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| Type |
Poster Presentation |
| Area |
Medicinal Chemistry |
| Room No. |
Event Hall |
| Time |
4월 19일 (목요일) 11:00~12:30 |
| Code |
MEDI.P-628 |
| Subject |
Regulation of AIMP2-DX2, oncogenic splicing variant using small molecule |
| Authors |
Srigouri Huddar, Chul Min Park1,*, Sunkyung Lee1
Medicinal Chemistry and pharmacology, University of Science & Technology, Korea
1Center for Medicinal Chemistry, Korea Research Institute of Chemical Technology, Korea
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| Abstract |
Aminoacyl-tRNA synthetase-interacting multifunctional protein 2 (AIMP2) is a potent tumor suppressor inducing apoptosis upon various signals. AIMP2-DX2, an exon2-deleted splicing variant of AIMP2, is upregulated in several cancer cells and competitively suppresses the pro-apoptotic activity of AIMP2 resulting in tumorigenesis. We identified that a series of hydrazone derivatives inhibited the expression of AIMP2-DX2. Herein, we report that 1) how new scaffolds were designed and validated; 2) optimization process through syntheses and evaluation of derivatives; 3) structure-activity relationship (SAR) analysis of a series of compounds; 4) profiles of validated hits. Additionally we disclose the results of in vivo assay.
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| E-mail |
srigouri.huddar@gmail.com |
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121st General Meeting of the KCS