# US 2014/0155331 A1 · Novel high affinity bivalent helically constrained peptide against cancer > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 2014/0155331 A1 - Document ID: US20140155331A1 - Status: Published application - Kind: A1 - Application number: 13/980,701 - Filed: 2012-01-30 - Published: 2014-06-05 - Earliest claimed: 2011-01-31 - Assignees: Council of Scientific and Industrial Research - Inventors: Amlanjyoti Dhar; Shampa Mallick; Israr Ahmed; Aditya Konar; Santu Bandyopadhyay; Siddhartha Roy - Web page: https://patentgrep.com/patent/US20140155331A1 ## CPC - A61K 38/16: Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof {(enzyme inhibitors A61K38/005)} - A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)} - A61K 38/10: Peptides having 12 to 20 amino acids {(A61K38/043 - A61K38/046 take precedence)} - A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca - C07K 14/00: Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof - C07K 14/47: from mammals - 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) - 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 describes a novel bivalent helically constrained peptide targeted against S100B that is an effective anti-cancer drug against cancers that over-express S100B. This helix mimetic targeted against S100B induces rapid apoptosis in cancer cells that over-express a calcium binding protein S100B through simultaneous inhibition of key growth pathways including activation of p53. ## Claims ### Claim 1 A novel high affinity bivalent helically constrained peptide against cancer, wherein the said peptide is represented by SEQ ID No. 4-Lysine-SEQ ID No. 4 and having the following general formula: ### Claim 2 (depends on 1) A peptide as claimed in claim 1, wherein it has enhanced cell penetrability relative to the corresponding unmodified peptides represented by SEQ ID No. 3-Lysine-SEQ ID No. 3 and SEQ ID No. 5-Lysine-SEQ ID No. 5. ### Claim 3 (depends on 1) A peptide as claimed in claim 1, wherein it comprises of one or more helix stabilizing amino acids and two parallel helices. ### Claim 4 (depends on 1) A peptide as claimed in claim 1, useful for the treatment of human cancers having over-expression of S100B and/or down regulation of p53 including but not limited to melanoma, glioma and sarcoma. ### Claim 5 (depends on 1) A pharmaceutical composition comprising a therapeutically effective amount of the novel high affinity bivalent helically constrained peptide as claimed in claim 1 as an active ingredient optionally along with at least one pharmaceutically acceptable peptide stabilizer and excipients. ### Claim 6 (depends on 5) A composition as claimed in claim 5, further comprising at least one approved chemotherapeutic agent. ### Claim 7 (depends on 5) A composition as claimed in claim 5, wherein the said composition comprises 20% to 80% (w/w) of the bi-helical peptidomimetic represented by SEQ ID No. 4-Lysine-SEQ ID No. 4. ### Claim 8 (depends on 5) A composition as claimed in claim 5, wherein the said composition is formulated for oral, parental, subcutaneous, intravenous or intra-articular administration. ### Claim 9 (depends on 5) A composition as claimed in claim 5, wherein the said composition is administered in the dosage of approximately 50 mg/kg body weight per day for a period of 1 to 7 days. ### Claim 10 (depends on 5, 6, 7, 8, 9) A composition as claimed in claims 5 to 9, useful for the treatment of human cancers having over-expression of S100B and/or down regulation of p53 including but not limited to melanoma, glioma and sarcoma. ### Claim 11 (depends on 5, 6, 7, 8, 9) A composition as claimed in claims 5 to 9, wherein the said composition is useful for inducing rapid apoptosis within 1 to 6 hours in a group of cancers having wild-type p53 which is down-regulated by S100B. ### Claim 12 (depends on 5) Use of the composition as claimed in the claim 5 for the manufacture of a medicament for the treatment of S100B over-expressing and/or p53 under-expressing human cancers. ### Claim 13 (depends on 5) A method for the treatment of human cancers having over-expression of S100B and/or down-regulation of p53 comprising administering a therapeutically effective amount of the composition as claimed in claim 5 to a patient in need thereof. ### Claim 14 (depends on 13) A method as claimed in claim 13, wherein the composition is administered parenterally, subcutaneously, intravenously or intraarticularly. ### Claim 15 (depends on 13) A method as claimed in claim 13, wherein the composition is administered in a dosage of about 50 mg/kg body weight per day for a period of 1 to 7 days. ### Claim 16 (depends on 13) A method as claimed in claim 13, wherein the composition is administered in conjunction with a standard method of care including chemotherapy, radiation therapy and surgery.