# US 2014/0155317 A1 · Selectively targeted antimicrobial peptides and the use thereof

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- Number: US 2014/0155317 A1
- Document ID: US20140155317A1
- Status: Published application
- Kind: A1
- Application number: 14/178,061
- Filed: 2014-02-11
- Published: 2014-06-05
- Earliest claimed: 2006-09-06
- Assignees: C3 Jian, Inc.; The Regents of the University of California
- Applicants: C3 Jian, Inc.; The Regents of the University of California
- Inventors: Randal H. Eckert; Daniel K. Yarbrough; Wenyuan Shi; Maxwell H. Anderson; Fengxia Qi; Jian He; Ian H. McHardy
- Web page: https://patentgrep.com/patent/US20140155317A1

## CPC

- A61K 38/10: Peptides having 12 to 20 amino acids {(A61K38/043 - A61K38/046 take precedence)}
- A01N 37/18: containing the group —CO—N<, e.g. carboxylic acid amides or imides; Thio analogues thereof
- A01N 37/46: N-acyl derivatives
- A61K 38/1709: {from mammals}
- A61K 47/65: Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
- A61P 31/04: Antibacterial agents
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07K 7/06: having 5 to 11 amino acids
- C07K 7/08: having 12 to 20 amino acids (gastrins C07K14/595; somatostatins C07K14/655; melanotropins C07K14/68)
- C07K 14/001: {by chemical synthesis}
- C07K 14/315: from Streptococcus (G), e.g. Enterococci
- A61K 38/00: Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00)
- C07K 2319/01: containing a localisation/targetting motif
- 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)
- A01N: PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF (preservation of food or foodstuff A23); BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES (preparations for medical, dental or toiletry purposes which kill or prevent the growth or proliferation of unwanted organisms A61K); PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- 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

The present invention relates to targeting peptides capable of specifically binding to microbial organisms (e.g., P. aeruginosa or S. mutans), antimicrobial peptides having antimicrobial activities, and specifically/selectively targeted antimicrobial peptides (STAMPs). In addition, the present invention provides methods of selectively killing or inhibiting microbial organisms by using the peptides or compositions provided by the present invention.

## Claims

### Claim 1

A composition comprising a targeting peptide having an amino acid sequence as shown in SEQ ID NO 2, 5 or 10.

### Claim 2 (depends on 1)

The composition of claim 1 wherein the targeting peptide is linked to one terminus of a linker peptide, wherein the other terminus of the linker peptide is linked to an antimicrobial peptide.

### Claim 3 (depends on 2)

The composition of claim 2 wherein the linker peptide has an amino acid sequence selected from the group consisting of SEQ ID NOs 17, 18, 19, 20, 21, 22, 23 24, 25, 26, 27 and 28.

### Claim 4 (depends on 2)

The composition of claim 2 wherein the antimicrobial peptide is selected from the group consisting of SEQ ID NOs 34-35 and SEQ ID NOs 54-97.

### Claim 5 (depends on 1)

The composition of claim 1 wherein the antimicrobial peptide has an amino acid sequence selected from the group consisting of SEQ ID NOs 3, 7 and 11.

### Claim 6 (depends on 1)

The composition of claim 1 further comprising a detectable agent.

### Claim 7 (depends on 6)

The composition of claim 6 wherein the targeting peptide is conjugated to the detectable agent.

### Claim 8 (depends on 7)

The composition of claim 7 wherein the detectable agent is selected from the group consisting of a radioisotope, a fluorescent agent, and an enzyme-substrate agent.

### Claim 9

A composition comprising an antimicrobial peptide having an amino acid sequence as shown in SEQ ID NO 3, 7, or 11.

### Claim 10 (depends on 9)

The composition of claim 9 wherein the antimicrobial peptide is linked to one terminus of a linker peptide, wherein the other terminus of the linker peptide is linked to a targeting peptide.

### Claim 11 (depends on 10)

The composition of claim 10 wherein the linker peptide has an amino acid sequence selected from the group consisting of SEQ ID NOs 17, 18, 19, 20, 21, 22, 23 24, 25, 26, 27 and 28.

### Claim 12 (depends on 10)

The composition of claim 10 wherein the targeting peptide has an amino acid sequence selected from the group consisting of SEQ ID NOs 2, 5, and 10.

### Claim 13

A STAMP composition comprising
a) a targeting peptide, wherein the targeting peptide having an amino acid sequence selected from the group consisting of SEQ ID NOs 2, 5 and 10;
b) a linker peptide, wherein one terminus of the linker peptide is linked to the targeting peptide; and
c) an antimicrobial peptide, wherein the antimicrobial peptide is linked to the other terminus of the linker peptide.

### Claim 14 (depends on 13)

The STAMP composition of claim 13 wherein the linker peptide has an amino acid sequence selected from the group consisting of SEQ ID NOs 17, 18, 19, 20, 21, 22, 23 24, 25, 26, 27 and 28.

### Claim 15 (depends on 13)

The STAMP composition of claim 13 wherein the antimicrobial peptide is selected from the group consisting of SEQ ID NOs 34-35 and SEQ ID NOs 54-97.

### Claim 16 (depends on 13)

The STAMP composition of claim 13 wherein the antimicrobial peptide has an amino acid sequence selected from the group consisting of SEQ ID NOs 3, 7 and 11.

### Claim 17 (depends on 16)

The STAMP composition of claim 16 wherein the STAMP having an amino acid sequence selected from the group consisting of SEQ ID NOs 4, 6, 8, 9, 12, 13, 14, 15, and 16.

### Claim 18

A STAMP composition comprising:
a) an antimicrobial peptide, wherein the antimicrobial peptide having an amino acid sequence selected from the group consisting of SEQ ID NOs 3, 7, and 11;
b) a linker peptide, wherein one terminus of the linker peptide is linked to the antimicrobial peptide; and
c) a targeting peptide, wherein the targeting peptide is linked to the other terminus of the linker peptide.

### Claim 19 (depends on 18)

The STAMP composition of claim 18 wherein the linker peptide has an amino acid sequence selected from the group consisting of SEQ ID NOs 17, 18, 19, 20, 21, 22, 23 24, 25, 26, 27 and 28.

### Claim 20

A STAMP composition comprising:
a) a targeting peptide, wherein the targeting peptide having an amino acid sequence length of 4-50 amino acids;
b) a linker peptide, wherein one terminus of the linker peptide is linked to the targeting peptide;
c) an antimicrobial peptide, wherein the antimicrobial peptide is linked to the other terminus of the linker peptide; and
d) an antibiotic.
