121st General Meeting of the KCS

Type Poster Presentation
Area Medicinal Chemistry
Room No. Event Hall
Time 4월 19일 (목요일) 11:00~12:30
Code MEDI.P-644
Subject Induced degradation of cereblon (CRBN) by a proteolysis targeting chimera (PROTAC)
Authors Yeong Uk Jeon, Jong Yeon Hwang1,*, PILHO KIM1, jae du ha2, Sung Yun Cho2
pharmacy, Sungkyunkwan University, Korea
1Center for Medicinal Chemistry, Korea Research Institute of Chemical Technology, Korea
2WCI, Korea Research Institute of Chemical Technology, Korea
Abstract Recently, a new and powerful technology called “proteolysis targeting chimeras” (PROTACs) has been actively applied in the field of drug development. PROTAC strategy employs the protein degradation machinery of the cell ; the ubiquitin-proteasome pathway. Proteins removed via this pathway are targeted for degradation by the attachment of a polyubiquitin chain leading to their recognition and subsequent degradation by the 26S proteasome. The PROTAC molecule consist of a ligand, which binds an E3 ubiquitin ligase, connected by a linker to another ligand that binds the target protein. The association between a protein and an E3 ligase, as induced by a PROTAC molecule, will lead to the transfer of ubiquitin and degradation of the targeted protein. As part of our efforts to develop novel PROTAC-based small molecule inhibitors, we were interested in CRBN as a targeted protein due to its distinct role in cells. Here we report the synthesis and activities of pomalidomide-based CRBN degraders.
E-mail duddnr1701@naver.com