# US 12,600,785 B2 · Method of screening for compounds that inhibit proliferation of pancreatic cancer cells having a loss-of-function mutation in the RNF43 gene

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- Number: US 12,600,785 B2
- Document ID: US12600785B2
- Status: Granted
- Kind: B2
- Application number: 17/176,155
- Filed: 2021-02-15
- Published: 2021-08-19
- Granted: 2026-04-14
- Earliest claimed: 2016-01-29
- Assignees: Antlera Therapeutics Inc.
- Applicants: Antlera Therapeutics Inc.
- Inventors: Guohua Pan; Jason Moffat; Sachdev Sidhu; Stephane Angers; Zachary Steinhart; Xiaowei Wang
- Web page: https://patentgrep.com/patent/US12600785B2

## CPC

- C07K 16/2863: {against receptors for growth factors, growth regulators}
- A61K 47/6849: {the antibody targeting a receptor, a cell surface antigen or a cell surface determinant}
- A61K 47/6851: {the antibody targeting a determinant of a tumour cell}
- A61P 35/00: Antineoplastic agents
- G01N 33/575: for cancer
- A61K 2039/505: {comprising antibodies}
- C07K 2317/21: from primates, e.g. man
- C07K 2317/52: Constant or Fc region; Isotype
- C07K 2317/55: Fab or Fab'
- C07K 2317/56: variable (Fv) region, i.e. VH and/or VL
- C07K 2317/565: Complementarity determining region [CDR]
- C07K 2317/567: Framework region [FR]
- C07K 2317/73: Inducing cell death, e.g. apoptosis, necrosis or inhibition of cell proliferation
- C07K 2317/76: Antagonist effect on antigen, e.g. neutralization or inhibition of binding
- C07K 2317/92: Affinity (KD), association rate (Ka), dissociation rate (Kd) or EC50 value
- G01N 2333/726: G protein coupled receptor, e.g. TSHR-thyrotropin-receptor, LH/hCG receptor, FSH
- G01N 2800/7028: Cancer
- 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
- 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 present disclosure is directed to novel FZD5-binding agents and methods and uses thereof for treating a disease or disorder associated with aberrant expression of activity of Frizzled protein.

## Claims

### Claim 1

A method of screening for compounds that inhibit proliferation of pancreatic cancer cells having a loss-of-function mutation in the RNF43 gene by inhibition of the binding between FZD5 and Wnt7B, the method comprising:
measuring binding between FZD5 and Wnt7B in said pancreatic cancer cells;
exposing FZD5 and Wnt7B to a test agent; and
determining if the test agent inhibits binding between FZD5 and Wnt7B,
wherein inhibition of said binding identifies the test agent as a compound that inhibits proliferation of said pancreatic cancer cells.

### Claim 2 (depends on 1)

The method of claim 1 further comprising that the test agent inhibits binding between FZD5 and Wnt7B by at least 5%.

### Claim 3 (depends on 1)

The method of claim 1 further comprising that the test agent inhibits
binding between FZD5 and Wnt7B by at least 10%.

### Claim 4 (depends on 1)

The method of claim 1 further comprising that the test agent inhibits binding between FZD5 and Wnt7B by at least 25%.

### Claim 5 (depends on 1)

The method of claim 1 further comprising that the test agent inhibits binding between FZD5 and Wnt7B by at least 75%.