# US 11,110,107 B2 · Methods for treatment of cancer by targeting SIRT5

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- Number: US 11,110,107 B2
- Document ID: US11110107B2
- Status: Granted
- Kind: B2
- Application number: 16/414,912
- Filed: 2019-05-17
- Published: 2019-10-03
- Granted: 2021-09-07
- Earliest claimed: 2011-09-07
- Assignees: Cornell University
- Applicants: Cornell University
- Inventors: Hening Lin
- Web page: https://patentgrep.com/patent/US11110107B2

## CPC

- A61K 31/7016: Disaccharides, e.g. lactose, lactulose (lactobionic acid A61K31/7032)
- A61K 31/198: Alpha-amino acids, e.g. alanine or edetic acid [EDTA] (betaine A61K31/205; proline A61K31/401; tryptophan A61K31/405; histidine A61K31/4172; peptides not degraded to individual amino acids A61K38/00)
- A61K 31/702: Oligosaccharides, i.e. having three to five saccharide radicals attached to each other by glycosidic linkages
- A61K 31/7088: Compounds having three or more nucleosides or nucleotides
- A61K 31/713: Double-stranded nucleic acids or oligonucleotides
- A61K 38/02: Peptides of undefined number of amino acids; Derivatives thereof
- A61K 38/03: Peptides having up to 20 amino acids in an undefined or only partially defined sequence; Derivatives thereof
- A61K 38/1709: {from mammals}
- A61P 35/00: Antineoplastic agents
- C07K 7/06: having 5 to 11 amino acids
- C07K 14/47: from mammals
- C12N 9/1077: {Pentosyltransferases (2.4.2)}
- C12N 15/1137: {against enzymes (viral enzymes C12N15/1131; receptors C12N15/1138)}
- C12Y 204/02: Pentosyltransferases (2.4.2)
- 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)
- C12N 2310/14: interfering nucleic acids [NA]
- C12Y 305/01098: Histone deacetylase (3.5.1.98), i.e. sirtuin deacetylase
- 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)
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)
- C12Y: ENZYMES

## Abstract

This disclosure demonstrates that inhibition of Sirt5 can suppress malignant transformation of cells. Therefore, methods of treating cancer based on inhibition of Sirt5 are disclosed.

## Claims

### Claim 1

A compound that inhibits Sirt5 demalonylase or desuccinylase activity, having the formula:
wherein:
R1 is a carboxylate alkyl ester;
R2 is S;
X0, X1, X2, X3, X6, and X7 are each —CH2—;
X4 is —NR5—, wherein R5 is H, methyl, ethyl, isopropyl, phenyl, or benzyl;
X5 is —CH2— or —NR5—;
R3 and R4 are independently selected from H, hydrocarbon (R), amino acid, dipeptide, tripeptide, oligopeptide, protein, nucleobase, nucleotide, dinucleotide, trinucleotide, oligonucleotide, monosaccharide, disaccharide, oligosaccharide, and protecting groups or a combination thereof or modified form thereof.

### Claim 2 (depends on 1)

The compound of claim 1, wherein X5 is —CH2—.

### Claim 3 (depends on 1)

The compound of claim 1, wherein R3 and R4 are independently selected from amino acid, dipeptide, tripeptide, oligopeptide, and protein.

### Claim 4 (depends on 1)

The compound of claim 1, wherein the compound is H3K9 thiosuccinyl peptide.

### Claim 5 (depends on 1)

The compound of claim 1, wherein X5 is —NR5—.