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제114회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Development of a simple ANS-based displacement assay for the characterization of druggability

등록일
2014년 8월 26일 11시 51분 45초
접수번호
0230
발표코드
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발표시간
10월 15일 (수요일) 16:00~19:00
발표형식
포스터
발표분야
분석화학
저자 및
공동저자
이주운, Jin Hyung Lee1, Eun Jeong Cho2,*
한국교통대학교 교양학부 - 화학, Korea
1Emory University, Atlanta, GA, USA, United States
2University of Texas at Austin, Austin, TX, USA, United States
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승인 2건
Development of a simple, inexpensive, robust, and high throughput method to characterize promiscuous drug candidates is described. The method utilizes a fluorescent probes, 1,8-anilinonaphthalene-8-sulfonate (ANS), in which its inherent fluorescence intensity increases upon binding to protein targets. The fluorescence signal diminution when they are displaced by small competing chemicals provides a quantitative tool to compare, or rank, non-specific binding affinity and is therefore directly applicable to assess druggability of chemical compounds. As a proof of principle, 446 chemical compounds from NIH clinical collection were screened and the displacement activity was evaluated. Most compounds did not show significant activities against ANS displacement. This result demonstrated that comparative biological analysis on non-specific binging affinities allows us to quickly examine druggability of small molecules and prioritization of compounds from commercial or house-produced libraries at very early drug development stage. Key words: Fluorescence, displacement, high throughput screening, drug, promiscuous inhibitors

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