# US 7,745,388 B2 · Peptides for activation and inhibition of δPKC > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 7,745,388 B2 - Document ID: US7745388B2 - Status: Granted - Kind: B2 - Application number: 10/843,731 - Filed: 2004-05-12 - Published: 2004-10-14 - Granted: 2010-06-29 - Earliest claimed: 2001-01-18 - Assignees: National Institute of Health (NIH); The United States of America as represented by the Department of Health and Human Services; The United States of America as represented by NIH Division of Extramural Inventions and Technology Resources (DEITR) - Inventors: Daria Mochly-Rosen; Leon E. Chen - Web page: https://patentgrep.com/patent/US7745388B2 ## CPC - C12N 9/12: transferring phosphorus containing groups, e.g. kinases (2.7) - A61P 9/00: Drugs for disorders of the cardiovascular system - A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis - A61P 13/12: of the kidneys - A61P 25/00: Drugs for disorders of the nervous system - A61P 27/02: Ophthalmic agents - 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 - C07K 5/101: {the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu} - 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) - 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 - 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) ## Abstract Peptides able to inhibit or activate the translocation or function of δPKC are identified. Administration of the peptides for protection or enhancement of cell damage due to ischemia is described. Therapeutic methods to reduce damage to cells or to enhance damage to cells due to ischemia are also described, as well as methods for screening test compounds for δPKC-selective agonists and antagonists. ## Claims ### Claim 1 A method for reducing cardiac tissue damage in a subject due to ischemia, comprising: administering to said subject a conjugate comprising (a) a peptide comprising the amino acid sequence of SEQ ID NO: 4, and (b) a transport moiety effective to facilitate transport across a cell membrane, wherein said peptide and transport moiety are linked, and wherein said administering is effective to reduce cardiac tissue damage due to ischemia. ### Claim 2 (depends on 1) The method of claim 1, wherein the peptide consists of the amino acid sequence of SEQ ID NO:4. ### Claim 3 A method for reducing cardiac tissue damage in a subject due to ischemia, comprising: administering to said subject a conjugate comprising (a) a first peptide comprising the amino acid sequence of SEQ ID NO: 4, and (b) a second peptide comprising the amino acid sequence of SEQ ID NO: 9, wherein said first and second peptides are cross-linked via a disulfide bond, and wherein said administering is effective to reduce cardiac tissue damage due to ischemia. ### Claim 4 (depends on 3) The method of claim 3, wherein said first peptide consists of the amino acid sequence of SEQ ID NO:4 and a terminal cysteine. ### Claim 5 A method for reducing cardiac tissue damage in a subject due to ischemia, comprising: administering to said subject a conjugate comprising (a) a first peptide consisting of the amino acid sequence of SEQ ID NO: 4 and a first terminal cysteine, and (b) a second peptide consisting of the amino acid sequence of SEQ ID NO: 9 and a second terminal cysteine, wherein the first and second peptides are cross-linked via a disulfide bond between the first and second terminal cysteine, and wherein said administering is effective to reduce cardiac tissue damage due to ischemia. ### Claim 6 A method for reducing cardiac tissue damage in a subject due to ischemia, comprising: administering to said subject a composition comprising a conjugate and a carrier or encapsulant, wherein said conjugate comprises (a) a peptide comprising the amino acid sequence of SEQ ID NO: 4, and (b) a transport moiety effective to facilitate transport across a cell membrane, wherein said peptide and transport moiety are linked, and wherein said administering is effective to reduce cardiac tissue damage due to ischemia. ### Claim 7 (depends on 6) The method of claim 6, wherein said peptide consists of the amino acid sequence of SEQ ID NO:4. ### Claim 8 A method for reducing cardiac tissue damage in a subject due to ischemia, comprising: administering to said subject a composition comprising a conjugate and a carrier or encapsulant, wherein said conjugate comprises (a) a first peptide comprising the amino acid sequence of SEQ ID NO: 4, and (b) a second peptide comprising the amino acid sequence of SEQ ID NO: 9, wherein the first and second peptides are cross-linked via a disulfide bond, and wherein said administering is effective to reduce cardiac tissue damage due to ischemia. ### Claim 9 (depends on 8) The method of claim 8, wherein said first peptide consists of the amino acid sequence of SEQ ID NO:4 and a terminal cysteine. ### Claim 10 A method for reducing cardiac tissue damage in a subject due to ischemia, comprising: administering to said subject a composition comprising a conjugate and a carrier or encapsulant, wherein said conjugate comprises (a) a first peptide consisting of the amino acid sequence of SEQ ID NO: 4 and a first terminal cysteine; and (b) a second peptide consisting of the amino acid sequence of SEQ ID NO: 9 and a second terminal cysteine, wherein the first and second peptides are cross-linked via a disulfide bond between the first and second terminal cysteine, and wherein said administering is effective to reduce cardiac tissue damage due to ischemia. ### Claim 11 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10) The method of any one of claims 1-10, wherein said administering comprises intravenously administering.