# US 9,434,933 B2 · Crystal

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- Number: US 9,434,933 B2
- Document ID: US9434933B2
- Status: Granted
- Kind: B2
- Application number: 14/297,500
- Filed: 2014-06-05
- Published: 2014-12-25
- Granted: 2016-09-06
- Earliest claimed: 2006-01-10
- Assignees: Angiodesign (UK) Ltd.
- Applicants: University of Bath; University of Cape Town
- Inventors: Ravi Acharya; Edward Sturrock
- Web page: https://patentgrep.com/patent/US9434933B2

## CPC

- C12N 9/485: {Exopeptidases (3.4.11-3.4.19)}
- A61K 38/4813: {Exopeptidases (3.4.11. to 3.4.19)}
- C07K 14/70596: {Molecules with a "CD"-designation not provided for elsewhere}
- C12N 9/48: acting on peptide bonds (3.4)
- C12Q 1/37: involving peptidase or proteinase
- C12Y 304/15001: Peptidyl-dipeptidase A (3.4.15.1)
- 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 2299/00: Coordinates from 3D structures of peptides, e.g. proteins or enzymes
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)
- 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)
- 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)
- C12Q: MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS (immunoassay G01N33/53); COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
- C12Y: ENZYMES

## Abstract

The present invention relates to a crystal. In particular the present invention relates to a crystal of the N-domain of ACE protein. The present invention also relates to methods, processes, domain specific modulators, pharmaceutical compositions and uses of the N-domain crystal and the structure co-ordinates thereof.

## Claims

### Claim 1

A crystal of an N-Domain of ACE protein wherein the crystal belongs to the space group C2221, or wherein the crystal has the unit cell dimensions: a=101.12 Å, b=211.32 Å, c=171.27 Å, where in the N-domain consists of amino acids 1-629 of SEQ ID NO: 4.

### Claim 2 (depends on 1)

A crystal according to claim 1 wherein the N-domain of ACE protein is glycosylated with less than ten sugar moieties at amino acids 25, 45, 117, 289 and 480 of SEQ ID NO: 4.

### Claim 3 (depends on 1)

A crystal according to claim 1 wherein the crystal further comprises a ligand bound to the N domain of the ACE protein.

### Claim 4 (depends on 3)

A crystal according to claim 3 wherein the ligand is bound to the N-domain of the ACE protein by contacting one or more residues of the N-domain of the ACE protein selected from: Gln259, Lys489, Tyr498 of SEQ ID NO: 4.

### Claim 5 (depends on 3)

A crystal according to claim 3 wherein the ligand is an inhibitor of the N-domain of ACE protein.

### Claim 6 (depends on 5)

A crystal according to claim 5 wherein the inhibitor of ACE is lisinopril, captopril or a derivative thereof.