# US 5,708,145 A · Immunglobulins reactive with protegrins

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- Number: US 5,708,145 A
- Document ID: US5708145A
- Status: Granted
- Kind: A
- Application number: 08/243,879
- Filed: 1994-05-17
- Granted: 1998-01-13
- Earliest claimed: 1993-07-20
- Assignees: University of California
- Inventors: Robert I. Lehrer; Sylvia S.L. Harwig
- Web page: https://patentgrep.com/patent/US5708145A

## CPC

- C07K 7/08: having 12 to 20 amino acids (gastrins C07K14/595; somatostatins C07K14/655; melanotropins C07K14/68)
- A01N 63/50: Isolated enzymes; Isolated proteins (peptides A01N37/46)
- A61P 31/00: Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P 31/04: Antibacterial agents
- A61P 31/12: Antivirals
- A61P 37/04: Immunostimulants
- C07K 16/18: against material from animals or humans
- 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: 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)
- 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
- 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)

## Abstract

Peptide-based compounds containing four invariant cysteine residues which have been optionally oxidized to contain two intramolecular disulfide bonds, or modified forms where the cysteines are replaced are useful as preservatives and in preventing, treating, or ameliorating viral or microbial infection in animals and plants, and in inactivating endotoxin. These compounds, in one embodiment, are of the formula: A.sub.1 -A.sub.2 -A.sub.3 -A.sub.4 -A.sub.5 -C-A.sub.7 -C-A.sub.9 -A.sub.10 -A.sub.11 -A.sub.12 -C-A.sub.14 -C-A.sub.16 -(A.sub.17 -A.sub.18)(1) and the N-terminal acylated and/or C-terminal amidated or esterified forms thereof, either in optionally --SH stabilized linear or in cystine-bridged form wherein A.sub.1 and A.sub.9 are basic amino acids; A.sub.2, A.sub.3 and A.sub.10 are small amino acids; A.sub.5, A.sub.7, A.sub.12, A.sub.14 and A.sub.16 are hydrophobic amino acids; and A.sub.4 is a basic or a small amino acid; A.sub.11 is a hydrophobic amino acid; A.sub.17 is not present or, if present, is a small amino acid; A.sub.18 is not present or, if present, is a basic amino acid, and modified form of formula (1) wherein each of 1-4 cysteines is independently replaced by a hydrophobic amino acid or a small amino acid.

## Claims

### Claim 1

Antibodies specifically reactive with a compound of the formula (1)
A.sub.1 -A.sub.2 -A.sub.3 -A.sub.4 -A.sub.5 -C-A.sub.7 -C-A.sub.9 -A.sub.10 -A.sub.11 -A.sub.12 -C-A.sub.14 -C-A.sub.16 -(A.sub.17 -A.sub.18)(1)
and the N-terminal acylated and/or C-terminal amidated or esterified forms thereof, which is either in the optionally --SH stabilized linear or in the cystine-bridged form
wherein A.sub.1 and A.sub.9 are basic amino acids;
A.sub.2, A.sub.3 and A.sub.10 are small amino acids;
A.sub.5, A.sub.7, A.sub.12, A.sub.14 and A.sub.16 are hydrophobic amino acids; and
A.sub.4 is a basic or a small amino acid;
A.sub.11 is a hydrophobic amino acid;
A.sub.17 is not present or, if present, is a small amino acid;
A.sub.18 is not present or, if present, is a basic amino acid, or a modified form of formula (1) and the N-terminal acylated and/or C-terminal amidated or esterified forms thereof wherein each of 1-4 cysteines is independently replaced by a hydrophobic amino acid or a small amino acid.

### Claim 2 (depends on 1)

The antibodies of claim 1 which are monoclonal antibodies.

### Claim 3 (depends on 1)

The antibodies of claim 1 wherein the compound of formula (1) contains two cystine bridges.

### Claim 4 (depends on 1)

The antibodies of claim 1 wherein the compound of formula (1) is in the linear form.

### Claim 5 (depends on 1)

The antibodies of claim 1 wherein the compound of formula (1) is in the modified form.

### Claim 6 (depends on 1)

The antibodies of claim 1 wherein the compound of formula (1) is selected from the group consisting of PG-1, PG-2, PG-3 and PG-4.
