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  • 09월 10일 16시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

제124회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Identification of new human targets of antibiotics toward drug repositioning

2019년 9월 2일 18시 38분 32초
MEDI.O-5 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
목 10시 : 00분
Medicinal Chemistry - Oral Presentation of Young Discovery Chemists
저자 및
Sung Min Cho, Ho Jeong Kwon1,*
Biotechnology, Yonsei University, Korea
1Department of Biotechnology, Yonsei University, Korea
Drug repositioning saves the time and cost of drug development in difficulties of FDA approval. It is a promising approach reducing risk of side effects because it is already approved drugs. In this study, reverse chemical proteomics enables access to new targets and pathways of existing drugs targeting anti-infectious disases. Here are two case compounds of Artesunate (ART) and Daptomycin (DAP). Both ART and DAP are the most potent and safe antimalarial and antibacterial drugs, respectively. Despite their clinical potential, no human target for them are known. The unbiased interrogation of several human cDNA libraries, displayed on bacteriophage T7, revealed a high affinity human target of them; the Bcl-2 antagonist of cell death promoter (BAD) and ribosomal protein S19 (RPS19), respectively. ART inhibits the phosphorylation of BAD, promoting the formation of the BAD/Bcl-xL complex and the subsequent intrinsic apoptosis. In addition, DAP exhibits selective growth inhibition of some cell lines, particularly MCF7 and HUVECs. This ability of DAP is due to regulate the expression of cell growth related cytokines such as VEGF and EGF, resulting in suppressed tumour invasion. Collectively, these two case studies of reverse chemical proteomics demonstrate the potential of drug repositioning of antibiotics to anticancer drugs.