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03월 02일 17시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능
제109회 대한화학회 학술발표회, 총회 및 기기전시회 안내
Dissecting Biological Events using Molecular Diversity and Chemical Biology
2012년 3월 8일 14시 38분 25초
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목 09시 : 30분
KCS-RSC joint symposium- Chemical Biology
서울대학교 화학부, Korea
A study of 9-aryl-1,2-dihydropyrrolo[3,4-b]indolizin-3-one, we name it Seoul-Fluor, were presented in this presentation. During our continuous efforts on the construction of drug-like small-molecule libraries using diversity-oriented synthesis (DOS) strategy, we identified a novel fluorescent core skeleton, 1,2-dihydropyrrolo[3,4-b]indolizin-3-one. Guiding with computational simulation, 24 fluorescent compounds library were constructed in combinatorial fashion, and which covers the full-color range. Further bioapplication of these fluorescent compounds was successfully demonstrated in the immunofluorescent staining. After discovery of Seoul-Fluor, we analyzed the fluorescent core skeleton more systematically and extensively. Using a concise and practical one-pot synthetic procedure, a 44-member library of new fluorescent compounds was synthesized. The systematic perturbation of electronic densities on the specific positions of Seoul-Fluor, guided with the Hammett constant, allows tuning the emission wavelength in full-color range. Furthermore, on the basis of these observations and a computational analysis, we extracted a simple first-order correlation of emission wavelength with the theoretical calculation and accurately predicted the emission wavelength of Seoul-Fluors prior to their synthesis. Therefore, we clearly demonstrated that Seoul-Fluor could provide a powerful gateway for the generation of desired fluorescent probes without the need for tiresome synthesis and trial-and-error process. In addition, we developed a new technology platform, fluorescence difference in two-dimensional gel electrophoresis (FITGE), which aims to preserve protein-small molecule interactions under the intact cellular environment. We also demonstrated its application for the target identification of a new antitumor agent screened from our in-house small-molecule library. After a series of failures using conventional target ID methods, we successfully identified the protein target of anti-proliferative compound 1 with FITGE only under the live cell condition and observed the environment-dependent binding events of a functional small molecule by direct comparison between live cells and cell lysates. Even though it still requires the synthesis of bioactive probes with photo-crosslinker moiety, the FITGE strategy can address the current limitation of conventional target identification methods and significantly enhance the possibility of target ID via covalent capturing of target proteins under the intact cellular environment and the efficient exclusion of nonspecific protein labelling using two-color 2DGE. We believe our FITGE strategy can provide a unique technology platform for target identification in live cells.
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