# US 12,595,288 B2 · Vasopressin-2 receptor antagonist peptides and uses thereof > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 12,595,288 B2 - Document ID: US12595288B2 - Status: Granted - Kind: B2 - Application number: 18/002,625 - Filed: 2021-06-23 - Published: 2023-07-27 - Granted: 2026-04-07 - Earliest claimed: 2020-06-24 - Assignees: Commissariat A L'energie Atomique Et Aux Energies Alternatives - Applicants: Commissariat A L'energie Atomique Et Aux Energies Alternatives - Inventors: Nicolas Gilles; Justyna Ciolek; Laura Droctove; Bernard Maillere; Herve Nozach - Web page: https://patentgrep.com/patent/US12595288B2 ## CPC - C07K 14/46: from vertebrates - A61K 38/17: from animals; from humans {(enzyme inhibitors A61K38/005)} - C12N 15/63: Introduction of foreign genetic material using vectors; Vectors; Use of hosts therefor; Regulation of expression - G01N 33/5008: {for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics} - 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) - G01N 2333/72: for hormones - G01N 2333/726: G protein coupled receptor, e.g. TSHR-thyrotropin-receptor, LH/hCG receptor, FSH - 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) - C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00) - G01N: INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES (measuring or testing apparatus or processes other than immunoassay, involving enzymes or microorganisms C12M, C12Q) ## Abstract A peptide may include a sequence having 80% or more amino acid identity with the amino acid sequence of SEQ ID NO. 1, i.e., RPSX1CNLPVKPGPCX2GFFSAFYYSQKX3NKCHSFTYGGCAGNANRFSTX4EKCRRTC X5X6, wherein, X1 is the amino acid residue F or G, X2 is any amino acid residue, except a basic amino acid residue, X3 is the amino acid residue T or D, X4 is the amino acid residue I, L, or E, (i) X5 is V and X6 is G or (ii) X5 is G and X6 is V, and the amino acid located at position 39 is A. Such peptides may have various diagnostic and therapeutic uses. ## Claims ### Claim 1 A peptide comprising the amino acid sequence that is at least 80% identical to the amino acid sequence set forth below: (SEQ ID NO: 1) RPSX1CNLPVKPGPCX2GFFSAFYYSQKX3NKCHSFTYGGCAGNANRFST X4EKCRRTCX5X6, wherein: X1 is F or G; X2 is any amino acid residue except K, R or H; X3 is T or D; X4 is I, L or E; (i) X5 is V and X6 is G, or (ii) X5 is G and X6 is V; and wherein the alanine at position 39 of SEQ ID NO: 1 in the peptide is unsubstituted. ### Claim 2 (depends on 1) The peptide of claim 1, wherein X1 is G. ### Claim 3 (depends on 1) The peptide of claim 1, wherein X2 is selected from the group consisting of A, D, E, F, G, I, L, N, M, Q, S, T, V and Y. ### Claim 4 (depends on 1) The peptide of claim 1, wherein X3 is D. ### Claim 5 (depends on 1) The peptide of claim 1, wherein X4 is E or L. ### Claim 6 (depends on 1) The peptide of claim 1, wherein X4 is L. ### Claim 7 (depends on 1) The peptide of claim 1, wherein the peptide comprises the amino acid sequence of SEQ ID NO: 1. ### Claim 8 (depends on 1) The peptide of claim 1, wherein the peptide comprises the amino acid sequence selected from the group consisting of SEQ ID NOS: 2-6. ### Claim 9 (depends on 1) The peptide of claim 1, wherein the peptide is conjugated to a detectable molecule. ### Claim 10 (depends on 1) A pharmaceutical composition comprising a peptide of claim 1 and a pharmaceutically acceptable carrier. ### Claim 11 (depends on 8) A method of inhibiting type 2 vasopressin receptor (V2R) activity in a subject in need thereof, wherein the method comprises administering to the subject a peptide of claim 8. ### Claim 12 (depends on 8) A method of treating a disease in a subject in need thereof, wherein the method comprises administering to the subject a peptide of claim 8, and wherein the disease is selected from the group consisting of euvolemic hyponatremia, hypovolemic hyponatremia polycystic kidney disease, refractory liver disease, and heart failure. ### Claim 13 A method for detecting one or more cells expressing vasopressin-2 receptor, wherein the method comprises contacting the cell in vitro with a conjugate comprising a detectable molecule linked to a peptide comprising the amino acid sequence selected from the group consisting of SEQ ID NOs: 2-6. ### Claim 14 A method for detecting a dysregulation of vasopressin-2 receptor expression of a cell, wherein the method comprises: (a) contacting the cell in vitro with a conjugate comprising a detectable molecule linked to a peptide comprising the amino acid sequence selected from the group consisting of SEQ ID NOs: 2-6; (b) measuring the expression level of vasopressin-2 receptor expression of the cell; (c) comparing the expression level obtained in the measuring (b) with a reference expression level; and (d) determining an occurrence of a dysregulation of vasopressing-2 receptor expression.