Novel BRD4 protein targeted degradation agent as well as preparation method and application thereof
The invention discloses a novel BRD4 protein targeted degradation agent as well as a preparation method and application thereof. Belongs to the field of pharmaceutical chemistry. An activity test result shows that the novel PROTAC molecule for targeted degradation of the BRD4 directly degrades the BRD4 protein by utilizing a ubiquitin-proteasome way, the degradation efficiency is remarkable, tumor cells highly expressed by the BRD4 protein can be directly killed, and the effect is superior to that of a positive control drug (+)-JQ-1. Meanwhile, the PROTAC molecules can avoid the regulation of the feedback increase of the target protein content caused by the application of the conventional small-molecule inhibitor (+)-JQ-1 of the BRD4..
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Patent| Erscheinungsjahr: |
2024 |
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| Erschienen: |
2024 |
| Enthalten in: |
Europäisches Patentamt - (2024) vom: 19. Jan. Zur Gesamtaufnahme - year:2024 |
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| Sprache: |
Englisch |
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| Beteiligte Personen: |
QIAN HAI [VerfasserIn] |
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| Links: |
Volltext [kostenfrei] |
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| Anmerkungen: |
Source: www.epo.org (no modifications made), First posted: 2024-01-19, Last update posted on www.tib.eu: 2024-05-06, Last updated: 2024-05-10 |
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| Patentnummer: |
CN117417338 |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
EPA002622475 |
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| 520 | |a The invention discloses a novel BRD4 protein targeted degradation agent as well as a preparation method and application thereof. Belongs to the field of pharmaceutical chemistry. An activity test result shows that the novel PROTAC molecule for targeted degradation of the BRD4 directly degrades the BRD4 protein by utilizing a ubiquitin-proteasome way, the degradation efficiency is remarkable, tumor cells highly expressed by the BRD4 protein can be directly killed, and the effect is superior to that of a positive control drug (+)-JQ-1. Meanwhile, the PROTAC molecules can avoid the regulation of the feedback increase of the target protein content caused by the application of the conventional small-molecule inhibitor (+)-JQ-1 of the BRD4. | ||
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