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Molecular structure and synthesis method of new triple negative breast cancer drug

A triple-negative breast cancer and molecular structure technology, which is applied in drug combinations, antineoplastic drugs, and pharmaceutical formulations, can solve problems such as poor prognosis and achieve the effect of inhibiting tumor cell proliferation

Inactive Publication Date: 2020-06-23
THE AFFILIATED HOSPITAL OF QINGDAO UNIV
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Problems solved by technology

Triple-negative breast cancer (TNBC) has clinical characteristics such as aggressiveness, rapid progression, and poor prognosis, and is ineffective for endocrine therapy and targeted therapy commonly used in breast cancer treatment, so it is urgent to develop new treatments for triple-negative breast cancer (TNBC) Drugs, Improved Treatment Strategies

Method used

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  • Molecular structure and synthesis method of new triple negative breast cancer drug
  • Molecular structure and synthesis method of new triple negative breast cancer drug
  • Molecular structure and synthesis method of new triple negative breast cancer drug

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Embodiment Construction

[0013] combined with Figure 1-4 , a molecular structure and a synthetic method of a novel anti-triple negative breast cancer drug, the molecular structure is pHLIP (Var7)-P1AP, wherein pHLIP (Var7)—AEEQNPWARYLEWLFPTETLLLELC, P1AP—CKKSRALF, and the synthetic method is as follows:

[0014] 1) Synthesize the pHLIP (Var7) Cys polypeptide sequence by solid-phase peptide synthesis: AEEQNPWARYLEWLFPTETLLLELC;

[0015] 2) Synthesize Cys P1AP polypeptide sequence by solid-phase peptide synthesis method: CKKSRALF;

[0016] 3) pHLIP(Var7)Cys and CysP1AP are linked by a disulfide bond to obtain the pHLIP(Var7)-P1AP sequence: AEEQNPWARYLEWLFPTETLLLELC-CKKSRALF.

[0017] The present invention can specifically insert the C-terminus of pHLIP(Var7)-P1AP into triple-negative breast cancer cells, the disulfide bond is cleaved to release P1AP into tumor cells, and P1AP can target the intracellular part of tumor cell PAR1 receptor , to achieve the purpose of inhibiting tumor cell proliferation....

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Abstract

The invention discloses a molecular structure and a synthesis method of a new triple negative breast cancer drug. The molecular structure is pHLIP (Var7)-P1AP, wherein pHLIP (Var7)-AEEQNPWARYLEWLFPTETLLLELC and P1AP-CKKSRALF are synthesized by the steps of 1) synthesizing a pHLIP (Var7) Cys polypeptide sequence through a solid-phase polypeptide synthesis method: AEEQNPWARYLEWLFPTETLLLELC; 2) synthesizing a Cys P1AP polypeptide sequence through a solid-phase polypeptide synthesis method: CKKSRALF; and 3) enabling the pHLIP (Var7) Cys to be connected with the Cys P1AP through a disulfide bond toobtain the pHLIP (Var7)-P1AP sequence: AEEQNPWARYLEWLFPTETLLLELC-CKKSRALF. The C end of the pHLIP (Var7)-P1AP can be specifically inserted into triple negative breast cancer cells, the disulfide bondcracks to release P1AP to tumor cells, and P1AP can be targeted to the internal parts of tumor cell PAR1 recipient cells to achieve the purpose of inhibiting tumor cell proliferation.

Description

technical field [0001] The invention relates to the technical field of chemical medicines, in particular to the molecular structure and synthesis method of a novel anti-triple-negative breast cancer medicine. Background technique [0002] 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), and accounts for all breast cancer patients. 15% to 20%. Triple-negative breast cancer (TNBC) has clinical characteristics such as aggressiveness, rapid progression, and poor prognosis, and is ineffective for endocrine therapy and targeted therapy commonly used in breast cancer treatment, so it is urgent to develop new treatments for triple-negative breast cancer (TNBC) Drugs, Improved Treatment Strategies. Contents of the invention [0003] The technical problem to be solved by the present invention is to overcome the defects of the above-mentioned technolog...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/00C07K7/06A61K38/16A61P35/00
CPCA61K38/00A61P35/00C07K7/06C07K14/00
Inventor 于明明陈月华王振光李大成杨光杰
Owner THE AFFILIATED HOSPITAL OF QINGDAO UNIV
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