# US 11,078,243 B2 · Cystine knot scaffold platform

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- Number: US 11,078,243 B2
- Document ID: US11078243B2
- Status: Granted
- Kind: B2
- Application number: 16/574,910
- Filed: 2019-09-18
- Published: 2020-05-07
- Granted: 2021-08-03
- Earliest claimed: 2015-09-15
- Assignees: Genentech, Inc.
- Applicants: Genentech, Inc.
- Inventors: Rami Hannoush; Harini Kaluarachchi; Aaron Nile; Cameron Noland; Yingnan Zhang; Lijuan Zhou; Xinxin Gao
- Web page: https://patentgrep.com/patent/US11078243B2

## CPC

- C07K 14/415: from plants
- A61K 9/0051: {Ocular inserts or implants}
- A61K 9/5031: {obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poly(lactide-co-glycolide)}
- 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)
- A61K 38/168: {from plants}
- A61K 47/34: Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers (A61K47/10 takes precedence)
- A61P 27/02: Ophthalmic agents
- C07K 14/001: {by chemical synthesis}
- C07K 14/4702: {Regulators; Modulating activity}
- C07K 14/811: {Serine protease (E.C. 3.4.21) inhibitors}
- C07K 2319/70: containing domain for protein-protein interaction
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

Provided are non-naturally occurring cystine knot peptides (CKPs) that bind to VEGF-A. Additionally, provided are methods of using non-naturally occurring CKPs that bind to VEGF-A, including diagnostic and therapeutic compositions and methods. Non-naturally CKPs that bind low density lipoprotein receptor-related protein 6 (LRP6) are also provided.

## Claims

### Claim 1

A peptide that comprises the amino acid sequence of any one of SEQ ID NOs: 102-112, 216-219, 221-223, 361-362, 365, 369-384, 405-413, 415, 417, 419-426, 428, 430-432, 436-446, 538-548, 555-566, and 568.

### Claim 2 (depends on 1)

The peptide of claim 1, wherein:
(a) the C-terminal carboxyl group of the peptide is capped;
(b) the N-terminal amine of the peptide is capped; or
(c) the C-terminal carboxyl group and the N-terminal amine of the peptide is capped.

### Claim 3 (depends on 1)

The peptide of claim 1 conjugated to a therapeutic agent.

### Claim 4 (depends on 1)

The peptide of claim 1 conjugated to a label.

### Claim 5 (depends on 1)

A composition comprising the peptide of claim 1 and a pharmaceutically acceptable carrier.

### Claim 6 (depends on 1)

The peptide of claim 1, wherein the peptide is formulated for long acting delivery.

### Claim 7 (depends on 1)

The peptide of claim 1, wherein the peptide binds to vascular endothelial growth factor A (VEGF-A).

### Claim 8 (depends on 1)

An isolated nucleic acid encoding the peptide of claim 1.

### Claim 9 (depends on 8)

An expression vector encoding the nucleic acid molecule of claim 8.

### Claim 10 (depends on 9)

A cell comprising the expression vector of claim 9.

### Claim 11 (depends on 10)

A method of producing a peptide comprising culturing the cell of claim 10 under conditions where the peptide is expressed, and recovering the peptide expressed by the cell.

### Claim 12 (depends on 1)

A method of producing the peptide of claim 1, comprising chemically synthesizing the peptide.