# US 8,147,840 B2 · Human immunodeficiency virus (HIV) immunization strategies employing conformationally-stabilized, surface-occluded peptides comprising a gp41 2F5 epitope in association with lipid

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- Number: US 8,147,840 B2
- Document ID: US8147840B2
- Status: Granted
- Kind: B2
- Application number: 11/596,494
- Filed: 2005-05-13
- Published: 2009-09-03
- Granted: 2012-04-03
- Earliest claimed: 2004-05-14
- Assignees: The United States of America, as represented by the Secretary, Department of Health and Human Services
- Inventors: Gilad Ofek; Peter D. Kwong; Richard Wyatt; Min Tang
- Web page: https://patentgrep.com/patent/US8147840B2

## CPC

- C07K 16/1145: {Env proteins, e.g. gp41, gp110/120, gp160, V3, principal neutralising domain [PND] or CD4-binding site}
- C07K 14/005: from viruses
- A61K 2039/505: {comprising antibodies}
- A61K 2039/53: {DNA (RNA) vaccination}
- A61K 2039/555: {characterised by a specific combination antigen/adjuvant}
- A61K 2039/6056: {Antibodies}
- A61K 2039/64: {characterised by the architecture of the carrier-antigen complex, e.g. repetition of carrier-antigen units}
- C07K 2299/00: Coordinates from 3D structures of peptides, e.g. proteins or enzymes
- C12N 2740/16122: New viral proteins or individual genes, new structural or functional aspects of known viral proteins or genes
- 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)
- 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)
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)

## Abstract

This invention relates to novel peptide immunogens that generate an immune response in mammals against HIV gp41, to pharmaceutical compositions that comprise such immunogens, and to methods of treating Immunodeficiency disease, especially HIV infection and AIDS, that employ such pharmaceutical compositions.

## Claims

### Claim 1

An isolated peptide that comprises at least ten contiguous amino acids of the sequence EKNEQELLELDKWASLW (SEQ ID NO: 1) and that binds to monoclonal antibody 2F5, wherein (i) the isolated peptide is conformationally stabilized to provide a three dimensional structure that corresponds to that of SEQ ID NO: 1 when complexed with the 2F5 antibody, (ii) the isolated peptide comprises a face that does not bind to the 2F5 antibody, and (iii) the isolated peptide is associated with a lipid.

### Claim 2 (depends on 1)

An isolated peptide of claim 1, wherein the face that does not bind to the 2F5 antibody is occluded with appended groups.

### Claim 3 (depends on 2)

An isolated peptide of claim 2, wherein the appended groups are carbohydrate moieties.

### Claim 4 (depends on 1)

An isolated peptide of claim 1, wherein the peptide is conformationally stabilized with a linkage selected from the group consisting of a disulfide bond and a lactam bridge.

### Claim 5 (depends on 1)

The isolated peptide of claim 1, wherein lipid is a phospholipid not normally found on the outer cytoplasmic membrane of human cells.

### Claim 6 (depends on 1)

The isolated peptide of claim 1, wherein the lipid is in the form of a proteoliposome.

### Claim 7

A method of generating a humoral immune response against a human immunodeficiency virus type 1 (HIV-1) gp41 envelope glycoprotein in a mammal, which method comprises (a) preparing a composition comprising the isolated peptide of claim and a pharmaceutically acceptable carrier, and (b) administering the composition to a mammal, whereupon a humoral immune response is generated against the HIV-1 gp41 envelope glycoprotein in the mammal.