123rd General Meeting of the KCS

Type Poster Presentation
Area Life Chemistry
Room No. Exhibition Hall 2
Time 4월 19일 (금요일) 11:00~12:30
Code LIFE.P-370
Subject Synthesis of a Label-Free Föster Resonance Energy Transfer Probe for the Detection of Mouse double minute 2 homolog (MDM2) and B-cell lymphoma 2 (Bcl-2).
Authors A Ro Han, Sang Jeon Chung1,*
Sungkyunkwan University, Korea
1College of Pharmacy, SungKyunKwan University, Korea
Abstract Tumor suppressor is a key factor in cancer cell suppression and is present at a low concentration in normal cells. However, when normal cells receive a cellular stress, such as DNA damage or hypoxia, causes activation of various tumor suppressors. In conclusion, depending on the cellular stress and cell type, the activation of tumor suppressor can lead to various responses. One of the important tumor suppressors, p73 acts as a transcription factor, and is able to activate many genes to induce these specific functions and cancer suppression. p73 is an attractive therapeutic target in oncology because its tumor-suppressor activity can be stimulated to eradicate tumor cells. MDM2 is an important negative regulator of the p73 tumor suppressor. After binding to p73, it inhibits its transcriptional activity, favors its nuclear export and stimulates its degradation. The inhibition of the p73–MDM2 interaction is an attractive strategy to activate p73-mediated apoptosis in tumors with overexpressed MDM2. Another target is Bcl-2 that regulate cell death, by either inducing or inhibiting apoptosis. In this experiment, we synthesized probe in which a portion of the p73 peptide sequence was modified to detect MDM2 and Bcl-2. MDM2 and Bcl-2 play a crucial role in the regulation of cancer growth. Generally, the label-free detection probe emits the strong signal when target protein which is a tryptophan and a probe is closed. In this system, the phase of MDM2 or Bcl-2 with tryptophan and a probe is affected energy transfer efficiency. So, changing of florescent intensity give us the information which is the binding conformation & affinity of MDM2 or Bcl-2 toward the probe. The label free FRET-based probe can be used as a tool for novel drug screening of MDM2 and Bcl-2 oncogenic proteins.
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