# US 12,758,483 B2 · Antibacterial and mineralizing compositions and methods of use thereof

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- Number: US 12,758,483 B2
- Document ID: US12758483B2
- Status: Granted
- Kind: B2
- Application number: 18/546,733
- Filed: 2022-01-20
- Published: 2025-09-04
- Granted: 2026-10-13
- Earliest claimed: 2021-02-16
- Assignees: The University of Hong Kong
- Applicants: The University of Hong Kong
- Inventors: Hai Ming Wong; Quan Li Li; Li Zhou
- Web page: https://patentgrep.com/patent/US12758483B2

## CPC

- A61K 8/64: Proteins; Peptides; Derivatives or degradation products thereof
- A61Q 11/00: Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
- C07K 14/47: from mammals
- 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)
- A61Q: SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY 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

Peptides that bind with high affinity to oral cavity surfaces, such as tooth enamel, have been discovered. The peptides exhibit antibacterial and mineralizing abilities, and are useful in many aspects of oral care. A preferred peptide includes the amino acid sequence AKRHHGYKRKFH-SpSp. The peptides can be included in oral care compositions such as toothpastes and mouthwashes. The oral care compositions can be used in methods to treat or prevent diseases or conditions induced by acidophilic oral bacteria. Exemplary methods include reducing or preventing tooth decay or demineralization, biofilm or dental plaque formation, and/or bacterial adhesion to a tooth surface; and promoting mineralization of teeth surfaces.

## Claims

### Claim 1

An isolated peptide comprising an antimicrobial domain and a phosphoserine domain, wherein the antimicrobial domain comprises a histatin 5 segment,
wherein the histatin 5 segment comprises a histatin 5 protein, a variant thereof, a portion thereof, or a variant of a portion thereof,
wherein the phosphoserine domain comprises a phosphorylated serine,
wherein upon contact with a tooth, the isolated peptide binds to the tooth enamel, reduces or prevents tooth decay, reduces or prevents bacterial biofilm formation on the tooth surface, reduces or prevents dental plaque formation, reduces or prevents bacterial adhesion to the tooth surface, induces or increases mineralization, or combinations thereof,
and
(a) wherein the phosphoserine domain comprises two or more phosphorylated serines, or
(b) wherein the phosphoserine domain is at the C-terminus of the isolated peptide.

### Claim 2 (depends on 1)

The peptide of claim 1, wherein the antimicrobial domain comprises AKRHHGYKRKFH (SEQ ID NO:2) or a sequence comprising at least 90% sequence identity to AKRHHGYKRKFH (SEQ ID NO:2).

### Claim 3 (depends on 1)

The peptide of claim 1, wherein the histatin 5 segment comprises the sequence DSHAKRHHGYKRKFHEKHHSHRGY (SEQ ID NO:1) or a sequence comprising at least 90% sequence identity to DSHAKRHHGYKRKFHEKHHSHRGY (SEQ ID NO: 1).

### Claim 4 (depends on 1)

The peptide of claim 1, wherein the phosphoserine domain comprises two or more phosphorylated serines.

### Claim 5 (depends on 1)

The peptide of claim 1, wherein the phosphoserine domain is at the C-terminus of the isolated peptide.

### Claim 6 (depends on 4)

The peptide of claim 4, wherein the peptide comprises the sequence AKRHHGYKRKFH-SpSp (SEQ ID NO:4), wherein each Sp independently represents a phosphorylated serine.

### Claim 7 (depends on 1)

An oral care composition or device comprising the isolated peptide of claim 1.

### Claim 8 (depends on 7)

The oral care composition or device of claim 7 comprising a plurality of copies of the isolated peptide.

### Claim 9 (depends on 8)

The oral care composition or device of claim 8 further comprising a pharmaceutically acceptable excipient, wherein the excipient is suitable for administration to oral cavity.

### Claim 10 (depends on 8)

The oral care composition or device of claim 8, wherein the composition or device is selected from mouthwash, toothpaste, dental cream, oral spray, a rinse, a gargle, a gum, a tablet, an oral lozenge, dental floss, a tooth whitening strip or solution, a cleaning solution, a toothpick, a toothbrush, a varnish, or composite resin.

### Claim 11 (depends on 8)

A method comprising applying the oral care composition or device of claim 8 to teeth and/or oral cavity of a subject.

### Claim 12

A method of reducing, preventing, and/or repairing tooth decay in a subject in need thereof, the method comprising contacting the subject's teeth and/or oral cavity with a peptide comprising the sequence AKRHHGYKRKFH-SpSp (SEQ ID NO:4) or a sequence comprising at least 90% sequence identity to AKRHHGYKRKFH-SpSp (SEQ ID NO:4).

### Claim 13

A method of reducing or preventing enamel demineralization and/or promoting enamel mineralization in a subject in need thereof, the method comprising contacting the subject's teeth and/or oral cavity with a peptide comprising the sequence AKRHHGYKRKFH-SpSp (SEQ ID NO:4) or a sequence comprising at least 90% sequence identity to AKRHHGYKRKFH-SpSp (SEQ ID NO:4).

### Claim 14 (depends on 12)

The method of claim 12, wherein the peptide is comprised in composition or device selected from mouthwash, toothpaste, dental cream, oral spray, a rinse, a gargle, a gum, a tablet, an oral lozenge, dental floss, a tooth whitening strip or solution, a cleaning solution, a toothpick, a toothbrush, a varnish, or composite resin,
wherein the composition or device comprises a plurality of copies of the peptide.

### Claim 15 (depends on 12)

The method of claim 12, wherein the peptide is in an amount effective to reduce or prevent tooth decay, reduce or prevent bacterial biofilm formation, reduce or prevent dental plaque formation, reduce or prevent bacterial adhesion to tooth surfaces, inhibit growth and/or proliferation of oral bacteria, induce or increase enamel mineralization, or combinations thereof.

### Claim 16 (depends on 15)

The method of claim 15, wherein the bacteria is selected from Streptococcus mutans, Streptococcus faecalis, Streptococcus sobrinus, Lactobaccilus acidophilus, Lactobacillus casei, or combinations thereof.