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| Type |
Poster Presentation |
| Area |
Medicinal Chemistry |
| Room No. |
Exhibition Hall 2 |
| Time |
4월 18일 (목요일) 11:00~12:30 |
| Code |
MEDI.P-382 |
| Subject |
Induced target degradation of BET by target degraducers(TDs) |
| Authors |
AhRa Go, Jae du Ha1, Jong Yeon Hwang*, Yeong Uk Jeon2, Pilho Kim, Sung Yun Cho1, Chunghoon Shin3, Hyung Soo Kim4, WooRi Lee5
Center for Medicinal Chemistry, Korea Research Institute of Chemical Technology, Korea
1WCI, Korea Research Institute of Chemical Technology, Korea
2pharmacy, Sungkyunkwan University, Korea
3organic chemistry, Sogang University, Korea
4organic chemistry, Korea University, Korea
5Drug discovery, Chungnam National University, Korea
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| Abstract |
Immunomodulatory drugs (IMiDs) exert anti-myeloma activity by binding to the protein cereblon (CRBN) and subsequently degrading IKZF1/3. Recently, their ability to recruit E3 ubiquitin ligase has been used in the proteolysis targeting chimera (PROTAC) technology. Of these, BRD4 is the most commonly-targeted protein in PROTAC technology. Herein, we synthesize the TD-428, which comprises TD-106 linked to a BET inhibitor, JQ1 efficiently induce BET protein degradation in the prostate cancer cell line 22Rv1. Consequently, cell proliferation is inhibited due to suppressed C-MYC transcription. |
| E-mail |
rhrkfk@hanmail.net |
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123rd General Meeting of the KCS