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| Type |
Poster Presentation |
| Area |
의약화학 |
| Room No. |
포스터발표장 |
| Time |
4월 20일 (목요일) 11:00~12:30 |
| Code |
MEDI.P-446 |
| Subject |
Discovery of small molecule inhibitors of Bromodomain Protein controlling c-Myc for treatment of cancers |
| Authors |
유민진, 조석준1, 정관영2,*
과학기술연합대학원대학교(UST) 한국화학연구원/의약화학, Korea
1충북대학교 약학부, Korea
2한국화학연구원 의약화학연구센터, Korea
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| Abstract |
c-Myc is a regulator gene that codes for a transcription factor and overexpress in cancer cell. Indirect way of downregulation of c-Myc is the bromodomain inhibition. Bromodomain is a protein domain that recognizes acetylated lysine residues and control the c-Myc protein. We discovered 1H-indazole-4,7-dione scaffold using high throughput screening and synthesized a series of 1H-indazole-4,7-dione derivatives as a small molecule inhibitor of bromodomain protein. Among these synthesized small molecule inhibitors, 4H-1,2,4-triazolyl derivative represents the most potent inhibition effect toward c-Myc protein (IC50= 0.24 μM). The result suggest that 1H-indazole-4,7-dione scaffold would be potent bromodomain inhibitor. |
| E-mail |
yminjin10@gmail.com |
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119th General Meeting of the KCS