# US 10,118,947 B2 · Modulation of structured polypeptide specificity

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- Number: US 10,118,947 B2
- Document ID: US10118947B2
- Status: Granted
- Kind: B2
- Application number: 14/781,294
- Filed: 2014-04-11
- Published: 2016-02-18
- Granted: 2018-11-06
- Earliest claimed: 2013-04-11
- Assignees: BicycleRD Limited
- Applicants: Bicycle Therapeutics Limited
- Inventors: Daniel Paul Teufel; Catherine Stace; Edward Walker; John Tite
- Web page: https://patentgrep.com/patent/US10118947B2

## CPC

- C07K 7/08: having 12 to 20 amino acids (gastrins C07K14/595; somatostatins C07K14/655; melanotropins C07K14/68)
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 11/02: Nasal agents, e.g. decongestants
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/04: Antipruritics
- A61P 27/02: Ophthalmic agents
- A61P 27/16: Otologicals
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 31/00: Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P 35/00: Antineoplastic agents
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- 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 7/50: Cyclic peptides containing at least one abnormal peptide link
- C07K 7/54: with at least one abnormal peptide link in the ring
- C12N 9/6445: {Kallikreins (3.4.21.34; 3.4.21.35)}
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)

## Abstract

The invention describes peptide ligands specific for human plasma Kallikrein.

## Claims

### Claim 1

A peptide ligand specific for human Kallikrein comprising a polypeptide comprising at least three reactive groups, separated by two loop sequences, and a molecular scaffold which forms covalent bonds with the reactive groups of the polypeptide such that two polypeptide loops are formed on the molecular scaffold, wherein the loops of the peptide ligand comprise five amino acids and wherein a first loop comprises the motif GrxWx1Ax2Gr (SEQ ID NO: 3) or GrxFx1Yx2Gr (SEQ ID NO: 6) and a second loop comprises the motif GrA(ψCH2NH)HQ/TXLGr (SEQ ID NO: 212), wherein Gr at the C-terminal of the motif in the first loop is the Gr at the N-terminal of the motif in the second loop, and wherein x is any amino acid, x1 is proline or azetidine carboxylic acid, x2 is arginine, N-methyl arginine, homoarginine, or guanidylphenylalanine, and Gr represents cysteine.

### Claim 2 (depends on 1)

A peptide ligand according to claim 1, wherein in the first loop x1 is azetidine carboxylic acid; and/or in the first loop x2 is N-methyl arginine or homoarginine or guanidylphenylalanine.

### Claim 3 (depends on 2)

A peptide ligand according to claim 2, wherein the polypeptide comprises a first loop which comprises the motif GrxFx1Yx2Gr (SEQ ID NO: 6), wherein x1 is azetidine carboxylic acid and/or x2 is N-methyl arginine or homoarginine or guanidylphenylalanine.

### Claim 4 (depends on 1)

The peptide according to claim 1, which comprises: Cys Ser1 Phe 2 Aze3 Tyr4 HArg5 Cys Ala(ψCH2NH)6 His7 Gln8 Asp9 Leu10 Cys (SEQ ID NO: 201).

### Claim 5 (depends on 1)

The peptide ligand according to claim 1, which comprises:

### Claim 6 (depends on 1)

The peptide ligand according to claim 1, which is attached to an antibody.