# US 7,745,109 B2 · Regulation of cell growth by MUC1

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- Number: US 7,745,109 B2
- Document ID: US7745109B2
- Status: Granted
- Kind: B2
- Application number: 10/733,212
- Filed: 2003-12-11
- Published: 2004-08-26
- Granted: 2010-06-29
- Earliest claimed: 2003-12-11
- Assignees: Dana-Farber Cancer Insitute
- Inventors: Donald W. Kufe
- Web page: https://patentgrep.com/patent/US7745109B2

## CPC

- G01N 33/5758: {involving compounds serving as markers for tumours, cancers or neoplasias, e.g. cellular determinants, receptors, heat shock/stress proteins, A-protein, oligosaccharides or metabolites}
- A61P 35/00: Antineoplastic agents
- A61P 35/02: specific for leukemia
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07K 14/4727: {Mucins, e.g. human intestinal mucin}
- C12Q 1/485: {involving kinase}
- G01N 33/5011: {for testing antineoplastic activity}
- 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 2333/4725: Mucins, e.g. human intestinal mucin
- G01N 2500/10: involving cells
- G01N 2500/20: cell-free systems
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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)
- C12Q: MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS (immunoassay G01N33/53); COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
- 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 invention features a method of identifying a compound that inhibits (a) the physical interaction (binding) between MUC1 and tumor progressors (e.g., β-catenin, c-Src, EGF-R, p120ctn, or PKCδ) and/or (b) phosphorylation of MUC1 by tumor progressors with kinase activity (e.g., c-Src, EGF-R, or PKCδ). The invention also includes a method of inhibiting an interaction between MUC1 and β-catenin and a method of inhibiting expression of MUC1 or a tumor progressor in a cell.

## Claims

### Claim 1

A method of identifying a compound that inhibits binding of MUC1 to a tumor progressor, the method comprising:
(a) providing a MUC1 test agent, wherein the MUC1 test agent comprises a phosphorylated YEKV site;
(b) providing a tumor progressor test agent that has increased binding to the phosphorylated MUC1 test agent as compared to a MUC1 test agent that does not comprise a phosphorylated YEKV site;
(c) contacting the phosphorylated MUC1 test agent with the tumor progressor test agent in the presence of a test compound; and
(d) determining whether the test compound inhibits binding of the phosphorylated MUC1 test agent to the tumor progressor test agent.

### Claim 2 (depends on 1)

The method of claim 1, wherein the tumor progressor test agent is a c-Src test agent.

### Claim 3 (depends on 1)

The method of claim 1, wherein the tumor progressor test agent is a p120ctn test agent.

### Claim 4 (depends on 1)

The method of claim 1, wherein the tumor progressor test agent is an epidermal growth factor receptor (EGF-R) test agent.

### Claim 5 (depends on 1)

The method of claim 1, wherein the tumor progressor test agent is a β-catenin test agent.

### Claim 6 (depends on 5)

The method of claim 5, wherein the MUC1 test agent comprises SEQ ID NO:1 phosphorylated at Y46.

### Claim 7 (depends on 5)

The method of claim 5, wherein providing a phosphorylated MUC 1 test agent comprises combining a MUC1 test agent, a tumor progressor test agent with kinase activity, and ATP, wherein a MUC1 test agent phosphorylated at a YEKV site is formed.

### Claim 8 (depends on 7)

The method of claim 7, wherein the tumor progressor test agent with kinase activity is c-src, EGF-R, or PKCδ.

### Claim 9 (depends on 1)

The method of claim 1, wherein the tumor progressor test agent is a protein kinase Cδ (PKCδ) test agent.

### Claim 10 (depends on 1)

The method of claim 1, wherein the contacting is carried out in a cell-free system.

### Claim 11 (depends on 1)

The method of claim 1, wherein the contacting occurs in a cell.

### Claim 12 (depends on 11)

The method of claim 11, wherein the cell is a cancer cell.

### Claim 13 (depends on 12)

The method of claim 12, wherein the cancer cell expresses MUC1.

### Claim 14 (depends on 12)

The method of claim 12, wherein the cancer cell is a breast cancer cell, a lung cancer cell, a colon cancer cell, a pancreatic cancer cell, a renal cancer cell, a stomach cancer cell, a liver cancer cell, a bone cancer cell, a hematological cancer cell, a neural tissue cancer cell, a melanoma cell, an ovarian cancer cell, a testicular cancer cell, a prostate cancer cell, a cervical cancer cell, a vaginal cancer cell, or a bladder cancer cell.

### Claim 15 (depends on 1)

The method of claim 1, wherein the test compound is a peptide fragment of the tumor progressor.

### Claim 16 (depends on 15)

The method of claim 15, wherein the tumor progressor test agent is a c-Src test agent.

### Claim 17 (depends on 15)

The method of claim 15, wherein the tumor progressor test agent is a p120ctn test agent.

### Claim 18 (depends on 15)

The method of claim 15, wherein the tumor progressor test agent is an epidermal growth factor receptor (EGF-R) test agent.

### Claim 19 (depends on 15)

The method of claim 15, wherein the tumor progressor test agent is a β-catenin test agent.

### Claim 20 (depends on 15)

The method of claim 15, wherein the tumor progressor test agent is a protein kinase Cδ (PKCδ) test agent.

### Claim 21 (depends on 15)

The method of claim 15, wherein the contacting is carried out in a cell-free system.

### Claim 22 (depends on 15)

The method of claim 15, wherein the contacting occurs in a cell.

### Claim 23 (depends on 1)

The method of claim 1, wherein the MUC1 test agent comprises SEQ ID NO:1.