# US 10,766,926 B2 · Composition for autophagy inhibiting in cell, and pharmaceutical composition for preventing or treating tumor disease, or inhibiting anti-cancer agents resistance containing the same > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 10,766,926 B2 - Document ID: US10766926B2 - Status: Granted - Kind: B2 - Application number: 15/780,347 - Filed: 2018-05-28 - Published: 2020-03-19 - Granted: 2020-09-08 - Earliest claimed: 2018-04-23 - Assignees: L-Base Co., Ltd. - Applicants: L-Base Co., Ltd - Inventors: Do Yong Jeon; Chang Hoon Moon; Ji Eun Jung - Web page: https://patentgrep.com/patent/US10766926B2 ## CPC - C07K 7/06: having 5 to 11 amino acids - A61P 35/00: Antineoplastic agents - 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) - 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) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS - 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 Provided are a polypeptide having the activity of inhibiting autophagy in a cell, a composition for inhibiting autophagy in a cell, and particularly in a tumor cell, containing the polypeptide as an active ingredient, and a pharmaceutical composition containing the polypeptide, and more specifically, a composition for inhibiting autophagy in a cell containing a polypeptide inhibiting the control mechanism of autophagy as an active ingredient, and a pharmaceutical composition for preventing or treating a neoplastic disease or for inhibiting resistance to anticancer agents, containing the polypeptide. ## Claims ### Claim 1 A method of inhibiting autophagy in a cell, comprising administering to the cell a polypeptide consisting of the amino acid sequence of X3-X1-T-X1-K—X2, wherein, T is threonine, K is lysine; X1 is alanine, isoleucine, or proline; X2 is alanine, or threonine; and X3 is glutamine-threonine, glycine-asparagine-threonine, or serine. ### Claim 2 (depends on 1) The method of claim 1, wherein X1 and X2 are alanine. ### Claim 3 (depends on 1) The method of claim 1, wherein X1 is proline; and X2 is threonine. ### Claim 4 (depends on 1) The method of claim 1, wherein X1 is isoleucine; and X2 is threonine. ### Claim 5 (depends on 1) The method of claim 1, wherein X3 is glutamine-threonine. ### Claim 6 (depends on 1) The method of claim 1, wherein X3 is serine. ### Claim 7 (depends on 1) The method of claim 1, wherein X3 is glycine-asparagine-threonine. ### Claim 8 (depends on 1) The method of claim 1, wherein the polypeptide inhibits autophagy in a cell by reducing the expression of at least one protein selected from the group consisting of p-AMPK, ATG5-ATG12, Beclin1, p-Beclin1, LC3-I, and LC3-II. ### Claim 9 (depends on 1) The method of claim 1, wherein the polypeptide inhibits autophagy in a cell by increasing the expression of p-mTOR or p62 protein. ### Claim 10 (depends on 1) The method of claim 1, wherein the polypeptide is labeled with any one labeling material selected from the group consisting of chromogenic enzymes, radioisotopes, chromophores, luminescent materials, fluorescers, magnetic resonance imaging (MRI) materials, super paramagnetic particles, and ultrasuper paramagnetic particles. ### Claim 11 (depends on 1) The method of claim 1, wherein the cell is a tumor cell. ### Claim 12 A method for treating a neoplastic disease comprising administering to a subject in need thereof a pharmaceutical compositing comprising a polypeptide consisting of the amino acid sequence of X3-X1-T-X1-K-X2, wherein, T is threonine, K is lysine; X1 is alanine, isoleucine, or proline X2 is alanine, or threonine; and X3 is glutamine-threonine, glycine-asparagine-threonine, or serine. ### Claim 13 (depends on 12) The method of claim 12, wherein the neoplastic disease is selected from the group consisting of lung cancer, liver cancer, colon cancer, pancreatic cancer, stomach cancer, breast cancer, ovarian cancer, kidney cancer, thyroid cancer parathyroid cancer, esophageal cancer, prostate cancer, brain cancer, skin cancer, osteosarcoma, soft tissue sarcoma, glioma, lymphoma, nasopharyngeal cancer, larynx cancer, adrenal gland cancer, colon carcinoma, ureteral cancer, gallbladder cancer, bladder cancer, testis cancer, uterine cervical cancer, endometrial cancer, choriocarcinoma, head and neck cancer, malignant melanoma, leukemia, multiple myeloma, chronic myeloid leukemia, neuroblastoma, and aplastic anemia. ### Claim 14 A method for inhibiting resistance to anticancer agents, comprising a polypeptide consisting of the amino acid sequence of X3-X1-T-X1-K—X2, wherein T is threonine, K is lysine; X1 is alanine, isoleucine, or proline X2 is alanine, or threonine; and X3 is glutamine-threonine, glycine-asparagine-threonine, or serine. ### Claim 15 (depends on 14) The method of claim 14, wherein the composition has resistance to at least one anticancer agent selected from the group consisting of erlotinib, celastrol, cisplatin, docetaxel, osimertinib, taxol, pemetrexed, and tamoxifen.