# US 10,441,624 B2 · Application of dipeptide as ace enzyme activity inhibitor

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- Number: US 10,441,624 B2
- Document ID: US10441624B2
- Status: Granted
- Kind: B2
- Application number: 15/503,328
- Filed: 2014-08-11
- Published: 2018-07-26
- Granted: 2019-10-15
- Earliest claimed: 2014-08-11
- Assignees: Withyou Biotechnology Co., Ltd.
- Applicants: Withyou Biotechnology Co., Ltd.
- Inventors: Xionglei He; Wei Zhu
- Web page: https://patentgrep.com/patent/US10441624B2

## CPC

- A61K 38/05: Dipeptides
- A61K 38/55: Protease inhibitors
- A61K 38/556: {Angiotensin converting enzyme inhibitors}
- A61P 9/12: Antihypertensives
- 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

An application of dipeptide as an ACE enzyme activity inhibitor. Virtual screening is performed on 400 types of dipeptide based on ACE inhibiting effects thereof according to a detected ACE enzyme crystal structure by using self-developed software and adopting a molecular docking method, experiments are conducted to verify the ACE inhibitory activity of the dipeptide obtained by virtual screening, and it finds out that the dipeptide with the N terminal as cysteine has better ACE inhibitory activity.

## Claims

### Claim 1

A method of inhibiting an ACE enzyme by exposing the ACE enzyme to an ACE enzyme activity inhibitor, wherein the ACE enzyme activity inhibitor is a dipeptide, wherein said dipeptide is selected from the group consisting of CA, CH, CI, or CK;
the N-terminal of the dipeptide is a cysteine, the amino acid in the dipeptide is in L-form or D-form, and at least one amino acid in the dipeptide is optionally modified with a group which can improve the stability of the dipeptide in vivo;
wherein the C-terminal amino acid of the dipeptide is a basic amino acid or an aliphatic amino acid;
wherein the basic amino acid is H or K; and
wherein the aliphatic amino acid is A or I.

### Claim 2 (depends on 1)

The method according to claim 1, wherein the ACE enzyme activity inhibitor is administered to a patient to lower blood pressure.