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  • 05월 20일 18시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

제125회 대한화학회 학술발표회 및 총회 Preparation and Biological Evaluations of Cell-penetrating peptide Mediated Drug Conjugate for Cancer Therapy

2020년 5월 20일 16시 35분 32초
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Organic Chemistry
저자 및
Tejinder Singh, Jungkyun Im*
Department of Chemical Engineering, Soonchunhyang University, Korea
Gene therapy has been perceived as one of the most potential approaches in the field of cancer treatment. Camptothecin (CPT) and its derivatives have been found to uniquely inhibit the catalytic activity of mammalian DNA topoisomerase I, which is responsible for DNA breakage and subsequent apoptosis. In vitro analyses revealed that CPT-induced topoisomerase I was covalently linked to the 3' end of the broken DNA. Despite CPT’s high rates of clinical responses, its utilization has been restricted due to extremely poor solubility, which contributes to their low bioavailability, enhanced toxicity, and lack of target specificity. Therefore, to tackle these issues, through rational drug design we assembled a novel cell-penetrating peptide (CPP), and the drug, CPT. CPPs could facilitate the penetration of various drugs through diverse pathways and this conjugation strategy is perceived to be very effective for improved efficacy. The drug conjugate was characterized by analytical techniques such as proton NMR, carbon-13 NMR, and MALDI-TOF. A further analysis evaluating its biological features is under process.