TARGETED NONINVASIVE IMAGING PROBES OF EGFR EXPRESSING CELLS

• US 20190315805A1
• Filed: 04/26/2019
• Published: 10/17/2019
• Est. Priority Date: 11/08/2011
• Status: Abandoned Application

• Current Assignee: Case Western Reserve University
• Original Assignee: Case Western Reserve University
• Inventors: Basilion, James P., Agnes, Richard
• Application Number:
  US16/396,265
• Publication Number:
  US 20190315805A1
• Time in Patent Office: Days
• CPC Class Codes: C07K 7/08 having 12 to 20 amino acids gastrins C07K14/595; somatostatins C07K14/655; melanotropins C07K14/68
• CPC Class Codes: C07K 7/56 the cyclisation not occurring through 2,4-diamino-butanoic acid

Abstract

A probe for imaging EGFR expressing cells includes an EGFR targeting moiety, a reporter moiety, and a hydrophilic linker that links the EGFR targeting moiety to the reporter moiety. The hydrophilic linker enhances solubility of the probe in an aqueous media as well as binding affinity of the probe to EGFR expressing cells.

Claims

1. A probe for imaging EGFR expressing cells, comprising:

an EGFR targeting moiety,

a reporter moiety, and

a hydrophilic linker that links the EGFR targeting moiety to the reporter moiety, the hydrophilic linker enhancing solubility of the probe in an aqueous media as well as binding affinity of the probe to EGFR expressing cells.

2. The probe of claim 1, EGFR targeting moiety comprising a peptide having SEQ ID NO:

1 or SEQ ID NO;

2.

3. The probe of claim 1, the reporter moiety comprising a fluorochrome.

4. The probe of claim 1, the linker comprising a polyethylene glycol linker.

5. The probe of claim 1, upon systemic administration to subject being capable of crossing the blood brain barrier.

6. The probe of claim 1, the EGFR expressing cells comprising EGFR expressing cancer cells.

7. The probe of claim 1, comprising the following formula:

8. A probe for imaging EGFR expressing cells, comprising:

a hydrophobic EGFR targeting moiety,

a reporter moiety, and

a hydrophilic linker that links the hydrophobic EGFR targeting moiety to the reporter moiety, the hydrophilic linker enhancing solubility of the probe in an aqueous media as well as binding affinity of the probe to EGFR expressing cells.

9. The probe of claim 8, EGFR targeting moiety comprising a peptide having SEQ ID NO:

1 or SEQ ID NO;

2.

10. The probe of claim 9, the reporter moiety comprising a fluorochrome.

11. The probe of claim 9, the linker comprising a polyethylene glycol linker.

12. The probe of claim 9, upon systemic administration to subject being capable of crossing the blood brain barrier.

13. The probe of claim 9, the EGFR expressing cells comprising EGFR expressing cancer cells.

14. The probe of claim 8, comprising the following formula:

15. A probe for imaging EGFR expressing cells, comprising:

a hydrophobic EGFR targeting moiety that includes a peptide having SEQ ID NO;

1 or SEQ ID NO;

2,

a fluorochrome reporter moiety, and

a hydrophilic linker that links the hydrophobic EGFR targeting moiety to the reporter moiety, the hydrophilic linker enhancing solubility of the probe in an aqueous media as well as binding affinity of the probe to EGFR expressing cells.

16. The probe of claim 15, the linker comprising a polyethylene glycol linker.

17. The probe of claim 15, upon systemic administration to subject being capable of crossing the blood brain barrier.

18. The probe of claim 15, the EGFR expressing cells comprising EGFR expressing cancer cells.

19. The probe of claim 15, comprising the following formula:

20. The probe of claim 15, selected from the group consisting of: