# US 10,117,903 B1 · Method for regulating cancer stem cell growth by inhibiting phosphorylation of 120th threonine residue of TSPYL5 protein, a composition containing the peptide sequence functioning to inhibit the phosphorylation and a use thereof > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 10,117,903 B1 - Document ID: US10117903B1 - Status: Granted - Kind: B1 - Application number: 15/774,208 - Filed: 2017-06-15 - Published: 2018-11-08 - Granted: 2018-11-06 - Earliest claimed: 2016-06-15 - Assignees: Korea Atomic Energy Research Institute - Applicants: Korea Atomic Energy Research Institute - Inventors: In Gyu Kim; Seo Yeon Kim; Jei Ha Lee; Soo Im Choi; Min Sik Kim; Jung Yul Kim; Byungchul Shin; Uhee Jung - Web page: https://patentgrep.com/patent/US10117903B1 ## CPC - A61K 38/02: Peptides of undefined number of amino acids; Derivatives thereof - A61P 35/04: specific for metastasis - C07K 7/08: having 12 to 20 amino acids (gastrins C07K14/595; somatostatins C07K14/655; melanotropins C07K14/68) - C07K 14/4702: {Regulators; Modulating 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) - 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 - 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) ## Abstract The present invention relates to a peptide suppressing the phosphorylation of threonine (T120), the 120th residue of TSPYL5 (testis-specific Y-like protein 5), which is specifically as follows. The present inventors constructed T120D, the mutant of the 120th residue threonine (T120) of TSPYL5, and T120A-TSPYL5 gene and then transfected cells with them in order to investigate the effect of phosphorylation on T120 residue. As a result, wild-type TSPYL5 and T120D moved into nucleus and stayed there. But in the case of T120A-TSPYL5, TSPYL5 did not move into nucleus and instead it was expressed only in cytoplasm. The protein could not bind to AKT, either. Instead, ubiquitination of TSPYL5 was increased but SUMOylation was inhibited. Also, the expressions of ALDH1-A1, -A3, CD44 gene and protein were reduced, and thereby the growth and metastasis of lung cancer cells were suppressed and sphere formation was reduced. Based on the observation above, the inventors constructed the peptide composed of the amino acid sequences represented by SEQ. ID. NO: 43 or NO: 44 that could inhibit phosphorylation of the 120th residue threonine of TSPYL5. The said peptide can be effectively used as a composition for the inhibition of cancer cell growth, metastasis, and cancer stem cell growth. ## Claims ### Claim 1 A peptide composed of the amino acid sequence of SEQ ID NO: 43 or SEQ ID NO: 44. ### Claim 2 (depends on 1) The peptide according to claim 1, wherein the peptide inhibits TSPYL5 (testis-specific protein, Y-encoded like 5) expressing cancer cell proliferation, metastasis, or sphere formation. ### Claim 3 (depends on 1) The peptide according to claim 1, wherein the peptide inhibits the phosphorylation of the 120th amino acid of TSPYL5. ### Claim 4 (depends on 1) The peptide according to claim 1, wherein the peptide accelerates ubiquitination but inhibits SUMOylation of TSPYL5. ### Claim 5 (depends on 1) A method for preventing or treating TSPYL5 expressing cancer, comprising administering to a patient in need thereof a therapeutically effective amount of the peptide of claim 1 as an active ingredient. ### Claim 6 (depends on 1) A method for preventing the reoccurrence of or inhibiting TSPYL5 expressing cancer metastasis, comprising administering to a patient in need thereof a therapeutically effective amount of the peptide of claim 1. ### Claim 7 (depends on 1) A method for inhibiting the growth of TSPYL5 expressing cancer stem cells comprising administering to a patient in need thereof a therapeutically effective amount of the peptide of claim 1. ### Claim 8 (depends on 7) The method of claim 7, wherein the TSPYL5 expressing cancer stem cell is selected by one of the cancer stem cell selection markers selected from the group consisting of CD133 (prominin-1; AC133), CD44 (hyaluronate receptor; P glycoprotein 1), and ALDH1 (Aldehyde dehydrogenase 1).