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Application of human PCID2 protein in preparation or screening of antitumor drugs and compound with antitumor activity

A technology of anti-tumor drugs and compounds, applied in the field of compounds with anti-tumor activity, can solve the problems of lack of specific functional targets, structural optimization of efficient antagonists, etc., to inhibit the proliferation of liver cancer cells and promote the apoptosis of liver cancer cells death effect

Pending Publication Date: 2022-05-03
THE FIRST HOSPITAL OF LANZHOU UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, the development of multi-target natural small molecule inhibitors is a promising direction for tumor molecular targeted therapy, but due to the lack of specific functional targets, the structural optimization of highly effective antagonists is impossible

Method used

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  • Application of human PCID2 protein in preparation or screening of antitumor drugs and compound with antitumor activity
  • Application of human PCID2 protein in preparation or screening of antitumor drugs and compound with antitumor activity
  • Application of human PCID2 protein in preparation or screening of antitumor drugs and compound with antitumor activity

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Embodiment 1 antitumor compound and tumor suppression experiment

[0026] 1. Screening of antitumor compounds

[0027] (1) Crystal structure determination of PCID2 domain and PCID2-DSS1 complex

[0028] Human PCID2 combines with disordered protein DSS1 (26S proteasome complex subunit, 26S proteasome complex subunit) (referred to as PCID2-DSS1 complex) to maintain the stability of PCID2 protein structure. This embodiment has determined the crystal structure of the PCID2 structural domain and the PCID2-DSS1 complex, and the results are as follows figure 1 As shown, the WH (winged helix) domain is the main interaction site and one of the important functional regions of the PCID2 protein.

[0029] (2) Preparation of virtual compound library

[0030] Using shape similarity methods (such as ROCS) and fingerprint similarity methods, screening from existing small molecule databases (SPECS, ChemDiv, and TCMD, etc.), at the three substitution positions of the chalcone parent, ...

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Abstract

The invention belongs to the technical field of biotechnology and gene therapy, and particularly relates to application of human PCID2 protein in preparation or screening of anti-tumor drugs and an anti-tumor compound. It is found that the PCID2 gene promotes tumor cell proliferation and regulates the cell cycle, is a key molecule for regulating tumor generation and development, and can be used as a target protein for preparing or screening anti-tumor drugs; meanwhile, human PCID2 protein is used as target protein, a class of PCID2 protein targeting antitumor compounds are screened out through a molecular docking technology, and the compounds can significantly inhibit tumor cell proliferation and promote tumor cell apoptosis.

Description

[0001] This case is a divisional application of the original application, original patent number: 2021103641290; original patent name: application of human PCID2 protein in the preparation or screening of anti-tumor drugs and compounds with anti-tumor activity; original application date: April 3, 2021 . technical field [0002] The invention belongs to the technical field of new targets for cancer precision medicine and drugs, and specifically relates to the application of human PCID2 protein in the preparation or screening of anti-tumor drugs and the compound with anti-tumor activity. Background technique [0003] Tumor is a disease in which cell damage or malignant transformation leads to infinite proliferation. Liver cancer is one of the most common malignant tumors. Every year, new liver cancer cases in my country account for more than 50% of the world's total. The onset of liver cancer is hidden, the early symptoms are not obvious, and the rate of intrahepatic and extr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C49/84C07C205/45A61P35/00
CPCA61P35/00C07C49/84C07C205/45
Inventor 白仲添张保新席莉莉周建业
Owner THE FIRST HOSPITAL OF LANZHOU UNIV
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