# US 10,501,507 B2 · Griffithsin mutants

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- Number: US 10,501,507 B2
- Document ID: US10501507B2
- Status: Granted
- Kind: B2
- Application number: 15/550,323
- Filed: 2016-02-10
- Published: 2018-01-18
- Granted: 2019-12-10
- Earliest claimed: 2015-02-10
- Assignees: The United States of America, as represented by the Secretary, Department of Health and Human Services; University of Louisville Research Foundation, Inc.; University of Pittsburgh—Of the Commonwealth System of Higher Education
- Applicants: The United States of America, as represented by the Secretary, Department of Health and Human Services; University of Louisville Research Foundation, Inc.; University of Pittsburgh-Of the Commonwealth System of Higher Education
- Inventors: Barry R. O'Keefe; Tinoush Moulaei; Kenneth E. Palmer; Lisa C. Rohan; Joshua L. Fuqua; Lindsay F. Kramzer
- Web page: https://patentgrep.com/patent/US10501507B2

## CPC

- C07K 14/405: from algae
- A61K 38/16: Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof {(enzyme inhibitors A61K38/005)}
- 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)
- 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

The invention provides modified griffithsin polypeptides comprising the amino acid sequence of SEQ ID NO: 1, as well as corresponding nucleic acids, vectors, cells, fusion proteins, constructs, conjugates, and methods of inhibiting viral infection.

## Claims

### Claim 1

A polypeptide comprising the amino acid sequence of SLTHRKFGGSGGSPFSGLSSIAVRSGSYLDAIIIDGVHHGGSGGNLSPTFTFGSGEYISN X1TIRSGDYIDNISFX2TNX3GRRFGPYGGSGGSANTLSNVKVIQINGX4X5GDYLDSLD X6YYX7QY (SEQ ID NO: 1), wherein X1 can be M or V, X2 is Q, X3 can be M, A, K, V, F, L, I, Q, R, or G, X4 can be S or R, X5 can be A or S, X6 can be I or F, and X7 can be E or Q provided that the polypeptide does not comprise the amino acid sequence of SEQ ID NO: 2.

### Claim 2 (depends on 1)

The polypeptide of claim 1, wherein X3 is Q.

### Claim 3 (depends on 1)

The polypeptide of claim 1, wherein the polypeptide forms a dimer.

### Claim 4 (depends on 1)

A conjugate comprising the polypeptide of claim 1, and at least one effector component.

### Claim 5 (depends on 4)

The conjugate of claim 4, wherein the at least one effector component, which can be same or different, is selected from the group consisting of polyethylene glycol, albumin, dextran, a toxin, an immunological reagent, a virus, a viral envelope glycoprotein, an antiviral agent, and a solid support matrix.

### Claim 6 (depends on 1)

A nucleic acid molecule encoding the polypeptide of claim 1.

### Claim 7 (depends on 6)

The nucleic acid molecule of claim 6, wherein the nucleic acid molecule comprises the nucleotide sequence of SEQ ID NO: 4, 6, 8, or 10.

### Claim 8 (depends on 6)

A vector comprising the nucleic acid molecule of claim 6.

### Claim 9 (depends on 6)

A cell comprising the nucleic acid molecule of claim 6.

### Claim 10 (depends on 1)

A composition comprising the polypeptide of claim 1, and a carrier.

### Claim 11 (depends on 1)

A method of prophylactically or therapeutically inhibiting an viral infection in a cell or host comprising administering to the cell or host the polypeptide of claim 1, such that the viral infection is inhibited.

### Claim 12 (depends on 11)

The method of claim 11, wherein the viral infection is an HIV infection.

### Claim 13 (depends on 1)

A method of inhibiting a virus in a biological sample or in/on an inanimate object comprising contacting the biological sample or the inanimate object with a viral-inhibiting amount of the polypeptide of claim 1, which method optionally further comprises the prior, simultaneous, or subsequent contacting of the biological sample or inanimate object with an antiviral agent or another agent that is efficacious in inhibiting the virus, whereupon the virus is inhibited.

### Claim 14 (depends on 1)

The polypeptide of claim 1, wherein X3 is A, K, L, or Q.

### Claim 15 (depends on 1)

The polypeptide of claim 1, wherein the polypeptide is a mutant griffithsin polypeptide.

### Claim 16

A polypeptide consisting of the amino acid sequence of SEQ ID NO: 1.
