# US 10,308,682 B2 · Inhibition of tumor growth with aggregates of small molecules > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 10,308,682 B2 - Document ID: US10308682B2 - Status: Granted - Kind: B2 - Application number: 14/773,690 - Filed: 2014-03-06 - Published: 2016-01-21 - Granted: 2019-06-04 - Earliest claimed: 2013-03-06 - Assignees: Brandeis University - Applicants: Brandeis University - Inventors: Bing Xu; Yi Kuang - Web page: https://patentgrep.com/patent/US10308682B2 ## CPC - C07K 5/06121: {the second amino acid being aromatic or cycloaliphatic} - A61K 31/195: having an amino group - A61P 35/00: Antineoplastic agents - 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) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS ## Abstract Disclosed herein are fibrillar molecular aggregates, which are morphologically and phenotypically similar to oligomers of aberrant proteins. The molecular aggregates, formed by self-assembly of small hydrophobic molecules, prevent the growth of microtubules. This unprecedented mechanism of “self-assembly to interfere with self-organization” allows inhibition of the growth of cancer cells. ## Claims ### Claim 1 A method of treating cancer, comprising the step of: administering to a subject in need thereof a plurality of hydrophobic, self-assembling monomers of Formula (I): wherein independently for each occurrence: is naphthyl; R is H or alkyl; R1 is substituted or unsubstituted aralkyl or heteroaralkyl; R2 is H, alkyl, —OR, or —NR2; and n is 2, 3, 4, 5, or 6; wherein R1 is an unsubstituted aralkyl for at least one of said R1 groups and R1 is a substituted aralkyl or substituted heteroarylalkyl for at least one of said R1 groups; and wherein the cancer is selected from the group consisting of cervical carcinoma, hepatocarcinoma, glioblastoma, breast carcinoma, pancreatic carcinoma, and uterine sarcoma. ### Claim 2 (depends on 1) The method of claim 1, wherein the cancer is glioblastoma. ### Claim 3 (depends on 1) The method of claim 1, wherein the hydrophobic, self-assembling monomer comprises a dipeptide. ### Claim 4 (depends on 1) The method of claim 1, wherein R is H. ### Claim 5 (depends on 1) The method of claim 1, wherein R1 is substituted aralkyl for at least one of said R1 groups. ### Claim 6 (depends on 1) The method of claim 1, wherein R1 is hydroxyaralkyl for at least one of said R1 groups. ### Claim 7 (depends on 1) The method of claim 1, wherein R1 is benzyl for at least one of said R1 groups. ### Claim 8 (depends on 1) The method of claim 1, wherein R1 is substituted benzyl for at least one of said R1 groups. ### Claim 9 (depends on 1) The method of claim 1, wherein R1 is hydroxybenzyl for at least one of said R1 groups. ### Claim 10 (depends on 1) The method of claim 1, wherein R1 is 4-hydroxybenzyl for at least one of said R1 groups. ### Claim 11 (depends on 1) The method of claim 1, wherein R2 is —OR or —NR2. ### Claim 12 (depends on 1) The method of claim 1, wherein R2 is —OR. ### Claim 13 (depends on 1) The method of claim 1, wherein R2 is —OH. ### Claim 14 (depends on 1) The method of claim 1, wherein n is 2, 3, 4, or 5. ### Claim 15 (depends on 1) The method of claim 1, wherein n is 3, 4, 5, or 6; and R1 is benzyl for two of said R1 groups. ### Claim 16 (depends on 1) The method of claim 1, wherein the monomers of Formula (I) are present at a concentration of 200 μM or greater. ### Claim 17 (depends on 1) The method of claim 1, wherein the monomers of Formula (I) are present at a concentration of 200 μM to 600 μM. ### Claim 18 A method of treating cancer, comprising the step of: administering to a subject in need thereof a plurality of hydrophobic, self-assembling monomers, wherein the hydrophobic, self-assembling monomer is wherein the cancer is selected from the group consisting of cervical carcinoma, hepatocarcinoma, glioblastoma, breast carcinoma, pancreatic carcinoma, and uterine carcinoma.