LU500790B1 - Molecular structure and synthesis method of a novel anti-triple-negative breast cancer drug - Google Patents
Molecular structure and synthesis method of a novel anti-triple-negative breast cancer drug Download PDFInfo
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- LU500790B1 LU500790B1 LU500790A LU500790A LU500790B1 LU 500790 B1 LU500790 B1 LU 500790B1 LU 500790 A LU500790 A LU 500790A LU 500790 A LU500790 A LU 500790A LU 500790 B1 LU500790 B1 LU 500790B1
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- var7
- phlip
- p1ap
- synthesis method
- breast cancer
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/001—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof by chemical synthesis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
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- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
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- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Gastroenterology & Hepatology (AREA)
- Biochemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
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- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
The present invention discloses the molecular structure and synthesis method of a novel anti- triple-negative breast cancer drug, the molecular structure is pHLIP(Var7)- P1AP, among which pHLIP(Var7)- AEEQNPWARYLEWLFPTETLLLELC, P1AP- CKKSRALF, the synthesis method is as follows: 1) synthesize pHLIP(Var7)Cys peptide sequence by solid-phase peptide synthesis method: AEEQNPWARYLEWLFPTETLLLELC; 2) synthesis of Cys P1AP peptide sequence by solid-phase peptide synthesis method: CKKSRALF; 3) pHLIP(Var7)Cys and CysP1AP are connected by disulfide bonds to obtain the pHLIP(Var7)- P1AP sequence: AEEQNPWARYLEWLFPTETLLLELC-CKKSRALF; the present invention can specifically insert the C-terminus of pHLIP(Var7)- P1AP into triple- negative breast cancer cells, the disulfide bonds cleavage release P1AP into tumor cells, P1AP can perform the intracellular part of the receptor through targeting tumor cells PAR1 to achieve the purpose of inhibiting tumor cells proliferation.
Description
BL-5317 LU500790
FIELD OF THE INVENTION The present invention relates to the technical field of chemical drugs, in particular to the molecular structure and synthesis method of a novel anti-triple-negative breast cancer drug.
BACKGROUND OF THE RELATED ART Triple-negative breast cancer (TNBC) refers to breast cancer that is negative for estrogen receptor (ER), progesterone receptor (PR), and epidermal growth factor receptor 2 (Her-2), accounting for all breast cancer patients 15%-20%. Triple-negative breast cancer (TNBC) has clinical characteristics such as strong invasiveness, rapid progress and poor prognosis. It is ineffective for endocrine therapy and targeted therapy commonly used in breast cancer treatment. Therefore, there is an urgent need to develop new therapeutic drugs for triple-negative breast cancer (TNBC) to improve treatment strategies.
SUMMARY OF THE INVENTION The technical problem to be solved by the present invention is to overcome the shortcomings of the above-mentioned technology and provide the molecular structure and synthesis method of a novel anti-triple-negative breast cancer drug.
In order to solve the above technical problems, the technical solution provided by the present invention is: the molecular structure and synthesis method of a novel anti-triple-negative breast cancer drug, the molecular structure is pHLIP(Var7) - PIAP, among which pHLIP(Var7) — AEEQNPWARYLEWLFPTETLLLELC, PIAP—CKKSRALF, the synthesis method is as follows:
BL-5317 1) synthesize pHLIP(Var7)Cys peptide sequence by solid-phase peptide synthesis method.” AEEQNPWARYLEWLFPTETLLLELC; 2) synthesis of Cys P1AP peptide sequence by solid-phase peptide synthesis method: CKKSRALF; 3) pHLIP(Var7)Cys and CysP1AP are connected by disulfide bonds to obtain the pHLIP(Var7)- P1AP sequence: AEEQNPWARYLEWLFPTETLLLELC-CKKSRALF, the present invention can specifically insert the C-terminus of pHLIP(Var7)- P1AP into triple- negative breast cancer cells, the disulfide bonds cleavage release P1AP into tumor cells, P1AP can perform the intracellular part of the receptor through targeting tumor cells PAR1 to achieve the purpose of inhibiting tumor cells proliferation.
BRIEF DESCRIPTION OF THE DRAWING Figure 1 is the HPLC(A) and ESI-MS(B) analysis of .(FITC) pHLIP(Var7)-P1AP.
Figure 2 is the positive expression of PAR] in triple-negative breast cancer MDA-MB-231 cells and negative PAR1 expression in MCF-10A cells (400 times).
Figure 3 is the fluorescence imaging of (FITC) pHLIP(Var7)-P1AP combined with MDA-MB- 231 cells (200 times).
Figure 4 is the effect of (FITC) pHLIP(Var7)-P1AP on the proliferation of MDA-MB-231 cells under different pH conditions.
DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENT In conjunction with Figures 1-4, the molecular structure and synthesis method of a novel anti- triple-negative breast cancer drug, the molecular structure is pHLIP(Var7)-P1AP, among which pHLIP(Var7)—AEEQNPWARYLEWLFPTETLLLELC, PIAP—CKKSRALF, the synthesis method is as follows: synthesize pHLIP(Var7)Cys peptide sequence by solid-phase peptide synthesis method: AEEQNPWARYLEWLFPTETLLLELC, synthesis of Cys P1AP peptide sequence by solid-phase peptide synthesis method: CKKSRALF; pHLIP(Var7)Cys and CysP1AP are connected by disulfide bonds to obtain the pHLIP(Var7)- P1AP
BL-5317 sequence: AEEQNPWARYLEWLFPTETLLLELC-CKKSRALF, 0500790 the present invention can specifically insert the C-terminus of pHLIP(Var7)- P1AP into triple- negative breast cancer cells, the disulfide bonds cleavage release P1AP into tumor cells, P1AP can perform the intracellular part of the receptor through targeting tumor cells PAR1 to achieve the purpose of inhibiting tumor cells proliferation.
The present invention and its embodiment are described above and this description is not restrictive. If a person of ordinary skill in the art receives its enlightenment and does not deviate from the purpose of the present invention, he/she can design a technical solution without any creativity. Similar embodiments should fall within the protection scope of the present invention.
Claims (1)
1. Molecular structure and synthesis method of a novel anti-triple-negative breast cancer drug, which is characterized in that : the molecular structure is pHLIP(Var7)-P1AP, among which pHLIP(Var7)— AEEQNPWARYLEWLFPTETLLLELC, PIAP—CKKSRALF, the synthesis method is as follows: 1) synthesize pHLIP(Var7)Cys peptide sequence by solid-phase peptide synthesis method: AEEQNPWARYLEWLFPTETLLLELC, 2) synthesis of Cys P1AP peptide sequence by solid-phase peptide synthesis method: CKKSRALF; 3) pHLIP(Var7)Cys and CysP1AP are connected by disulfide bonds to obtain the pHLIP(Var7)- P1AP sequence: AEEQNPWARYLEWLFPTETLLLELC-CKKSRALF.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| LU500790A LU500790B1 (en) | 2021-10-27 | 2021-10-27 | Molecular structure and synthesis method of a novel anti-triple-negative breast cancer drug |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| LU500790A LU500790B1 (en) | 2021-10-27 | 2021-10-27 | Molecular structure and synthesis method of a novel anti-triple-negative breast cancer drug |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| LU500790B1 true LU500790B1 (en) | 2022-04-27 |
Family
ID=81307123
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| LU500790A LU500790B1 (en) | 2021-10-27 | 2021-10-27 | Molecular structure and synthesis method of a novel anti-triple-negative breast cancer drug |
Country Status (1)
| Country | Link |
|---|---|
| LU (1) | LU500790B1 (en) |
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2021
- 2021-10-27 LU LU500790A patent/LU500790B1/en active IP Right Grant
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| FG | Patent granted |
Effective date: 20220427 |