화학공학소재연구정보센터
학회 한국공업화학회
학술대회 2016년 봄 (05/02 ~ 05/04, 여수 엑스포 컨벤션)
권호 20권 1호
발표분야 생물공학_포스터
제목 Generation of glycosylated macrolactam analogues through chemoenzymatic synthesis.
초록  Macrocyclic poliketides have been identified as rich sources of novel metabolites with promising therapeutic potentials. While the macrolactone plays a pivotal role in pharmacological acivity of the compounds, the susceptibility of this ring system to degradation by acidic PH, esterases, and various enzymes has increased our interest for analogue generation through structural modification. YC-17 is a macrolactone antibiotic produced from S. venezuelae and is composed of the polyketide macrolactone appended with a sugar moiety. Through a combined approach involving chemical synthesis and biotransformation, eight new analogues of YC-17 were generated. Some YC-17 analogues displayed enhanced activity against erythromycin resistant bacterial pathogens and improved metabolic stability in vitro. These results demonstrate the successful application of chemoenzymatic synthesis in therapeutic agents discovery and development.
저자 김면수, 김은지, 황재연, Cui Hequing, Jin Shi Ying, 정진아, 이나령, 윤여준
소속 이화여자대
키워드 macrolide glycosides; antibacterial activity
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