# US 7,745,412 B2 · Isozyme-specific antagonists of protein kinase C

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- Number: US 7,745,412 B2
- Document ID: US7745412B2
- Status: Granted
- Kind: B2
- Application number: 12/283,921
- Filed: 2008-09-15
- Published: 2009-06-04
- Granted: 2010-06-29
- Earliest claimed: 2003-12-11
- Assignees: The Board of Trustees of the Leland Stanford Junior University
- Inventors: Daria Mochly-Rosen
- Web page: https://patentgrep.com/patent/US7745412B2

## CPC

- C12N 9/1205: {Phosphotransferases with an alcohol group as acceptor (2.7.1), e.g. protein kinases}
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- 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 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 5/16: for decreasing, blocking or antagonising the activity of the thyroid hormones
- A61P 7/02: Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 11/06: Antiasthmatics
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/06: Antipsoriatics
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 31/04: Antibacterial agents
- A61P 37/00: Drugs for immunological or allergic disorders
- A61P 37/02: Immunomodulators
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

A method of changing or otherwise converting the biological activity of a PKC peptide agonist to a peptide antagonist is described. The method involves substituting one or more amino acid residues so as to effect a change in charge in the peptide and/or to otherwise make the sequence similar to a sequence derived from the PKC binding site on the RACK protein for the respective PKC enzyme. Methods of inhibiting the activity of a PKC enzyme, and various peptide antagonists of εPKC are also disclosed.

## Claims

### Claim 1

A composition comprising a peptide consisting of an amino acid sequence selected from the group consisting of SEQ ID NO:50; SEQ ID NO:51; SEQ ID NO:52; SEQ ID NO:53; SEQ ID NO:54; SEQ ID NO:55; SEQ ID NO:56; and SEQ ID NO:57, crosslinked via an N-terminal Cys-Cys bond to a peptide to facilitate transport cellular uptake.

### Claim 2 (depends on 1)

The composition of claim 1, wherein the peptide to facilitate transport cellular uptake is selected from the group consisting of a Tat-derived peptide, an Antennapedia homeodomain-derived sequence, and a polyarginine peptide.

### Claim 3 (depends on 2)

The composition of claim 2, wherein the peptide to facilitate transport cellular uptake is selected from the group consisting of SEQ ID NO:91 and SEQ ID NO:92.

### Claim 4

A composition comprising a peptide consisting of SEQ ID NO: 55, crosslinked via an N-terminal Cys-Cys bond to a Tat-derived peptide or to a polyarginine peptide.

### Claim 5 (depends on 4)

The composition of claim 4, wherein said Tat-derived peptide has a sequence identified as SEQ ID NO:92.