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제125회 대한화학회 학술발표회 및 총회 Induced target degradation of BET by target degraducers(TDs)

등록일
2020년 2월 12일 15시 20분 53초
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1402
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발표분야
Medicinal Chemistry
저자 및
공동저자
Hyung Soo Kim, Pilho Kim1, Sung Yun Cho2, Jae du Ha2, Jong Yeon Hwang1,*
department of chemistry, Korea University, Korea
1Center for Medicinal Chemistry, Korea Research Institute of Chemical Technology, Korea
2WCI, Korea Research Institute of Chemical Technology, Korea
The anti-oncogenic property exhibiting drugs exemplified as immunomodulatory drugs (IMiDs) usually leads to the subsequent degradation of IKZF1/3. The anticancer pharmacology studies recently revealed their ability to degrade the E3 ubiquitin ligase by the novel trend of degradation named as proteolysis targeting chimera (PROTAC). BRD4 is the most commonly-targeted protein in PROTAC technology. Deregulation of Bromodomain and Extra-Terminal domain (BET) protein activity, such as that of BRD4, is observed in cancer and inflammatory diseases, there by making BET proteins attractive therapeutic targets. In the present study, we highlighted TD-428 comprising of TD-106 linked to BET inhibitor efficiently degrades BET cancer protein in 22RV1 cell line.

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