Fragment-Based Drug Discovery of 2-Thiazolidinoes as BRD4 Inhibitors : Structure – Based Optimization 2014/04/03 Jun Min Jung.

Presentation on theme: "Fragment-Based Drug Discovery of 2-Thiazolidinoes as BRD4 Inhibitors : Structure – Based Optimization 2014/04/03 Jun Min Jung."— Presentation transcript:

1 Fragment-Based Drug Discovery of 2-Thiazolidinoes as BRD4 Inhibitors : Structure – Based Optimization 2014/04/03 Jun Min Jung

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3 Abstract

4 Introduction

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6 Chemistry R1NH2 = Cyclopentanamine

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8 Chemistry R1NH2 = Cyclopentanamine

9 Chemistry

10 Chemistry

11 Chemistry

12 Chemistry

13 Chemistry

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15 Chemistry

16 Results & Discussion Initial Optimization

17 Initial Optimization

18 Structure – Activity relationships

19 Structure – Activity relationships

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21 Structure – Activity relationships

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24 Effects on c-myc protein and mrna expression

25 Western Blot Southern blotting Northern blotting
Western blotting(Immunoblotting)은 antigenic epitope과 반응하는 antibody를 이용하여 항원- 항체 반응을 일으킴으로써 단백질 혼합물 중에서 원하는 특정단백질(antigen)만을 찾아내는 방법 이다 Southern blotting DNA molecules을 agarose gel로부터 membrane으로 옮긴 후, 특정적인 DNA sequence를 probe로 사용하여 detection해내는 방법 Northern blotting Northern blot은 Southern blot과 같은 원리이며, DNA 대신 특정한 RNA detection하는 방법이다.

26 In vitro Metabolic stability assessment

27 Thank you