# US 11,306,119 B2 · Peptide bound to PD-L1 and use thereof

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- Number: US 11,306,119 B2
- Document ID: US11306119B2
- Status: Granted
- Kind: B2
- Application number: 16/772,809
- Filed: 2018-12-17
- Published: 2021-06-03
- Granted: 2022-04-19
- Earliest claimed: 2017-12-15
- Assignees: Kyungpook National University Industry-Academic Cooperation Foundation
- Applicants: Kyungpook National University Industry-Academic Cooperation Foundation
- Inventors: Byung-Heon Lee; Smriti Gurung
- Web page: https://patentgrep.com/patent/US11306119B2

## CPC

- C07K 7/06: having 5 to 11 amino acids
- A61P 35/00: Antineoplastic agents
- C07K 14/70503: {Immunoglobulin superfamily}
- C07K 14/70532: {B7 molecules, e.g. CD80, CD86}
- G01N 33/575: for cancer
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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)
- 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 present invention relates to a peptide bound to PD-L1 and uses for cancer immunotherapy and anticancer using the same, and the peptide of the present invention specifically binds to PD-L1 and inhibits it, thereby activating the function of immune cells against cancer cells and exhibiting anticancer effects. The peptides of the present invention selected two peptides (PD-L1Pep-1 and PD-L1Pep-2) that bind well to cells with high expression of human PD-L1 protein using phage peptide display technology and it was confirmed that it inhibits its function by binding to PD-L1 in humans and mice. The peptide of the present invention showed an effect similar level to that of an antibody and is relatively stable in blood, indicating a high potential as a cancer immunotherapy in the future.

## Claims

### Claim 1

A peptide that specifically binds to PD-L1, consisting of the amino acid sequence of SEQ ID NO: 1 or SEQ ID NO: 2.

### Claim 2 (depends on 1)

A method for diagnosing cancer, comprising:
obtaining a biological sample from the patient;
contacting the biological sample with the peptide of claim 1; and
determining whether or not the peptide is bound to the biological sample.

### Claim 3 (depends on 2)

The method of claim 2, wherein the cancer is PD-L1 overexpressed cancer.

### Claim 4 (depends on 3)

The method of claim 3, wherein the PD-L1 overexpressed cancer is at least one selected from the group consisting of lung cancer, brain tumor, breast cancer, liver cancer, skin cancer, esophageal cancer, testicular cancer, kidney cancer, colorectal cancer, rectal cancer, stomach cancer, kidney cancer, bladder cancer, ovarian cancer, bile duct cancer, gallbladder cancer, uterine cancer, cervical cancer, prostate cancer, head and neck cancer, pancreatic cancer and squamous cell carcinoma.

### Claim 5 (depends on 1)

A method for preventing or treating cancer, comprising a step of administering to a subject in need thereof a pharmaceutical composition comprising the peptide of claim 1 as an active ingredient.

### Claim 6 (depends on 5)

The method of claim 5, wherein the cancer is PD-L1 overexpressed cancer.

### Claim 7 (depends on 6)

The method of claim 6, wherein the PD-L1 overexpressed cancer is at least one selected from the group consisting of lung cancer, brain tumor, breast cancer, liver cancer, skin cancer, esophageal cancer, testicular cancer, kidney cancer, colorectal cancer, rectal cancer, stomach cancer, kidney cancer, bladder cancer, ovarian cancer, bile duct cancer, gallbladder cancer, uterine cancer, cervical cancer, prostate cancer, head and neck cancer, pancreatic cancer and squamous cell carcinoma.

### Claim 8 (depends on 5)

The method of claim 5, wherein the pharmaceutical composition promotes immune cell activation against cancer cells.