# US 9,751,920 B2 · Muteins with tear lipocalin having affinity to human c-met receptor tyrosine kinase and methods for obtaining the same

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- Number: US 9,751,920 B2
- Document ID: US9751920B2
- Status: Granted
- Kind: B2
- Application number: 14/968,603
- Filed: 2015-12-14
- Published: 2016-07-14
- Granted: 2017-09-05
- Earliest claimed: 2008-01-30
- Assignees: Pieris Pharmaceuticals GmbH
- Applicants: Pieris Pharmaceuticals GmbH
- Inventors: Gabriele Matschiner; Andreas Hohlbaum; Martin Huelsmeyer; Stefan Trentmann
- Web page: https://patentgrep.com/patent/US9751920B2

## CPC

- C07K 14/47: from mammals
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- A61P 13/12: of the kidneys
- A61P 35/00: Antineoplastic agents
- A61P 35/04: specific for metastasis
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- G01N 33/573: for enzymes or isoenzymes
- 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)
- G01N 2333/47: Assays involving proteins of known structure or function as defined in the subgroups
- G01N 2333/91205: Phosphotransferases in general
- 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 novel muteins derived from human tear lipocalin having affinity to human c-Met receptor tyrosin kinase (c-Met). The invention also refers to a corresponding nucleic acid molecule encoding such a mutein and to a method for its generation. The invention further refers to a method for producing such a mutein. Finally, the invention is directed to a pharmaceutical composition comprising such a lipocalin mutein as well as to various uses of the mutein.

## Claims

### Claim 1

A nucleic acid molecule comprising a nucleotide sequence encoding a mutein of human tear lipocalin (hTLc) having detectable binding affinity to human Met receptor tyrosine kinase (c-Met) or a domain or fragment thereof and wherein said mutein comprises at least 8 amino acid substitutions with respect to the amino acid sequence of mature human tear lipocalin (SEQ ID NO:36), which are selected from the group consisting of Arg 26→Thr, Val, Pro, Ser, or Gly; Glu 27→Gln, Gly, Val, or Ser; Phe 28→Met, or Asp; Pro 29→Leu, Ile, Ala, or Trp; Glu 30→Leu, Gly, Arg, or Phe; Met 31→Ser; Asn 32→Leu, Arg, Val, or Gln; Leu 33→Tyr, Val, Ile, Thr, or Phe; Glu 34→Val, Arg, or Ala; Leu 56→Asn; Ile 57→Gln; Ser 58→Ile, or Val; Asp 80→Tyr; Lys 83→Ala; Glu 104→Asp; Leu 105→Thr; His 106→Trp; and Lys 108→Gly.

### Claim 2 (depends on 1)

A host cell comprising a nucleic acid molecule of claim 1.