# US 11,299,740 B2 · Artificial chemical entity comprising a DNA oligonucleotide aptamer that selectively binds MUC1 antigen > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 11,299,740 B2 - Document ID: US11299740B2 - Status: Granted - Kind: B2 - Application number: 16/476,297 - Filed: 2018-01-29 - Published: 2019-11-21 - Granted: 2022-04-12 - Earliest claimed: 2017-01-30 - Applicants: Ofer Nussbaum; Boaz Musafia - Inventors: Ofer Nussbaum; Boaz Musafia - Web page: https://patentgrep.com/patent/US11299740B2 ## CPC - C12N 15/115: Aptamers, i.e. nucleic acids binding a target molecule specifically and with high affinity without hybridising therewith {; Nucleic acids binding to non-nucleic acids, e.g. aptamers} - A61K 47/549: {Sugars, nucleosides, nucleotides or nucleic acids} - A61K 47/65: Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers - A61P 31/14: for RNA viruses - A61P 31/18: for HIV - A61P 35/00: Antineoplastic agents - A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection - A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14) - C07K 16/00: Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies - C07K 16/22: against growth factors {; against growth regulators} - C07K 16/3092: {against tumour-associated mucins} - C07K 2317/21: from primates, e.g. man - C07K 2317/30: characterized by aspects of specificity or valency - C07K 2317/32: specific for a neo-epitope on a complex, e.g. antibody-antigen or ligand-receptor - C07K 2317/52: Constant or Fc region; Isotype - C07K 2317/732: Antibody-dependent cellular cytotoxicity [ADCC] - C07K 2317/734: Complement-dependent cytotoxicity [CDC] - C12N 2310/16: Aptamers - C12N 2310/3513: Protein; Peptide - C12N 2310/3519: Fusion with another nucleic acid - C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00) - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS - C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00) ## Abstract Disclosed are artificial chemical entities, pharmaceutical compositions comprising such chemical entities and methods using the chemical entities. In some embodiments, the artificial chemical entity comprises a biomarker-bonding portion that selectively binds to a specified biomarker and an immune-response trigger that under in vivo conditions leads to positioning of an antibody Fc region in proximity of the biomarker to which the biomarker-bonding portion is bound. ## Claims ### Claim 1 An artificial chemical entity, comprising: a. a biomarker-bonding portion comprising a DNA oligonucleotide aptamer that selectively binds to Muc1 antigen; and b. an immune-response trigger comprising IgG or an Fc region of IgG; wherein under in vivo conditions binding of the biomarker-bonding portion to Muc1 antigen on a cell positions the IgG Fc region in proximity of said Muc1 antigen. ### Claim 2 (depends on 1) The chemical entity of claim 1, wherein said biomarker-bonding portion comprises a Muc1-binding oligonucleotide aptamer selected from the group consisting of an oligonucleotide set forth herein as SEQ ID NO: 3 and SEQ ID NO: 4. ### Claim 3 (depends on 1) The chemical entity of claim 1, wherein said biomarker-bonding portion is bonded to said immune-response trigger with a non-covalent associative bond. ### Claim 4 (depends on 1) The chemical entity of claim 1, wherein said biomarker-bonding portion is directly covalently bonded with a covalent bond to said immune-response trigger. ### Claim 5 (depends on 4) The chemical entity of claim 4, wherein said covalent bond is through a residue of a reactive group selected from the group consisting of NH2, SH, COOH, PO4, tosyl, thiol, a photo-reactive group, a click-chemistry group and a member of an affinity couple. ### Claim 6 (depends on 1) The chemical entity of claim 1, further comprising a linker bonded to said biomarker-bonding portion. ### Claim 7 (depends on 6) The chemical entity of claim 6, wherein said immune-response trigger is bonded to said linker. ### Claim 8 (depends on 6) The chemical entity of claim 6, wherein said linker is a chain comprising individual monomer residues selected from the group consisting of monosaccharide residues, nucleotide residues and combinations thereof. ### Claim 9 (depends on 1) A pharmaceutical composition comprising: the chemical entity of claim 1; and a pharmaceutically-acceptable carrier. ### Claim 10 (depends on 1) A method of treatment of breast cancer, comprising administering a pharmaceutically-effective amount of the chemical entity of claim 1 to a subject in need thereof.