# US 2020/0399630 A1 · Peptide libraries

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- Number: US 2020/0399630 A1
- Document ID: US20200399630A1
- Status: Published application
- Kind: A1
- Application number: 17/014,084
- Filed: 2020-09-08
- Published: 2020-12-24
- Earliest claimed: 2014-05-02
- Assignees: Morphosys AG
- Applicants: MorphoSys AG
- Inventors: Katja Siegers; Jan Van Den Brulle
- Web page: https://patentgrep.com/patent/US20200399630A1

## CPC

- C12N 15/1037: {Screening libraries presented on the surface of microorganisms, e.g. phage display, E. coli display}
- C07K 1/047: {Simultaneous synthesis of different peptide species; Peptide libraries}
- G01N 33/6845: {Methods of identifying protein-protein interactions in protein mixtures}
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)
- 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)
- G01N: INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES (measuring or testing apparatus or processes other than immunoassay, involving enzymes or microorganisms C12M, C12Q)

## Abstract

The invention relates to novel libraries of linear and cyclic peptides, and methods of generating and screening such libraries for biological, pharmaceutical and other uses.

## Claims

### Claim 1

A library of synthetic peptides, comprising linear and cyclic peptides,
wherein the cyclic peptides have different loop lengths, and
wherein some of the cyclic peptides have single loops and other cyclic peptides have two or more loops, and
wherein the synthetic peptides of said library comprise a controlled ratio of cysteines at certain positions,
wherein the cyclic peptides are formed by one or more covalent bonds,
wherein said covalent bond is a disulfide bond formed by two cysteine residues,
wherein each member of the library comprises an amino acid sequence
Cmix-(X)m-(Amix)n,
wherein
a) Cmix is a mixture of 50% cysteine and an equal mixture of the remaining natural occurring amino acids,
b) X are each an equal mixture of the natural occurring amino acids, excluding cysteine,
c) Amix are each a mixture of 5-50% cysteine and an equal mixture of the remaining natural occurring amino acids, and
d) m and n are both, and independently from each other, 3-20.

### Claim 2 (depends on 1)

The library of claim 1, wherein the loop lengths range from 3-17 amino acids in length.

### Claim 3 (depends on 1)

The library of claim 1, wherein the synthetic peptides of said library are translated from nucleic acids.

### Claim 4 (depends on 1)

The library of claim 1, wherein the synthetic peptides of said library are displayed on bacteriophage.

### Claim 5 (depends on 1)

The library of claim 1, wherein each member of the library comprises an amino acid sequence Cmix-(X)m-(Amix)n, wherein
a) Amix are each a mixture of 10-20% cysteine and an equal mixture of the remaining natural occurring amino acids,
b) m is 5-6, and
c) n is 3-20.

### Claim 6 (depends on 5)

The library of claim 5, wherein each member of the library comprises an amino acid sequence (X)l-Cmix-(X)m-(Amix)n, wherein
a) l is 1-3.

### Claim 7 (depends on 6)

The library of claim 6, wherein each member of the library comprises an amino acid sequence (X)l-Cmix-(X)m-(Amix)n, wherein
a) Amix are each a mixture of 15% cysteine and an equal mixture of the remaining natural occurring amino acids,
b) l is 3,
c) m is 6, and
d) n is 10.

### Claim 8 (depends on 1)

A library of nucleic acids encoding the library of peptides of claim 1.

### Claim 9 (depends on 8)

A vector comprising the nucleic acids of claim 8.

### Claim 10 (depends on 9)

The vector of claim 9, wherein said vector is a display vector or an expression vector.

### Claim 11 (depends on 1)

A method of identifying a peptide specific for an antigen, comprising
(a) contacting an antigen with a library of claim 1, and
(b) selecting one or more peptides specific for said antigen.