS-labeled cells showed that AS1411 decreases the fluidity of intracellular membranes. Thus, aptamer engagement of nucleolin affects lipid biosynthesis and homeostasis, likely contributing to its roles in cell size control."

Journal • Oncology • NCL

A dual-multivalent aptamer-DNA nanocarriers for enhancing antitumor effects of photodynamic-chemotherapy combined therapy. (PubMed, Colloids Surf B Biointerfaces) - "AMH-Ncas had an RCA scaffold with repeats units, which can self-assemble with the functional complementary chains of AS1411 aptamers, MUC1 aptamers and hypoxia inducible factor 1α (HIF-1α) antisense DNA. The thermodynamic data of the binding of photosensitizer new methylene blue N (NMBN) and chemotherapeutic drug doxorubicin (DOX) to AMH-Ncas indicated that AMH-Ncas had higher drug loading capacity and the first loading of NMBN was more favorable...AMH-Ncas + NMBN + DOX system exhibited excellent synergistic anti-tumor effects. This study provides a theoretical basis for the co-delivery of combined drugs by DNA nanocarriers to achieve enhanced PDT-chemotherapy synergistic therapy."

Journal • Oncology • HIF1A • MUC1

In Situ PROTAC Synthesis Enabled by Pathologically Activated Bioorthogonal Catalysis for Precision Cancer Therapy. (PubMed, J Am Chem Soc) - "These components are encapsulated within AS1411 aptamer-conjugated liposomes to enhance cellular uptake and systemic delivery...The modularity of the ABC-PROTAC strategy is demonstrated by utilizing diverse warheads, including small molecules and DNA motifs, to degrade BRD4, PARP1, and NF-κB. Together, this strategy establishes a precise method for targeted protein degradation while minimizing the systemic toxicity associated with conventional PROTACs."

Journal • Oncology • Targeted Protein Degradation • BRD4 • NCL • PARP1

Nanoscale mapping of nucleolin-aptamer interactions on lung cancer cells reveals binding affinity hierarchy and spatial heterogeneity. (PubMed, Anal Methods) - "This study localized nucleolin on lung cancer and normal cells at single-molecule resolution using the single molecule recognition imaging mode of Atomic Force Microscopy (AFM) with three aptamers: 9FU-AS1411, AS1411, and CRO...This work pioneers high-resolution spatial mapping of nucleolin-aptamer interactions, offering novel methodologies for studying protein-aptamer binding kinetics and electrical properties at unprecedented precision (0.1 mV resolution). The approaches established here not only advance nucleolin-targeted cancer therapy but also provide a framework for investigating other protein-aptamer systems in biomedical research."

Heterogeneity • Journal • Lung Cancer • Oncology • Solid Tumor • NCL

Nucleolin-Targeted DNA Nanoflowers Enable Multimodal Synergistic Cancer Therapy. (PubMed, Biomater Res) - "AS1411 aptamer, coded in the long single-stranded DNA sequence, provided GCD with tumor-targeting ability, enhancing its bio-safety...We also examined immune cell death induction and the immune regulation role of GCD and found that the combination of anti-programmed death-1 antibody further enhanced its antitumor effect. These results contribute to the further study and application of copper-based drug development."

Journal • Oncology • NCL

Shattering kinetic constraints: hierarchically activatable DNAzyme nanoantennas for in situ mRNA imaging and precise cancer theranostics. (PubMed, Biosens Bioelectron) - "Once encountering cancer cells, hairpin 1 (H1) recognizes the nucleolin via an aptamer AS1411, and meanwhile the i-motif in H1 undergoes structure switching at extracellular acid pH, enabling the cross-opening of H2, H3, H4, H5 for in situ self-assembly of two-sided DNAzyme nanoantennas...It can profile Egr-1 mRNA level in diverse human cells, and distinguish Egr-1 mRNA level in breast cancer tissues and healthy counterparts. Moreover, it can be applied for high-contrast imaging of Egr-1 mRNA in vivo, efficient gene silencing, and enhanced tumor ablation, with promising applications in smart gene therapeutics and precise nanomedicines."

Journal • Breast Cancer • Gene Therapies • Oncology • Solid Tumor • NCL

AS1411 Aptamer-Conjugated Liposomal siRNA Targeting MTA2 Suppresses PI3K/AKT Signaling in Pancreatic Cancer Cells. (PubMed, Int J Mol Sci) - "Treatment of MIA PaCa-2 cells with AS1411-Lipm[siRNA] significantly reduced MTA2 expression by ~60%, substantially restored PTEN, and inhibited AKT phosphorylation by ~50%, leading to decreased cell viability, impaired migration by ~75%, and increased apoptosis by ~35%, while sparing nucleolin-negative cells. These findings highlight AS1411-Lipm[siRNA] as a promising platform for selective siRNA delivery and potent molecular inhibition in PDAC therapy."

Journal • Oncology • Pancreatic Cancer • Pancreatic Ductal Adenocarcinoma • Solid Tumor • MTA2 • NCL • PTEN

An aptamer-conjugated mesoporous polydopamine formulation for synergistic targeted and photothermal therapy of hepatocellular carcinoma. (PubMed, Int J Pharm X) - "This study aimed to create multifunctional nanoparticles (NPs), specifically AS1411@MPDA-Len-Cy5.5 (AMLC), for the purpose of developing effective strategies for treating hepatocellular carcinoma (HCC) through targeted therapy and photothermal therapy (PTT). The study demonstrates that AMLC, a multifunctional nano-delivery system, significantly enhances Lenvatinib's tumor-targeting capacity while exhibiting excellent biocompatibility. Combined with photothermal therapy (PTT), it demonstrates potent antitumor efficacy, showing promising clinical translation potential for hepatocellular carcinoma (HCC) therapy."

Journal • Hepatocellular Cancer • Oncology • Solid Tumor

Au-CuS Hierarchical Self-Assembled Multimodal Diagnosis and Treatment Platform for the Synergistic Treatment of Melanoma. (PubMed, Langmuir) - "To further enhance the targeting ability of AuNRs-D12-CuS, we modified the surface with the AS1411 aptamer to achieve specific recognition of overexpressed nucleolin on the surface of B16. In addition, doxorubicin (DOX) was effectively incorporated into the AuNRs-D12-CuS, forming a multifunctional nanosystem with chemotherapeutic function (AuNRs-D12-CuS@DOX), and its drug encapsulation efficiency reached approximately 64%...In vitro experimental results showed that after labeling the prepared composite nanomaterials with nucleic acid red dye (NA-red), the material exhibited excellent fluorescence imaging performance when coincubated with cells for 30 min. In addition, under low-dose conditions, its killing efficiency against B16 cells could reach 50%, which was significantly superior to single-drug treatment or simple photothermal therapy."

Journal • Melanoma • Oncology • Solid Tumor • DNA2 • NCL

Neutrophil-Inspired Film for Nonadhesive Capture of Tumor Cells through Synergistic Functionalization of Zwitterions and Aptamers. (PubMed, Chem Bio Eng) - "Then, amino-modified aptamer (NH2-AS1411) targeting tumor cells, mimicking the β-integrin on neutrophil membranes, was further grafted onto hydrolyzed PAN surface to obtain the AS/PScG/PU-PAN film. The resulting AS/PScG/PU-PAN film demonstrates excellent specific capture ability of tumor cells, while maintaining the morphology of tumor cells, providing a promising solution for cancer therapy."

Journal • Oncology • VCAM1

Computational simulations of RNA-based aptamers targeting EpCAM+ breast cancer cells (ACS-Fall 2025) - "Based on these analyses, aptamer AS1411 was selected as the most appropriate candidate for EpCAM-mediated breast cancer cell detection. This work advances the potential of EpCAM-targeted aptamers as targeted therapeutic and diagnostic agents against breast cancer."

Breast Cancer • Oncology • Solid Tumor • EPCAM

Sonodynamic Therapy-Based DNA Nanocarriers with Hypoxia-Inducible Factor-1α Silencing Activation for Precision Lung Cancer Therapy. (PubMed, Biomater Res) - "In this study, manganese-containing DNA nanoflowers (DHA-DDF) loaded with doxorubicin (DOX) were functionalized with an AS1411 aptamer and a hypoxia-inducible factor-1α (HIF-1α) antisense sequence...The programmable, biocompatible, and multifunctional nanoflowers demonstrate a notable improvement in the efficacy of SDT and provide robust tumor inhibition in both cellular and animal models. The findings highlight the potential of DNA nanotechnology in advancing innovative cancer therapies."

Journal • Lung Cancer • Oncology • Solid Tumor • HIF1A

AS1411 aptamer in melanoma therapy: Harnessing targeted strategies for precision treatment. (PubMed, Pathol Res Pract) - "Additionally, AS1411-conjugated therapies, including peptide and siRNA constructs, show potential in disrupting tumor vasculature and silencing cancer-related genes. Overall, AS1411-modified nanoparticles represent a transformative approach in skin cancer therapy, warranting further clinical investigation."

Journal • Review • Genetic Disorders • Melanoma • Oncology • Skin Cancer • Solid Tumor • NCL

Anti-nucleolin aptamer-guided anticancer activity of AS1411-Chalcone conjugate in breast cancer. (PubMed, Biochem Biophys Res Commun) - "Moreover, the conjugate exhibited reduced cytotoxicity toward normal HDF cells and induced cell cycle arrest and apoptotic cell death selectively in cancer cells. These findings highlight the potential of AS1411-mediated chalcone delivery as a targeted therapeutic strategy that enhances drug potency while minimizing off-target effects."

Journal • Breast Cancer • Oncology • Solid Tumor • NCL

NIR-Responsive Carbon Dots Functionalized with AS1411 Aptamer: A Dual-Mode Approach to Enhanced Photothermal and Photodynamic Therapy. (PubMed, ACS Appl Bio Mater) - "In vitro experiments demonstrated that IRCDs@AS1411 served as effective agents for bioimaging, PDT, and PTT, overcoming the limitations of traditional organic dyes and efficiently eradicating tumor cells under 808 nm laser irradiation. These findings suggest that IRCDs@AS1411 hold significant promise for advanced cancer therapy and provide a versatile platform for developing other functional nanomaterials."

Journal • Oncology

Programmable Biporphyrin-G-Quadruplex Nanoflowers for Simultaneous Tumor Cell Recognition and Enhanced Photodynamic Therapy. (PubMed, Small Methods) - "The spatial arrangement of AS1411 aptamers and G4 motifs within the DNA nanoflowers increases the binding specificity to cancer cells, thereby facilitating targeted detection. Furthermore, the incorporation of hemin into the G4 complex endows the nanoflowers with peroxidase-like catalytic activity, enabling colorimetric detection of tumor cells through endogenous hydrogen peroxide production. This catalytic process generates oxygen to alleviate hypoxia within the TME and amplifies the production of reactive oxygen species (ROS), thereby enhancing PDT effectiveness. Additionally, the multifunctional DNA nanoflowers induce both ferroptosis and apoptosis in cancer cells, effectively inhibiting the progression of triple-negative breast cancer. In summary, these multifunctional DNA nanoflowers offer a promising and highly selective approach to enhancing cancer treatment outcomes."

Journal • Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer

Nucleolin as a Crucial Player in Head and Neck Cancer: Diagnostic and Therapeutic Perspectives. (PubMed, Curr Cancer Drug Targets) - "This review provides a fresh perspective on the underexplored potential of NCL as a therapeutic target in HPV-induced HNC and oral cancer. Emerging approaches, such as the AS1411 aptamer and F3 peptide, offer promising avenues for targeting NCL, paving the way for more effective, personalized cancer therapies."

Journal • Head and Neck Cancer • Human Papillomavirus Infection • Infectious Disease • Oncology • Oral Cancer • Solid Tumor • Squamous Cell Carcinoma • NCL

Novel Anticancer Triple Formula Based on Aptamer-Conjugated PEGylated Nanoliposomes. (PubMed, Technol Cancer Res Treat) - "The AS1411 aptamer was conjugated to the nanoliposomes to target nucleolin, a protein overexpressed in cancer cells...The encapsulation efficiencies were 88.63% (raloxifene), 41.73% (etoricoxib), and 39.26% (naringin) without the aptamer, and 81.99%, 36.66%, and 38.33%, respectively, with the aptamer. The IC50 of the formula for the three co-loaded agents was 167.4 µg/mL for A549 cells and 2.6 µg/mL for MCF-7 cells. Cytotoxicity was further enhanced using their aptamer conjugate, particularly against the MDA-MB-231 cell line.ConclusionThe novel triple-drug-loaded, aptamer-conjugated nanoliposome formula may be a future cancer treatment strategy."

Journal • Oncology • NCL

Tumor microenvironment-responsive dynamic self-assembly of DNAzyme nanowires for high-contrast imaging of multiple messenger RNAs and chemotherapy. (PubMed, Biosens Bioelectron) - "We design a cruciform DNA module (C-model) as a basic structural unit of DNAzyme nanowire, which consists of two DNAzyme strands and two substrate strands with the chemotherapeutic drug doxorubicin (DOX) being inserted into the C-models by inlaying between guanine and cytosine...AS1411 aptamer-functionalized DOX-nanowires can selectively endocytose into cancer cells via AS1411-mediated recognition of nucleolin overexpressed on the cancer cell surface. Notably, the dynamic self-assembly of DNAzyme nanowires is characterized by efficient intracellular delivery and intrinsic resistance to nucleases, facilitating the high-contrast imaging of mRNAs. This method can accurately measure TK1 mRNA and GalNAc-T mRNA in living cells and discriminate multiple mRNAs in breast cancer tissues and their normal counterparts, providing a powerful platform for clinical diagnosis."

Biomarker • Journal • Breast Cancer • Gene Therapies • Oncology • Solid Tumor • NCL

Shared molecular biomarkers and therapeutic targets in rheumatoid arthritis and osteoarthritis: Focus on EIF3B, KHSRP, NCL, PDCD1LG2, and SLC25A37. (PubMed, Cytokine) - "Several hub genes were targeted by existing drugs, such as NCL by AS1411, and PDCD1LG2 by Pembrolizumab. Mitoferrin 1 expression showed no significant differences among groups. These findings suggest that RA and OA share common molecular pathways that may serve as promising diagnostic biomarkers and therapeutic targets."

Biomarker • Journal • Immunology • Osteoarthritis • Pain • Rheumatoid Arthritis • Rheumatology • Targeted Protein Degradation • NCL • PD-L2 • SLC25A3 • SLC25A37 • SLC5A7

NIR-II Fluorescence Imaging-Guided Combinatorial Therapy of Breast Cancer Using ICG/Chelerythrine-Loaded Aptamer-Targeted Liposomes. (PubMed, ACS Appl Bio Mater) - "To address this, we developed AS1411 aptamer-functionalized liposomes coloaded with indocyanine green (ICG) and chelerythrine (I/C@Lipo-A) for enhanced breast cancer theranostics...This combinatorial strategy not only suppressed primary tumor growth but also inhibited distant metastases, significantly improving survival rates. Our work presents a robust, multifunctional platform for precision breast cancer theranostics, overcoming key barriers in drug delivery and imaging-guided therapy."

Journal • Breast Cancer • Metabolic Disorders • Oncology • Solid Tumor