Aptamer Conjugates with N-Heterocyclic Carbene Metal Complexes for Targeted Drug Delivery

• Main Authors: Veige, Adam S, Niu, Weijia, Garner, Mary E
• Format: Patent
• Language: English
• Published: 29.10.2020
• Subjects: BEER; BIOCHEMISTRY; CHEMISTRY; COMPOSITIONS THEREOF; CULTURE MEDIA; ENZYMOLOGY; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; MICROBIOLOGY; MICROORGANISMS OR ENZYMES; MUTATION OR GENETIC ENGINEERING; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; PROPAGATING, PRESERVING OR MAINTAINING MICROORGANISMS; SPIRITS; VINEGAR; WINE

An aptamer-N-heterocyclic-carbene metal complex conjugate (aptamer-NHCM conjugate) or an aptamer-bis-N-heterocyclic-carbene metal complex conjugate (aptamer-bis-NHCM conjugate) includes an aptamer coupled through a hydrolytically stable bond to an N-heterocyclic-carbene metal complex (NHCM) or a bis-N-heterocyclic-carbene metal complex (bis-NHCM). The aptamer-NHCM conjugate is prepared where the chosen aptamer displays selective binding to a cell specific receptor, such that the cytotoxic NHCM can be directed specifically to cells responsible for a target disease (e.g., a specific cancer type). A method of preparing the aptamer-N-heterocyclic-carbene metal complex conjugate involves installing a coupling group to an N-heterocyclic-carbene metal complex that can specifically bond with a functional group on an aptamer; the bond, covalent or non-covalent, is stable hydrolytically in the absence of an environment that promotes intentional cleavage of the bond.