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Inhibitors for disrupting the interaction of ubiquitination related enzymes and uses thereof

An inhibitor, halogen technology for use in inhibitors for disrupting the interaction of enzymes associated with ubiquitination and fields of application thereof

Inactive Publication Date: 2009-11-18
WUHAN HUASUKANG BIOTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Misdegradation of proteins can lead to many serious diseases

Method used

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  • Inhibitors for disrupting the interaction of ubiquitination related enzymes and uses thereof
  • Inhibitors for disrupting the interaction of ubiquitination related enzymes and uses thereof
  • Inhibitors for disrupting the interaction of ubiquitination related enzymes and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0070] The new compound (NCE) Mol11 obtained by the method described above. Its chemical structure is as follows:

[0071]

[0072] The route of synthesis is shown below. The molecular weight was determined to be 294 by mass spectrometry. The results of H NMR are shown in image 3 .

[0073]

Embodiment 2

[0075] The new compound (NCE) Mol 21 was obtained by the method described previously. Its chemical structure is as follows:

[0076]

[0077] The route of synthesis is shown below. The molecular weight was 403 as determined by mass spectrometry. The results of H NMR are shown in Figure 4 .

[0078]

Embodiment 3

[0080]The new compound (NCE) Mol 44 was obtained by the method described previously. Its chemical structure is as follows:

[0081]

[0082] The route of synthesis is shown below. The molecular weight was 402 as measured by mass spectrometry. The results of H NMR are shown in Figure 5 .

[0083]

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PUM

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Abstract

A hydrophobic binding pocket on ubiquitin-protein ligase E3 is described, and used in designing the inhibitors disrupting ubiquitin conjugating enzyme E2 and E3 interaction. Four types of inhibitors designed by using the binding pocket are provided, which can be used for cancer treatment.

Description

technical field [0001] The present invention relates to structure-based drug design targeting the ubiquitination pathway, and the use of these compounds for cancer therapy. In particular, the invention relates to the identification of a class of E2-E3 inhibitors that precisely regulate protein-protein surface interactions. The compounds described in this invention and their analogs are protected by patents. [0002] This patent can be applied to the treatment of cancer and other diseases in mammals. The biochemical indicators of human beings quoted in this article are only for the convenience of understanding and are not limited to this. The term "patient, human body or human being" cited herein is also for convenience of description, and actually includes all mammalian diseases or bodies. Background technique [0003] Ubiquitin-mediated degradation is a protein regulatory mechanism that controls protein abundance at the post-translational level. It is a regulatory mecha...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/47C07D519/00C07D231/18C07D237/26C07D209/14A61K31/437A61K31/415A61K31/517A61K31/403A61P35/00G01N33/68C07D471/04C07D333/70
CPCC07D471/04A61K31/437C07D239/93C07D231/18C07D209/14A61K31/403A61K31/517A61K31/415A61P35/00A61P35/02A61P43/00
Inventor 黄岚李兴
Owner WUHAN HUASUKANG BIOTECH CO LTD