APE1 inhibitor and application thereof in preparation of drugs for treatment of tumors and vascular poliferative diseases

A technology of vascular abnormalities and inhibitors, applied in the fields of biochemistry, etiology, and molecular biology, can solve the problems of short-term curative effect and inability to fundamentally cure diseases, etc., and achieve the effect of easy synthesis, good drug characteristics, and simple structure

Active Publication Date: 2017-09-22
SUN YAT SEN UNIV
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Problems solved by technology

Direct use of VEGF antagonists can only produce short-t...

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  • APE1 inhibitor and application thereof in preparation of drugs for treatment of tumors and vascular poliferative diseases
  • APE1 inhibitor and application thereof in preparation of drugs for treatment of tumors and vascular poliferative diseases
  • APE1 inhibitor and application thereof in preparation of drugs for treatment of tumors and vascular poliferative diseases

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Embodiment Construction

[0068] The present invention will be further described below in conjunction with drawings and embodiments.

[0069] 1. Interaction between C10 and APE1

[0070] The inventors used a computer to screen the small molecule compound library in Guangdong, and found a small molecule C10 with a completely different structure from the existing APE1 inhibitors. E3330 is a now recognized APE1 inhibitor. We compare each other with C10 and E3330 in the specific implementation process. First, we evaluated the small molecule compound C10 and its interaction with APE1 in vitro. C10 can lower the melting temperature of APE1 by 1.3 degrees, compared to E3330, which can lower the melting temperature of APE1 by 1 degree, and C10 can destabilize the protein structure of APE1 ( figure 1 A). C10 can cause APE1 protein to deflect light at a drug concentration of 10 μM, while E3330 can deflect light at a concentration of 500 mM ( figure 1 B). The affinity constant of C10 and APE1 is 170nM, and ...

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Abstract

The invention belongs to the fields of molecular biology, biochemistry and etiology, and discloses an APE1 inhibitor and application thereof in the preparation of drugs for the treatment of tumors and vascular poliferative diseases. The APE1 inhibitor has a structure shown in a following formula 1, by inhibiting the activity of the redox end of APE1, the formation process of tumors is inhibited from several aspects at the same time, compared with an existing APE1 inhibitor E3330, it is presented that the APE1 inhibitor is lower in cytotoxicity and has higher antiviral activity, antiangiogenic activity and anti-cell invasion activity and the like. The APE1 inhibitor has great application prospects on the treatment of various malignant tumors such as Kaposi's sarcoma, osteosarcoma, pancreatic cancers, bladder cancers, ovarian cancers and other cancers, and other abnormal vascular proliferative diseases such as age-related macular degeneration. The formula 1 is shown in the description.

Description

technical field [0001] The invention belongs to the fields of molecular biology, biochemistry and etiology, and specifically relates to an APE1 inhibitor and its application in the preparation of drugs for treating related tumors and abnormal blood vessel proliferation diseases that depend on the redox end function of APE1. Background technique [0002] Apurinic apyrimidinic endonuclease / redox factor (APE-1) is an extremely important intracellular bifunctional protein. Its C-terminal participates in base excision repair after DNA mismatch; N-terminal contains redox activity, which can reduce the inactive transcription factor in the oxidized state to the active transcription factor in the reduced state, and the active transcription factor can bind to the downstream DNA The promoter sequence of the gene promotes the expression of downstream genes, which has an important impact on cell proliferation, apoptosis and differentiation. The downstream regulated transcription factors...

Claims

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Application Information

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IPC IPC(8): A61K31/341A61P35/00A61P27/02
CPCA61K31/341
Inventor 袁岩徐峻
Owner SUN YAT SEN UNIV
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