RNA aptamers and uses thereof
Inventors
Serafini, Paolo • Bicciato, Silvio • Caroli, Jimmy • De La Fuente, Adriana • Simaeys, Dimitri Van • Zilio, Serena • Bronte, Vincenzo
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Assignees
Modena And Reggio Emilia Unimore, University of • Verona, University of
MemberUniversity of MiamiUniversity of MiamiThe University of Miami, established in 1925 and based in Coral Gables, Florida, is a private research university recognized for its comprehensive academic offerings, robust research infrastructure, and strong interdisciplinary focus. Home to more than 19,000 students and with more than 400 acres of campuses across the Miami region, its mission encompasses education, research, innovation, and community service. The institution supports clinical, biomedical, marine, and atmospheric research initiatives, delivers diverse undergraduate and graduate programs, and maintains numerous research centers and institutes dedicated to scientific, medical, and societal advancements.
The University of Miami, established in 1925 and based in Coral Gables, Florida, is a private research university recognized for its comprehensive academic offerings, robust research infrastructure, and strong interdisciplinary focus. Home to more than 19,000 students and with more than 400 acres of campuses across the Miami region, its mission encompasses education, research, innovation, and community service. The institution supports clinical, biomedical, marine, and atmospheric research initiatives, delivers diverse undergraduate and graduate programs, and maintains numerous research centers and institutes dedicated to scientific, medical, and societal advancements.
Publication Number
US-12648996-B2
Publication Date
2026-06-09
Expiration Date
Abstract
Described herein and RNA aptamers that specifically bind to tumor-infiltrating myeloid cells and uses thereof.
Core Innovation
The invention provides RNA aptamers comprising nucleic acid sequences set forth in SEQ ID NOs: 3, 6, 11, 12, 14, and 15. These RNA aptamers specifically bind tumor-infiltrating myeloid cells (TIMC) across multiple mouse models and preferentially recognize human TIMC in recurrent head and neck squamous cell carcinoma (HNSCC). The description further associates selected aptamers with putative ligands, including ANXA4 for aptamer 3 and vimentin for aptamer 11.
The aptamers accumulate in tumors in vivo and are usable as conjugates. In one use, an aptamer is conjugated to a chemotherapeutic agent, including doxorubicin, to increase tumor-site drug concentration and therapeutic index relative to free doxorubicin or Doxil, with reduced systemic toxicity.
The description also reports aptamer-mediated delivery of siRNA to TIMC and associated gene silencing, including silencing of CCR1/CCR5. In addition, the description states methods for detecting TIMC by using aptamer conjugates to detectable labels, including approaches compatible with imaging and flow cytometry as part of TIMC identification in relevant contexts.
Claims Coverage
The independent claim identified in the provided material is directed to an RNA aptamer sequence set (six SEQ ID NOs) that is conjugated to either a chemotherapeutic agent or a nucleic acid molecule. Dependent claims further specify the chemotherapeutic agent, the nucleic acid type, and method uses for delivery to tumor-infiltrating myeloid cells and detection using a detectable label.
RNA aptamer conjugate defined by SEQ ID sets
An RNA aptamer comprising the nucleic acid sequence set forth in SEQ ID NOs: 3, 6, 11, 12, 14, and 15 conjugated to a chemotherapeutic agent or a nucleic acid molecule.
Doxorubicin-conjugated aptamer
The RNA aptamer of the conjugate wherein its chemotherapeutic agent is doxorubicin.
Nucleic acid molecule types for aptamer conjugates
The RNA aptamer conjugate wherein the nucleic acid molecule is DNA, RNA, shRNA, siRNA, or miRNA.
Aptamer-mediated delivery to tumor-infiltrating myeloid cells
A method delivers a therapeutic to a tumor-infiltrating myeloid cell by contacting the cell with the aptamer of the conjugate, wherein the therapeutic is either a chemotherapeutic agent or a nucleic acid molecule.
Aptamer-based detection of tumor-infiltrating myeloid cells
A method detects tumor-infiltrating myeloid cells in a biological sample by contacting the sample with an aptamer conjugated to a detectable label.
Across the independent claim and its refinements, the patent centers on RNA aptamers defined by SEQ ID NOs 3, 6, 11, 12, 14, and 15, conjugated to either chemotherapeutic agents or nucleic acid molecules, with uses in delivering therapeutics to tumor-infiltrating myeloid cells and detecting those cells using detectable-label conjugates.
Stated Advantages
Increased tumor-site drug concentration and therapeutic index versus free doxorubicin or Doxil.
Reduced systemic toxicity.
Gene silencing in tumor-infiltrating myeloid cells, including CCR1/CCR5 silencing.
Documented Applications
Delivery of therapeutics to tumor-infiltrating myeloid cells using aptamer conjugates, including delivery of siRNA for gene silencing (CCR1/CCR5).
Detection of tumor-infiltrating myeloid cells in a biological sample using aptamer conjugates to detectable labels.
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