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학회명: 2009년도 한국분자•세포생물학회 정기학술대회 "RNA Biology and Disease"
주최기관: 한국분자•세포생물학회
기간: 2009.10.15-10.16
개최장소: 서울 코엑스 3층 컨퍼런스센터홀, 대서양홀8호
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[우수포스터 선정] 택산상역 우수포스터상 수상
Small-molecule-based approach reveals the requirement of armadillo reapeats for PKC α-mediated β-catenin phosphorylation/degradation
Jungsug Gwak, Hyuk Choi, Jae-Gook Shin, Sangtaek Oh
PharmcoGenomics Research Center, Inje University, Busan 614-735, Korea
The Wnt/β-catenin pathway is involved in diverse developmental processes and in oncogenesis. A key control of this pathway is the regulation of β-catenin activity, which depends on its intracellular protein level. The intracellular level of β-catenin is regulated predominantly by phosphorylation of the protein at its N-terminus (Ser33/37), leading to ubiquitin-dependent proteolysis. Here we show that SKL2001, which was identified by cell-based chemical screening, selectively inhibited the PKCα-mediated phosphorylation of β-catenin at Ser33/37 by displacing PKCα from β-catenin, leading to the stabilization of intracellular β-catenin. In addition, SKL2001, mimicking the activation of the Wnt/β-catenin pathway, promoted osteoblastogenesis and suppressed preadipocyte differentiation. |
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