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Discovery of PROTAC...
Discovery of PROTAC molecules that selectively degrade the IRAK3 pseudokinase
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Degorce, Sebastien L (author)
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Tavana, Omid (author)
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Banks, Erica (author)
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Crafter, Claire (author)
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Gingipalli, Lakshmaiah (author)
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Kouvchinov, David (author)
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- Mao, Yumeng (author)
- Bioscience, Research and Early Development, Oncology R&D, AstraZeneca, Cambridge Science Park, Unit 310 Darwin Building, Cambridge CB4 0WG, U.K.
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Pachl, Fiona (author)
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Solanki, Anisha (author)
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Valge-Archer, Viia (author)
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Yang, Bin (author)
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Edmondson, Scott (author)
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Bioscience, Research and Early Development, Oncology R&D, AstraZeneca, Cambridge Science Park, Unit 310 Darwin Building, Cambridge CB4 0WG, UK. (creator_code:org_t)
- 2020-08-17
- 2020
- English.
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In: Journal of Medicinal Chemistry. - : American Chemical Society (ACS). - 0022-2623 .- 1520-4804. ; 63:18, s. 10460-10473
- Related links:
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
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- We report the first disclosure of IRAK3 degraders in the scientific literature. Taking advantage of an opportune by-product obtained during our efforts to identify IRAK4 inhibitors, we identified ready to use, selective IRAK3 ligands in our compound collection with the required properties for conversion into PROTAC degraders. This work culminated with the discovery of PROTAC 23, which we demonstrated to be a potent and selective degrader of IRAK3. 23 induced proteasome-dependent degradation of IRAK3 and required both CRBN and IRAK3 binding for activity. We conclude that PROTAC 23 constitutes an excellent in vitro tool with which to interrogate the biology of IRAK3.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Läkemedelskemi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Medicinal Chemistry (hsv//eng)
Publication and Content Type
- ref (subject category)
- art (subject category)
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- By the author/editor
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Degorce, Sebasti ...
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Tavana, Omid
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Banks, Erica
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Crafter, Claire
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Gingipalli, Laks ...
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Kouvchinov, Davi ...
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show more...
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Mao, Yumeng
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Pachl, Fiona
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Solanki, Anisha
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Valge-Archer, Vi ...
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Yang, Bin
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Edmondson, Scott
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show less...
- About the subject
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Basic Medicine
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and Medicinal Chemis ...
- Articles in the publication
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Journal of Medic ...
- By the university
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Uppsala University